-
2
-
-
66249144426
-
The structure and function of G-protein-coupled receptors
-
Rosenbaum, D. M., Rasmussen, S. G., and Kobilka, B. K. (2009) The structure and function of G-protein-coupled receptors Nature 459, 356-363
-
(2009)
Nature
, vol.459
, pp. 356-363
-
-
Rosenbaum, D.M.1
Rasmussen, S.G.2
Kobilka, B.K.3
-
3
-
-
84912544840
-
Portraying G protein-coupled receptors with fluorescent ligands
-
Ciruela, F., Jacobson, K. A., and Fernández-Dueñas, V. (2014) Portraying G protein-coupled receptors with fluorescent ligands ACS Chem. Biol. 9, 1918-1928
-
(2014)
ACS Chem. Biol.
, vol.9
, pp. 1918-1928
-
-
Ciruela, F.1
Jacobson, K.A.2
Fernández-Dueñas, V.3
-
4
-
-
84883036652
-
Class A G-protein-coupled receptor (GPCR) dimers and bivalent ligands
-
Hiller, C., Kuhhorn, J., and Gmeiner, P. (2013) Class A G-protein-coupled receptor (GPCR) dimers and bivalent ligands J. Med. Chem. 56, 6542-6559
-
(2013)
J. Med. Chem.
, vol.56
, pp. 6542-6559
-
-
Hiller, C.1
Kuhhorn, J.2
Gmeiner, P.3
-
6
-
-
0034604451
-
Crystal structure of rhodopsin: A G protein-coupled receptor
-
Palczewski, K., Kumasaka, T., Hori, T., Behnke, C. A., Motoshima, H., Fox, B. A., Trong, I. L., Teller, D. C., Okada, T., Stenkamp, R. E., Yamamoto, M., and Miyano, M. (2000) Crystal structure of rhodopsin: A G protein-coupled receptor Science 289, 739-745
-
(2000)
Science
, vol.289
, pp. 739-745
-
-
Palczewski, K.1
Kumasaka, T.2
Hori, T.3
Behnke, C.A.4
Motoshima, H.5
Fox, B.A.6
Trong, I.L.7
Teller, D.C.8
Okada, T.9
Stenkamp, R.E.10
Yamamoto, M.11
Miyano, M.12
-
7
-
-
79953234218
-
Crystal structure of metarhodopsin II
-
Choe, H. W., Kim, Y. J., Park, J. H., Morizumi, T., Pai, E. F., Krauss, N., Hofmann, K. P., Scheerer, P., and Ernst, O. P. (2011) Crystal structure of metarhodopsin II Nature 471, 651-655
-
(2011)
Nature
, vol.471
, pp. 651-655
-
-
Choe, H.W.1
Kim, Y.J.2
Park, J.H.3
Morizumi, T.4
Pai, E.F.5
Krauss, N.6
Hofmann, K.P.7
Scheerer, P.8
Ernst, O.P.9
-
8
-
-
36448995359
-
High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor
-
Cherezov, V., Rosenbaum, D. M., Hanson, M. A., Rasmussen, S. G., Thian, F. S., Kobilka, T. S., Choi, H. J., Kuhn, P., Weis, W. I., Kobilka, B. K., and Stevens, R. C. (2007) High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor Science 318, 1258-1265
-
(2007)
Science
, vol.318
, pp. 1258-1265
-
-
Cherezov, V.1
Rosenbaum, D.M.2
Hanson, M.A.3
Rasmussen, S.G.4
Thian, F.S.5
Kobilka, T.S.6
Choi, H.J.7
Kuhn, P.8
Weis, W.I.9
Kobilka, B.K.10
Stevens, R.C.11
-
9
-
-
84930868579
-
GPCR crystal structures: Medicinal chemistry in the pocket
-
DOI
-
Shonberg, J., Kling, R. C., Gmeiner, P., and Löber, S. GPCR crystal structures: Medicinal chemistry in the pocket. Bioorg. Med. Chem. 2014, DOI: 10.1016/j.bmc.2014.12.034.
-
(2014)
Bioorg. Med. Chem.
-
-
Shonberg, J.1
Kling, R.C.2
Gmeiner, P.3
Löber, S.4
-
10
-
-
80051658642
-
Crystal structure of the beta2 adrenergic receptor-Gs protein complex
-
Rasmussen, S. G., DeVree, B. T., Zou, Y., Kruse, A. C., Chung, K. Y., Kobilka, T. S., Thian, F. S., Chae, P. S., Pardon, E., Calinski, D., Mathiesen, J. M., Shah, S. T., Lyons, J. A., Caffrey, M., Gellman, S. H., Steyaert, J., Skiniotis, G., Weis, W. I., Sunahara, R. K., and Kobilka, B. K. (2011) Crystal structure of the beta2 adrenergic receptor-Gs protein complex Nature 477, 549-555
-
(2011)
Nature
, vol.477
, pp. 549-555
-
-
Rasmussen, S.G.1
Devree, B.T.2
Zou, Y.3
Kruse, A.C.4
Chung, K.Y.5
Kobilka, T.S.6
Thian, F.S.7
Chae, P.S.8
Pardon, E.9
Calinski, D.10
Mathiesen, J.M.11
Shah, S.T.12
Lyons, J.A.13
Caffrey, M.14
Gellman, S.H.15
Steyaert, J.16
Skiniotis, G.17
Weis, W.I.18
Sunahara, R.K.19
Kobilka, B.K.20
more..
-
11
-
-
84864221004
-
A new era of GPCR structural and chemical biology
-
Granier, S. and Kobilka, B. (2011) A new era of GPCR structural and chemical biology Nat. Chem. Biol. 8, 670-673
-
(2011)
Nat. Chem. Biol.
, vol.8
, pp. 670-673
-
-
Granier, S.1
Kobilka, B.2
-
12
-
-
78651399683
-
Structure and function of an irreversible agonist-beta(2) adrenoceptor complex
-
Rosenbaum, D. M., Zhang, C., Lyons, J. A., Holl, R., Aragao, D., Arlow, D. H., Rasmussen, S. G., Choi, H. J., Devree, B. T., Sunahara, R. K., Chae, P. S., Gellman, S. H., Dror, R. O., Shaw, D. E., Weis, W. I., Caffrey, M., Gmeiner, P., and Kobilka, B. K. (2011) Structure and function of an irreversible agonist-beta(2) adrenoceptor complex Nature 469, 236-240
-
(2011)
Nature
, vol.469
, pp. 236-240
-
-
Rosenbaum, D.M.1
Zhang, C.2
Lyons, J.A.3
Holl, R.4
Aragao, D.5
Arlow, D.H.6
Rasmussen, S.G.7
Choi, H.J.8
Devree, B.T.9
Sunahara, R.K.10
Chae, P.S.11
Gellman, S.H.12
Dror, R.O.13
Shaw, D.E.14
Weis, W.I.15
Caffrey, M.16
Gmeiner, P.17
Kobilka, B.K.18
-
13
-
-
84861096654
-
Crystal structure of the mu-opioid receptor bound to a morphinan antagonist
-
Manglik, A., Kruse, A. C., Kobilka, T. S., Thian, F. S., Mathiesen, J. M., Sunahara, R. K., Pardo, L., Weis, W. I., Kobilka, B. K., and Granier, S. (2012) Crystal structure of the mu-opioid receptor bound to a morphinan antagonist Nature 485, 321-326
-
(2012)
Nature
, vol.485
, pp. 321-326
-
-
Manglik, A.1
Kruse, A.C.2
Kobilka, T.S.3
Thian, F.S.4
Mathiesen, J.M.5
Sunahara, R.K.6
Pardo, L.7
Weis, W.I.8
Kobilka, B.K.9
Granier, S.10
-
14
-
-
84904704143
-
Covalent agonists for studying G protein-coupled receptor activation
-
Weichert, D., Kruse, A. C., Manglik, A., Hiller, C., Zhang, C., Hübner, H., Kobilka, B. K., and Gmeiner, P. (2014) Covalent agonists for studying G protein-coupled receptor activation Proc. Natl. Acad. Sci. U.S.A. 111, 10744-10748
-
(2014)
Proc. Natl. Acad. Sci. U.S.A.
, vol.111
, pp. 10744-10748
-
-
Weichert, D.1
Kruse, A.C.2
Manglik, A.3
Hiller, C.4
Zhang, C.5
Hübner, H.6
Kobilka, B.K.7
Gmeiner, P.8
-
15
-
-
0023945272
-
Identification and sequence of a binding site peptide of the beta2-adrenergic receptor
-
Dohlman, H. G., Caron, M. G., Strader, C. D., Amlayki, M., and Lefkowitz, R. J. (1988) Identification and sequence of a binding site peptide of the beta2-adrenergic receptor Biochemistry 27, 1813-1817
-
(1988)
Biochemistry
, vol.27
, pp. 1813-1817
-
-
Dohlman, H.G.1
Caron, M.G.2
Strader, C.D.3
Amlayki, M.4
Lefkowitz, R.J.5
-
16
-
-
0028087860
-
Acetylcholine mustard labels the binding site aspartate in muscarinic acetylcholine receptors
-
Spalding, T. A., Birdsall, N. J., Curtis, C. A., and Hulme, E. C. (1994) Acetylcholine mustard labels the binding site aspartate in muscarinic acetylcholine receptors J. Biol. Chem. 269, 4092-4097
-
(1994)
J. Biol. Chem.
, vol.269
, pp. 4092-4097
-
-
Spalding, T.A.1
Birdsall, N.J.2
Curtis, C.A.3
Hulme, E.C.4
-
17
-
-
56049101882
-
Ligand-binding architecture of human CB2 cannabinoid receptor: Evidence for receptor subtype-specific binding motif and modeling GPCR activation
-
Pei, Y., Mercier, R. W., Anday, J. K., Thakur, G. A., Zvonok, A. M., Hurst, D., Reggio, P. H., Janero, D. R., and Makriyannis, A. (2008) Ligand-binding architecture of human CB2 cannabinoid receptor: evidence for receptor subtype-specific binding motif and modeling GPCR activation Chem. Biol. (Cambridge, MA, U. S.) 15, 1207-1219
-
(2008)
Chem. Biol. (Cambridge, MA, U. S.)
, vol.15
, pp. 1207-1219
-
-
Pei, Y.1
Mercier, R.W.2
Anday, J.K.3
Thakur, G.A.4
Zvonok, A.M.5
Hurst, D.6
Reggio, P.H.7
Janero, D.R.8
Makriyannis, A.9
-
18
-
-
0345259510
-
Chloroethylclonidine binds irreversibly to exposed cysteines in the fifth membrane-spanning domain of the human α2A-adrenergic receptor
-
Marjamaki, A., Pihlavisto, M., Cockcroft, V., Heinonen, P., Savola, J.-M., and Scheinin, M. (1998) Chloroethylclonidine binds irreversibly to exposed cysteines in the fifth membrane-spanning domain of the human α2A-adrenergic receptor Mol. Pharmacol. 53, 370-376
-
(1998)
Mol. Pharmacol.
, vol.53
, pp. 370-376
-
-
Marjamaki, A.1
Pihlavisto, M.2
Cockcroft, V.3
Heinonen, P.4
Savola, J.-M.5
Scheinin, M.6
-
19
-
-
0031937838
-
Validation of Furchgotts method to determine agonist-dependent A1-adenosine receptor reserve in guinea-pig atrium
-
Morey, T. E., Belardinelli, L., and Dennis, D. M. (1998) Validation of Furchgotts method to determine agonist-dependent A1-adenosine receptor reserve in guinea-pig atrium Br. J. Pharmacol. 123, 1425-1433
-
(1998)
Br. J. Pharmacol.
, vol.123
, pp. 1425-1433
-
-
Morey, T.E.1
Belardinelli, L.2
Dennis, D.M.3
-
20
-
-
84981848149
-
Comparison of dissociation constants and of relative efficacies of selected agonists acting on parasymthetic receptors
-
Furchgott, R. F. and Bursztyn, P. (1967) Comparison of dissociation constants and of relative efficacies of selected agonists acting on parasymthetic receptors Ann. N.Y. Acad. Sci. 144, 882-899
-
(1967)
Ann. N.Y. Acad. Sci.
, vol.144
, pp. 882-899
-
-
Furchgott, R.F.1
Bursztyn, P.2
-
21
-
-
84889564886
-
Activation and allosteric modulation of a muscarinic acetylcholine receptor
-
Kruse, A. C., Ring, A. M., Manglik, A., Hu, J., Hu, K., Eitel, K., Hubner, H., Pardon, E., Valant, C., Sexton, P. M., Christopoulos, A., Felder, C. C., Gmeiner, P., Steyaert, J., Weis, W. I., Garcia, K. C., Wess, J., and Kobilka, B. K. (2013) Activation and allosteric modulation of a muscarinic acetylcholine receptor Nature 504, 101-106
-
(2013)
Nature
, vol.504
, pp. 101-106
-
-
Kruse, A.C.1
Ring, A.M.2
Manglik, A.3
Hu, J.4
Hu, K.5
Eitel, K.6
Hubner, H.7
Pardon, E.8
Valant, C.9
Sexton, P.M.10
Christopoulos, A.11
Felder, C.C.12
Gmeiner, P.13
Steyaert, J.14
Weis, W.I.15
Garcia, K.C.16
Wess, J.17
Kobilka, B.K.18
-
22
-
-
14544271929
-
Disulfide trapping to localize small-molecule agonists and antagonists for a G protein-coupled receptor
-
Buck, E. and Wells, J. A. (2005) Disulfide trapping to localize small-molecule agonists and antagonists for a G protein-coupled receptor Proc. Natl. Acad. Sci. U.S.A. 102, 2719-2724
-
(2005)
Proc. Natl. Acad. Sci. U.S.A.
, vol.102
, pp. 2719-2724
-
-
Buck, E.1
Wells, J.A.2
-
23
-
-
14244265111
-
Site-specific disulfide capture of agonist and antagonist peptides on the C5a receptor
-
Buck, E., Bourne, H., and Wells, J. A. (2005) Site-specific disulfide capture of agonist and antagonist peptides on the C5a receptor J. Biol. Chem. 280, 4009-4012
-
(2005)
J. Biol. Chem.
, vol.280
, pp. 4009-4012
-
-
Buck, E.1
Bourne, H.2
Wells, J.A.3
-
24
-
-
0026755609
-
Analysis and refinement of criteria for predicting the structure and relative orientations of transmembranal helical domains
-
Ballesteros, J. A. and Weinstein, H. (1992) Analysis and refinement of criteria for predicting the structure and relative orientations of transmembranal helical domains Biophys. J. 62, 107-109
-
(1992)
Biophys. J.
, vol.62
, pp. 107-109
-
-
Ballesteros, J.A.1
Weinstein, H.2
-
25
-
-
0015836182
-
Stereospecific binding of the potent narcotic analgesic [3H]etorphine to rat-brain homogenate
-
Simon, E. J., Hiller, J. M., and Edelman, I. (1973) Stereospecific binding of the potent narcotic analgesic [3H]etorphine to rat-brain homogenate Proc. Natl. Acad. Sci. U.S.A. 70, 1947-1949
-
(1973)
Proc. Natl. Acad. Sci. U.S.A.
, vol.70
, pp. 1947-1949
-
-
Simon, E.J.1
Hiller, J.M.2
Edelman, I.3
-
26
-
-
0031009612
-
Identification in the μ-opioid receptor of cysteine residues responsible for inactivation of ligand binding by thiol alkylating and reducing agents
-
Gaibelet, G., Capeyrou, R., Dietrich, G., and Emorine, L. J. (1997) Identification in the μ-opioid receptor of cysteine residues responsible for inactivation of ligand binding by thiol alkylating and reducing agents FEBS Lett. 408, 135-140
-
(1997)
FEBS Lett.
, vol.408
, pp. 135-140
-
-
Gaibelet, G.1
Capeyrou, R.2
Dietrich, G.3
Emorine, L.J.4
-
27
-
-
0035975912
-
Discriminative disulfide-bonding affinity labeling of opioid receptor subtypes
-
Shirasu, N. and Shimohigashi, Y. (2001) Discriminative disulfide-bonding affinity labeling of opioid receptor subtypes J. Biochem. Biophys. Methods 49, 587-606
-
(2001)
J. Biochem. Biophys. Methods
, vol.49
, pp. 587-606
-
-
Shirasu, N.1
Shimohigashi, Y.2
-
28
-
-
15044351632
-
Site-directed affinity-labeling of delta opioid receptors by SNpys-containing enkephalin and dynorphin analogues
-
Isozaki, K., Fukahori, H., Honda, T., Shirasu, N., Okada, K., Nose, T., Sakaguchi, K., and Shimohigashi, Y. (2004) Site-directed affinity-labeling of delta opioid receptors by SNpys-containing enkephalin and dynorphin analogues Lett. Pept. Sci. 10, 511-522
-
(2004)
Lett. Pept. Sci.
, vol.10
, pp. 511-522
-
-
Isozaki, K.1
Fukahori, H.2
Honda, T.3
Shirasu, N.4
Okada, K.5
Nose, T.6
Sakaguchi, K.7
Shimohigashi, Y.8
-
29
-
-
50949109789
-
Specific affinity labeling of Cys60 in the δ opioid receptor by Npys-containing dynorphin A analog
-
Isozaki, K., Fukahori, H., Okada, K., Shirasu, N., Honda, T., Nose, T., Sakaguchi, K., Costa, T., and Shimohigashi, Y. (2003) Specific affinity labeling of Cys60 in the δ opioid receptor by Npys-containing dynorphin A analog Pept. Sci. 40, 273-276
-
(2003)
Pept. Sci.
, vol.40
, pp. 273-276
-
-
Isozaki, K.1
Fukahori, H.2
Okada, K.3
Shirasu, N.4
Honda, T.5
Nose, T.6
Sakaguchi, K.7
Costa, T.8
Shimohigashi, Y.9
-
30
-
-
67651204566
-
Structure-based design, synthesis, and biochemical and pharmacological characterization of novel salvinorin A analogues as active state probes of the kappa-opioid receptor
-
Yan, F., Bikbulatov, R. V., Mocanu, V., Dicheva, N., Parker, C. E., Wetsel, W. C., Mosier, P. D., Westkaemper, R. B., Allen, J. A., Zjawiony, J. K., and Roth, B. L. (2009) Structure-based design, synthesis, and biochemical and pharmacological characterization of novel salvinorin A analogues as active state probes of the kappa-opioid receptor Biochemistry 48, 6898-6908
-
(2009)
Biochemistry
, vol.48
, pp. 6898-6908
-
-
Yan, F.1
Bikbulatov, R.V.2
Mocanu, V.3
Dicheva, N.4
Parker, C.E.5
Wetsel, W.C.6
Mosier, P.D.7
Westkaemper, R.B.8
Allen, J.A.9
Zjawiony, J.K.10
Roth, B.L.11
-
31
-
-
0033678468
-
Identification and biological activity of the active metabolite of clopidogrel
-
Savi, P., Pereillo, J. M., Uzabiaga, M. F., Combalbert, J., Picard, C., Maffrand, J. P., Pascal, M., and Herbert, J. M. (2000) Identification and biological activity of the active metabolite of clopidogrel Thromb. Haemostasis 84, 891-896
-
(2000)
Thromb. Haemostasis
, vol.84
, pp. 891-896
-
-
Savi, P.1
Pereillo, J.M.2
Uzabiaga, M.F.3
Combalbert, J.4
Picard, C.5
Maffrand, J.P.6
Pascal, M.7
Herbert, J.M.8
-
32
-
-
84899755031
-
Structure of the human P2Y12 receptor in complex with an antithrombotic drug
-
Zhang, K., Zhang, J., Gao, Z.-G., Zhang, D., Zhu, L., Han, G. W., Moss, S. M., Paoletta, S., Kiselev, E., Lu, W., Fenalti, G., Zhang, W., Muller, C. E., Yang, H., Jiang, H., Cherezov, V., Katritch, V., Jacobson, K. A., Stevens, R. C., Wu, B., and Zhao, Q. (2014) Structure of the human P2Y12 receptor in complex with an antithrombotic drug Nature 509, 115-118
-
(2014)
Nature
, vol.509
, pp. 115-118
-
-
Zhang, K.1
Zhang, J.2
Gao, Z.-G.3
Zhang, D.4
Zhu, L.5
Han, G.W.6
Moss, S.M.7
Paoletta, S.8
Kiselev, E.9
Lu, W.10
Fenalti, G.11
Zhang, W.12
Muller, C.E.13
Yang, H.14
Jiang, H.15
Cherezov, V.16
Katritch, V.17
Jacobson, K.A.18
Stevens, R.C.19
Wu, B.20
Zhao, Q.21
more..
-
33
-
-
54149112344
-
Interaction of the active metabolite of prasugrel, R-138727, with cysteine 97 and cysteine 175 of the human P2Y12 receptor
-
Algaier, I., Jakubowski, J. A., Asai, F., and Von KU Gelgen, I. (2008) Interaction of the active metabolite of prasugrel, R-138727, with cysteine 97 and cysteine 175 of the human P2Y12 receptor J. Thromb. Haemost. 6, 1908-1914
-
(2008)
J. Thromb. Haemost.
, vol.6
, pp. 1908-1914
-
-
Algaier, I.1
Jakubowski, J.A.2
Asai, F.3
Von Ku Gelgen, I.4
-
34
-
-
0036852609
-
Covalent Modification of Amino Acid Nucleophiles by the Lipid Peroxidation Products 4-Hydroxy-2-nonenal and 4-Oxo-2-nonenal
-
Doorn, J. A. and Petersen, D. R. (2002) Covalent Modification of Amino Acid Nucleophiles by the Lipid Peroxidation Products 4-Hydroxy-2-nonenal and 4-Oxo-2-nonenal Chem. Res. Toxicol. 15, 1445-1450
-
(2002)
Chem. Res. Toxicol.
, vol.15
, pp. 1445-1450
-
-
Doorn, J.A.1
Petersen, D.R.2
-
35
-
-
84907478550
-
Promiscuity and selectivity in covalent enzyme inhibition: A systematic study of electrophilic fragments
-
Jöst, C., Nitsche, C., Scholz, T., Roux, L., and Klein, C. D. (2014) Promiscuity and selectivity in covalent enzyme inhibition: A systematic study of electrophilic fragments J. Med. Chem. 57, 7590-7599
-
(2014)
J. Med. Chem.
, vol.57
, pp. 7590-7599
-
-
Jöst, C.1
Nitsche, C.2
Scholz, T.3
Roux, L.4
Klein, C.D.5
-
36
-
-
84859845948
-
Reversible targeting of noncatalytic cysteines with chemically tuned electrophiles
-
Serafimova, I. M., Pufall, M. A., Krishnan, S., Duda, K., Cohen, M. S., Maglathlin, R. L., McFarland, J. M., Miller, R. M., Frödin, M., and Taunton, J. (2012) Reversible targeting of noncatalytic cysteines with chemically tuned electrophiles Nat. Chem. Biol. 8, 471-476
-
(2012)
Nat. Chem. Biol.
, vol.8
, pp. 471-476
-
-
Serafimova, I.M.1
Pufall, M.A.2
Krishnan, S.3
Duda, K.4
Cohen, M.S.5
Maglathlin, R.L.6
McFarland, J.M.7
Miller, R.M.8
Frödin, M.9
Taunton, J.10
-
37
-
-
0018900991
-
A novel opioid receptor site directed alkylating agent with irreversible narcotic antagonistic and reversible agonistic activities
-
Portoghese, P. S., Larson, D. L., Sayre, L. M., Fries, D. S., Smith, A. D., and Takemori, A. E. (1980) A novel opioid receptor site directed alkylating agent with irreversible narcotic antagonistic and reversible agonistic activities J. Med. Chem. 23, 233-234
-
(1980)
J. Med. Chem.
, vol.23
, pp. 233-234
-
-
Portoghese, P.S.1
Larson, D.L.2
Sayre, L.M.3
Fries, D.S.4
Smith, A.D.5
Takemori, A.E.6
-
38
-
-
0029829892
-
Determination of the amino acid residue involved in [3H]β-funaltrexamine covalent binding in the cloned rat μ opioid receptor
-
Chen, C., Yin, J., de Riel, J. K., DesJarlais, R. L., Raveglia, L. F., Zhu, J., and Liu-Chen, L.-Y. (1996) Determination of the amino acid residue involved in [3H]β-funaltrexamine covalent binding in the cloned rat μ opioid receptor J. Biol. Chem. 271, 21422-21429
-
(1996)
J. Biol. Chem.
, vol.271
, pp. 21422-21429
-
-
Chen, C.1
Yin, J.2
De Riel, J.K.3
Desjarlais, R.L.4
Raveglia, L.F.5
Zhu, J.6
Liu-Chen, L.-Y.7
-
39
-
-
84870033137
-
Fumaroylamino-4,5-epoxymorphinans and related opioids with irreversible μ opioid receptor antagonist effects
-
Moynihan, H. A., Derrick, I., Broadbear, J. H., Greedy, B. M., Aceto, M. D., Harris, L. S., Purington, L. C. S., Thomas, M. P., Woods, J. H., Traynor, J. R., Husbands, S. M., and Lewis, J. W. (2012) Fumaroylamino-4,5-epoxymorphinans and related opioids with irreversible μ opioid receptor antagonist effects J. Med. Chem. 55, 9868-9874
-
(2012)
J. Med. Chem.
, vol.55
, pp. 9868-9874
-
-
Moynihan, H.A.1
Derrick, I.2
Broadbear, J.H.3
Greedy, B.M.4
Aceto, M.D.5
Harris, L.S.6
Purington, L.C.S.7
Thomas, M.P.8
Woods, J.H.9
Traynor, J.R.10
Husbands, S.M.11
Lewis, J.W.12
-
40
-
-
84881629897
-
Design and pharmacological characterization of VUF14480, a covalent partial agonist that interacts with cysteine 98 of the human H4 receptor
-
Nijmeijer, S., E, H., Schultes, S., vand de Stolpe, A. C., Lusnik, V., de Graaf, C., Wijtmans, M., Haaksma, E. E. J., Esch, I. J.P., Stachurski, K., Vischer, H. F., and Leurs, R. (2013) Design and pharmacological characterization of VUF14480, a covalent partial agonist that interacts with cysteine 98 of the human H4 receptor Br. J. Pharmacol. 170, 89-100
-
(2013)
Br. J. Pharmacol.
, vol.170
, pp. 89-100
-
-
Nijmeijer, S.1
Schultes, S.2
Vand De Stolpe, A.C.3
Lusnik, V.4
De Graaf, C.5
Wijtmans, M.6
Haaksma, E.E.J.7
Esch, I.J.P.8
Stachurski, K.9
Vischer, H.F.10
Leurs, R.11
-
41
-
-
30144441512
-
A chemogenomic analysis of the transmembrane binding cavity of human G-protein-coupled receptors
-
Surgand, J.-S., Rodrigo, J., Kellenberger, E., and Rognan, D. (2005) A chemogenomic analysis of the transmembrane binding cavity of human G-protein-coupled receptors Proteins: Struct. Funct. Bioinf. 62, 509-538
-
(2005)
Proteins: Struct. Funct. Bioinf.
, vol.62
, pp. 509-538
-
-
Surgand, J.-S.1
Rodrigo, J.2
Kellenberger, E.3
Rognan, D.4
-
42
-
-
0024537574
-
Interaction of a chemically reactive prazosin analog with alpha-1 adrenoceptors of rat tissues
-
Kusiak, J. W., Pitha, J., and Piascik, M. T. (1989) Interaction of a chemically reactive prazosin analog with alpha-1 adrenoceptors of rat tissues J. Pharm. Exp. Ther. 249, 70-77
-
(1989)
J. Pharm. Exp. Ther.
, vol.249
, pp. 70-77
-
-
Kusiak, J.W.1
Pitha, J.2
Piascik, M.T.3
-
43
-
-
0027496774
-
Kinetics of activation and in vivo muscarinic receptor binding of N-(2-bromoethyl)-4-piperidinyl diphenylacetate: An analog of 4-DAMP mustard
-
Griffin, M. T., Thomas, E. A., and Ehlert, F. J. (1993) Kinetics of activation and in vivo muscarinic receptor binding of N-(2-bromoethyl)-4-piperidinyl diphenylacetate: an analog of 4-DAMP mustard J. Pharm. Exp. Ther. 266, 301-305
-
(1993)
J. Pharm. Exp. Ther.
, vol.266
, pp. 301-305
-
-
Griffin, M.T.1
Thomas, E.A.2
Ehlert, F.J.3
-
44
-
-
0016606787
-
The irreversible binding of acetylcholine mustard to muscarinic receptors in intestinal smuooth muscle of the guinea-pig
-
Robinson, D. A., Taylor, J. G., and Young, J. M. (1975) The irreversible binding of acetylcholine mustard to muscarinic receptors in intestinal smuooth muscle of the guinea-pig Br. J. Pharmacol. 53, 363-370
-
(1975)
Br. J. Pharmacol.
, vol.53
, pp. 363-370
-
-
Robinson, D.A.1
Taylor, J.G.2
Young, J.M.3
-
45
-
-
0033555146
-
Double mutant cycle analysis of aspartate 69, 97, and 103 to asparagine mutants in the m2 muscarinic acetylcholine receptor
-
Vogel, W. K., Peterson, G. L., Broderick, D. J., Mosser, V. A., and Schimerlik, M. I. (1999) Double mutant cycle analysis of aspartate 69, 97, and 103 to asparagine mutants in the m2 muscarinic acetylcholine receptor Arch. Biochem. Biophys. 361, 283-294
-
(1999)
Arch. Biochem. Biophys.
, vol.361
, pp. 283-294
-
-
Vogel, W.K.1
Peterson, G.L.2
Broderick, D.J.3
Mosser, V.A.4
Schimerlik, M.I.5
-
46
-
-
80052083563
-
Nanobody stabilization of G protein-coupled receptor conformational states
-
Steyaert, J. and Kobilka, B. K. (2011) Nanobody stabilization of G protein-coupled receptor conformational states Curr. Opin. Struct. Biol. 21, 567-572
-
(2011)
Curr. Opin. Struct. Biol.
, vol.21
, pp. 567-572
-
-
Steyaert, J.1
Kobilka, B.K.2
-
47
-
-
0013926158
-
An alkylating derivative of benzilylcholine with specific and long-lasting parasympatholytic activity
-
Gill, E. W. and Rang, H. P. (1966) An alkylating derivative of benzilylcholine with specific and long-lasting parasympatholytic activity Mol. Pharmacol. 2, 284-297
-
(1966)
Mol. Pharmacol.
, vol.2
, pp. 284-297
-
-
Gill, E.W.1
Rang, H.P.2
-
48
-
-
0015456385
-
Homologues of benzilylcholine mustard
-
Young, J. M., Hiley, R., and Burgen, A. S. (1972) Homologues of benzilylcholine mustard J. Pharm. Pharmacol. 24, 950-954
-
(1972)
J. Pharm. Pharmacol.
, vol.24
, pp. 950-954
-
-
Young, J.M.1
Hiley, R.2
Burgen, A.S.3
-
49
-
-
0032571228
-
The use of irreversible ligands to inactivate receptor subtypes: 4-DAMP mustard and muscarinic receptors in smooth muscle
-
Ehlert, F. J. and Griffin, M. T. (1998) The use of irreversible ligands to inactivate receptor subtypes: 4-DAMP mustard and muscarinic receptors in smooth muscle Life Sci. 62, 1659-1664
-
(1998)
Life Sci.
, vol.62
, pp. 1659-1664
-
-
Ehlert, F.J.1
Griffin, M.T.2
-
50
-
-
0021347734
-
An alkylating derivative of oxotremorine interacts irreversibly with the muscarinic receptor
-
Ehlert, F. J., Jenden, D. J., and Ringdahl, B. (1984) An alkylating derivative of oxotremorine interacts irreversibly with the muscarinic receptor Life Sci. 34, 985-991
-
(1984)
Life Sci.
, vol.34
, pp. 985-991
-
-
Ehlert, F.J.1
Jenden, D.J.2
Ringdahl, B.3
-
51
-
-
0025056723
-
Tertiary (2-haloethyl)amine derivatives of the muscarinic agent McN-A-343, [4-[[N-(3-chlorophenyl)carbamoyl]oxy]-2-butynyl]trimethylammonium chloride
-
Ringdahl, B., Mellin, C., Ehlert, F. J., Roch, M., Rice, K. M., and Jenden, D. J. (1990) Tertiary (2-haloethyl)amine derivatives of the muscarinic agent McN-A-343, [4-[[N-(3-chlorophenyl)carbamoyl]oxy]-2-butynyl]trimethylammonium chloride J. Med. Chem. 33, 281-286
-
(1990)
J. Med. Chem.
, vol.33
, pp. 281-286
-
-
Ringdahl, B.1
Mellin, C.2
Ehlert, F.J.3
Roch, M.4
Rice, K.M.5
Jenden, D.J.6
-
52
-
-
0022558887
-
Affinity labeling of the DDT1MF-2 cell α1-adrenergic receptor with [3H]phenoxybenzamine
-
Cornett, L. E. and Norris, J. S. (1986) Affinity labeling of the DDT1MF-2 cell α1-adrenergic receptor with [3H]phenoxybenzamine Biochem. Pharmacol. 35, 1663-1669
-
(1986)
Biochem. Pharmacol.
, vol.35
, pp. 1663-1669
-
-
Cornett, L.E.1
Norris, J.S.2
-
53
-
-
0022260762
-
Effects of the irreversible alpha-adrenoceptor antagonists phenoxybenzamine and benextramine on the effectiveness of nifedipine in inhibiting alpha1- and alpha2-adrenoceptor mediated vasoconstriction in pithed rats
-
Timmermans, P. B. M. W. M., Thoolen, M. J. M. C., Mathy, M. J., Wilfert, B., de Jong, A., and van Zwieten, P. A. (1985) Effects of the irreversible alpha-adrenoceptor antagonists phenoxybenzamine and benextramine on the effectiveness of nifedipine in inhibiting alpha1- and alpha2-adrenoceptor mediated vasoconstriction in pithed rats Arch. Pharmacol. 329, 404-413
-
(1985)
Arch. Pharmacol.
, vol.329
, pp. 404-413
-
-
Timmermans, P.B.M.W.M.1
Thoolen, M.J.M.C.2
Mathy, M.J.3
Wilfert, B.4
De Jong, A.5
Van Zwieten, P.A.6
-
54
-
-
0035903167
-
Phenoxybenzamine binding reveals the helical orientation of the third transmembrane domain of adrenergic receptors
-
Frang, H., Cockcroft, V., Karskela, T., Scheinin, M., and Marjamäki, A. (2001) Phenoxybenzamine binding reveals the helical orientation of the third transmembrane domain of adrenergic receptors J. Biol. Chem. 276, 31279-31284
-
(2001)
J. Biol. Chem.
, vol.276
, pp. 31279-31284
-
-
Frang, H.1
Cockcroft, V.2
Karskela, T.3
Scheinin, M.4
Marjamäki, A.5
-
55
-
-
0018772469
-
Synthesis and pharmacologic characterization of an alkylating analog chlornaltrexamine, of naltrexone with ultralong-lasting narcotic antagonist properties
-
Portoghese, P. S., Larson, D. L., Jiang, J. B., Caruso, T. P., and Takemori, A. E. (1979) Synthesis and pharmacologic characterization of an alkylating analog chlornaltrexamine, of naltrexone with ultralong-lasting narcotic antagonist properties J. Med. Chem. 22, 168-173
-
(1979)
J. Med. Chem.
, vol.22
, pp. 168-173
-
-
Portoghese, P.S.1
Larson, D.L.2
Jiang, J.B.3
Caruso, T.P.4
Takemori, A.E.5
-
56
-
-
0035899176
-
Fluorosulfonyl- and bis-(β-chloroethyl)amino-phenylamino functionalized pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives: Irreversible antagonists at the human A3 adenosine receptor and molecular modeling studies
-
Baraldi, P. G., Cacciari, B., Moro, S., Romagnoli, R., Ji, X.-d., Jacobson, K. A., Gessi, S., Borea, P. A., and Spalluto, G. (2001) Fluorosulfonyl- and bis-(β-chloroethyl)amino-phenylamino functionalized pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives: irreversible antagonists at the human A3 adenosine receptor and molecular modeling studies J. Med. Chem. 44, 2735-2742
-
(2001)
J. Med. Chem.
, vol.44
, pp. 2735-2742
-
-
Baraldi, P.G.1
Cacciari, B.2
Moro, S.3
Romagnoli, R.4
Ji, X.-D.5
Jacobson, K.A.6
Gessi, S.7
Borea, P.A.8
Spalluto, G.9
-
57
-
-
0031013450
-
The α-adrenoceptor-mediated actions of chloroethylclonidine
-
Docherty, J. R. and ORourke, M. (1997) The α-adrenoceptor-mediated actions of chloroethylclonidine Vascul. Pharmacol. 28, 197-201
-
(1997)
Vascul. Pharmacol.
, vol.28
, pp. 197-201
-
-
Docherty, J.R.1
Orourke, M.2
-
58
-
-
0029617613
-
Residues in the fifth membrane-spanning segment of the dopamine D2 receptor exposed in the binding-site crevice
-
Javitch, J. A., Fu, D., and Chen, J. (1995) Residues in the fifth membrane-spanning segment of the dopamine D2 receptor exposed in the binding-site crevice Biochemistry 34, 16433-16439
-
(1995)
Biochemistry
, vol.34
, pp. 16433-16439
-
-
Javitch, J.A.1
Fu, D.2
Chen, J.3
-
59
-
-
0023183818
-
Differential effects of fluphenazine-N-mustard, on calmodulin activity and on D1 and D2 dopaminergic responses
-
Winkler, J. D., Thermos, K., and Weiss, B. (1987) Differential effects of fluphenazine-N-mustard, on calmodulin activity and on D1 and D2 dopaminergic responses Psychopharmacology 92, 285-291
-
(1987)
Psychopharmacology
, vol.92
, pp. 285-291
-
-
Winkler, J.D.1
Thermos, K.2
Weiss, B.3
-
60
-
-
0020611560
-
Irreversible interaction of β-haloalkylamine derivatives with dopamine D1 and D2 receptors
-
Cross, A. J., Waddington, J. L., and Ross, S. T. (1983) Irreversible interaction of β-haloalkylamine derivatives with dopamine D1 and D2 receptors Life Sci. 32, 2733-2740
-
(1983)
Life Sci.
, vol.32
, pp. 2733-2740
-
-
Cross, A.J.1
Waddington, J.L.2
Ross, S.T.3
-
61
-
-
0019195760
-
Aporphines. 30. (-)-N(2-chloroethyl)-10,11-dihydroxynor-aporphine (chloroethylnorapomorphine), a novel irreversible dopamine receptor antagonist
-
Neumeyer, J. L., Law, S. J., Baldessarini, R. J., and Kula, N. S. (1980) Aporphines. 30. (-)-N(2-chloroethyl)-10,11-dihydroxynor-aporphine (chloroethylnorapomorphine), a novel irreversible dopamine receptor antagonist J. Med. Chem. 23, 594-595
-
(1980)
J. Med. Chem.
, vol.23
, pp. 594-595
-
-
Neumeyer, J.L.1
Law, S.J.2
Baldessarini, R.J.3
Kula, N.S.4
-
62
-
-
0021941757
-
Irreversible blockade of central 5-HT binding sites by 8-methoxy-2′-chloro-PAT
-
Emerit, M. B., Gozlan, H., Hall, M. D., and Marquet, A. (1985) Irreversible blockade of central 5-HT binding sites by 8-methoxy-2′-chloro-PAT Biochem. Pharmacol. 34, 883-892
-
(1985)
Biochem. Pharmacol.
, vol.34
, pp. 883-892
-
-
Emerit, M.B.1
Gozlan, H.2
Hall, M.D.3
Marquet, A.4
-
63
-
-
34248561378
-
Isothiocyanates from Tosyl Chloride Mediated Decomposition of in Situ Generated Dithiocarbamic Acid Salts
-
Wong, R. and Dolman, S. J. (2007) Isothiocyanates from Tosyl Chloride Mediated Decomposition of in Situ Generated Dithiocarbamic Acid Salts J. Org. Chem. 72, 3969-3971
-
(2007)
J. Org. Chem.
, vol.72
, pp. 3969-3971
-
-
Wong, R.1
Dolman, S.J.2
-
64
-
-
0021746723
-
Probes for narcotic receptor mediated phenomena. 7. Synthesis and pharmacological properties of irreversible ligands specific for. Mu or delta. Opiate receptors
-
Burke, T. R., Bajwa, B. S., Jacobson, A. E., Rice, K. C., Streaty, R. A., and Klee, W. A. (1984) Probes for narcotic receptor mediated phenomena. 7. Synthesis and pharmacological properties of irreversible ligands specific for.mu. or.delta. opiate receptors J. Med. Chem. 27, 1570-1574
-
(1984)
J. Med. Chem.
, vol.27
, pp. 1570-1574
-
-
Burke, T.R.1
Bajwa, B.S.2
Jacobson, A.E.3
Rice, K.C.4
Streaty, R.A.5
Klee, W.A.6
-
65
-
-
84903542386
-
Synthesis and pharmacological evaluation of analogues of benzyl quinolone carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the M1 muscarinic acetylcholine receptor
-
Davie, B. J., Valant, C., White, J. M., Sexton, P. M., Capuano, B., Christopoulos, A., and Scammells, P. J. (2014) Synthesis and pharmacological evaluation of analogues of benzyl quinolone carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the M1 muscarinic acetylcholine receptor J. Med. Chem. 57, 5405-5418
-
(2014)
J. Med. Chem.
, vol.57
, pp. 5405-5418
-
-
Davie, B.J.1
Valant, C.2
White, J.M.3
Sexton, P.M.4
Capuano, B.5
Christopoulos, A.6
Scammells, P.J.7
-
66
-
-
78049396160
-
HCB2 Ligand-interaction landscape: Cysteine residues critical to biarylpyrazole antagonist binding motif and receptor modulation
-
Mercier, R. W., Pei, Y., Pandarinathan, L., Janero, D. R., Zhang, J., and Makriyannis, A. (2010) hCB2 Ligand-interaction landscape: Cysteine residues critical to biarylpyrazole antagonist binding motif and receptor modulation Chem. Biol. (Cambridge, MA, U. S.) 17, 1132-1142
-
(2010)
Chem. Biol. (Cambridge, MA, U. S.)
, vol.17
, pp. 1132-1142
-
-
Mercier, R.W.1
Pei, Y.2
Pandarinathan, L.3
Janero, D.R.4
Zhang, J.5
Makriyannis, A.6
-
67
-
-
80053892522
-
Mass spectrometry-based proteomics of human cannabinoid receptor 2: Covalent cysteine 6.47(257)-ligand interaction affording megagonist receptor activation
-
Szymanski, D. W., Papanastasiou, M., Melchior, K., Zvonok, N., Mercier, R. W., Janero, D. R., Thakur, G. A., Cha, S., Wu, B., Karger, B., and Makriyannis, A. (2011) Mass spectrometry-based proteomics of human cannabinoid receptor 2: Covalent cysteine 6.47(257)-ligand interaction affording megagonist receptor activation J. Proteome Res. 10, 4789-4798
-
(2011)
J. Proteome Res.
, vol.10
, pp. 4789-4798
-
-
Szymanski, D.W.1
Papanastasiou, M.2
Melchior, K.3
Zvonok, N.4
Mercier, R.W.5
Janero, D.R.6
Thakur, G.A.7
Cha, S.8
Wu, B.9
Karger, B.10
Makriyannis, A.11
-
68
-
-
0020609373
-
Irreversible ligands with high selectivity toward delta and mu opiate receptors
-
Rice, K. C., Jacobson, A. E., Burke, T. R., Bajwa, B. S., Streaty, R. A., and Klee, W. A. (1983) Irreversible ligands with high selectivity toward delta and mu opiate receptors Science 220, 314-316
-
(1983)
Science
, vol.220
, pp. 314-316
-
-
Rice, K.C.1
Jacobson, A.E.2
Burke, T.R.3
Bajwa, B.S.4
Streaty, R.A.5
Klee, W.A.6
-
69
-
-
0022455209
-
Probes for narcotic receptor mediated phenomena. 12. Cis-(+)-3-Methylfentanyl isothiocyanate, a potent site-directed acylating agent for δ opioid receptors. Synthesis, absolute configuration, and receptor enantioselectivity
-
Burke, T. R., Jr., Jacobson, A. E., Rice, K. C., Silverton, J. V., Simonds, W. F., Streaty, R. A., and Klee, W. A. (1986) Probes for narcotic receptor mediated phenomena. 12. cis-(+)-3-Methylfentanyl isothiocyanate, a potent site-directed acylating agent for δ opioid receptors. Synthesis, absolute configuration, and receptor enantioselectivity J. Med. Chem. 29, 1087-1093
-
(1986)
J. Med. Chem.
, vol.29
, pp. 1087-1093
-
-
Burke, Jr.T.R.1
Jacobson, A.E.2
Rice, K.C.3
Silverton, J.V.4
Simonds, W.F.5
Streaty, R.A.6
Klee, W.A.7
-
70
-
-
0025316399
-
Naltrindole-5′-isothiocyanate: A nonequilibrium, highly selective δ-opioid receptor antagonist
-
Portoghese, P. S., Sultana, M., and Takemori, A. E. (1990) Naltrindole-5′-isothiocyanate: a nonequilibrium, highly selective δ-opioid receptor antagonist J. Med. Chem. 33, 1547-1548
-
(1990)
J. Med. Chem.
, vol.33
, pp. 1547-1548
-
-
Portoghese, P.S.1
Sultana, M.2
Takemori, A.E.3
-
71
-
-
0024614117
-
Selective and enantiospecific acylation of κ-opioid receptors by (1S,2S)-trans-2-isothiocyanato-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzeneacetamide. Demonstration of κ receptor heterogeneity
-
De Costa, B. R., Rothman, R. B., Bykov, V., Jacobson, A. E., and Rice, K. C. (1989) Selective and enantiospecific acylation of κ-opioid receptors by (1S,2S)-trans-2-isothiocyanato-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzeneacetamide. Demonstration of κ receptor heterogeneity J. Med. Chem. 32, 281-283
-
(1989)
J. Med. Chem.
, vol.32
, pp. 281-283
-
-
De Costa, B.R.1
Rothman, R.B.2
Bykov, V.3
Jacobson, A.E.4
Rice, K.C.5
-
72
-
-
0027010264
-
Prolonged D2 antidopaminergic activity of alkylating and nonalkylating derivatives of spiperone in rat brain
-
Baldessarini, R. J., Kula, N. S., Campbell, A., Bakthavachalam, V., Yuan, J., and Neumeyer, J. L. (1992) Prolonged D2 antidopaminergic activity of alkylating and nonalkylating derivatives of spiperone in rat brain Mol. Pharmacol. 42, 856-863
-
(1992)
Mol. Pharmacol.
, vol.42
, pp. 856-863
-
-
Baldessarini, R.J.1
Kula, N.S.2
Campbell, A.3
Bakthavachalam, V.4
Yuan, J.5
Neumeyer, J.L.6
-
73
-
-
0024205441
-
High affinity acylating antagonists for the A1 adenosine receptor: Identification of binding subunit
-
Stiles, G. L. and Jacobson, K. A. (1988) High affinity acylating antagonists for the A1 adenosine receptor: identification of binding subunit Mol. Pharmacol. 34, 724-728
-
(1988)
Mol. Pharmacol.
, vol.34
, pp. 724-728
-
-
Stiles, G.L.1
Jacobson, K.A.2
-
74
-
-
0028128225
-
A selective agonist affinity label for A3 adenosine receptors
-
Ji, X.-d., Gallo-Rodriguez, C., and Jacobson, K. A. (1994) A selective agonist affinity label for A3 adenosine receptors Biochem. Biophys. Res. Commun. 203, 570-576
-
(1994)
Biochem. Biophys. Res. Commun.
, vol.203
, pp. 570-576
-
-
Ji, X.-D.1
Gallo-Rodriguez, C.2
Jacobson, K.A.3
-
75
-
-
0024591557
-
Electrophilic derivatives of purines as irreversible inhibitors of A1 adenosine receptors
-
Jacobson, K. A., Barone, S., Kammula, U., and Stiles, G. L. (1989) Electrophilic derivatives of purines as irreversible inhibitors of A1 adenosine receptors J. Med. Chem. 32, 1043-1051
-
(1989)
J. Med. Chem.
, vol.32
, pp. 1043-1051
-
-
Jacobson, K.A.1
Barone, S.2
Kammula, U.3
Stiles, G.L.4
-
76
-
-
3042800470
-
Clonidine p-isothiocyanate, an affinity label for alpha 2-adrenergic receptors on human platelets
-
Atlas, D. and Steer, M. L. (1982) Clonidine p-isothiocyanate, an affinity label for alpha 2-adrenergic receptors on human platelets Proc. Natl. Acad. Sci. U. S. A. 79, 1378-1382
-
(1982)
Proc. Natl. Acad. Sci. U. S. A.
, vol.79
, pp. 1378-1382
-
-
Atlas, D.1
Steer, M.L.2
-
77
-
-
37049004220
-
Design, synthesis, and melatoninergic activity of new azido- and isothiocyanato-substituted indoles
-
Tsotinis, A., Afroudakis, P. A., Davidson, K., Prashar, A., Smith, A. D., and Sugden, D. (2007) Design, synthesis, and melatoninergic activity of new azido- and isothiocyanato-substituted indoles J. Med. Chem. 50, 6436-6440
-
(2007)
J. Med. Chem.
, vol.50
, pp. 6436-6440
-
-
Tsotinis, A.1
Afroudakis, P.A.2
Davidson, K.3
Prashar, A.4
Smith, A.D.5
Sugden, D.6
-
78
-
-
0026631803
-
High affinity acylating antagonists for muscarinic receptors
-
Baumgold, J., Karton, Y., Malka, N., and Jacobson, K. A. (1992) High affinity acylating antagonists for muscarinic receptors Life Sci. 51, 345-351
-
(1992)
Life Sci.
, vol.51
, pp. 345-351
-
-
Baumgold, J.1
Karton, Y.2
Malka, N.3
Jacobson, K.A.4
-
79
-
-
0025183105
-
Aprophit: An irreversible antagonist for muscarinic receptors
-
Newman, A. H., Covington, J., Oleshansky, M., Jackson, B. W., Weissman, B. A., Leader, H., and Chiang, P. K. (1990) Aprophit: An irreversible antagonist for muscarinic receptors Biochem. Pharmacol. 40, 1357-1364
-
(1990)
Biochem. Pharmacol.
, vol.40
, pp. 1357-1364
-
-
Newman, A.H.1
Covington, J.2
Oleshansky, M.3
Jackson, B.W.4
Weissman, B.A.5
Leader, H.6
Chiang, P.K.7
-
80
-
-
0030045457
-
NCS-MPP (4-(2′-methoxyphenyl)-1-[2′-(N-2′-pyridyl)-p-isothiocyanobenzamido]ethylpiperazine): A high affinity and irreversible 5-HT1A receptor ligand
-
Kung, M.-P., Mu, M., Zhuang, Z.-P., and Kung, H. F. (1995) NCS-MPP (4-(2′-methoxyphenyl)-1-[2′-(N-2′-pyridyl)-p-isothiocyanobenzamido]ethylpiperazine): a high affinity and irreversible 5-HT1A receptor ligand Life Sci. 58, 177-186
-
(1995)
Life Sci.
, vol.58
, pp. 177-186
-
-
Kung, M.-P.1
Mu, M.2
Zhuang, Z.-P.3
Kung, H.F.4
-
81
-
-
0141925616
-
Identification of the binding sites of the SR49059 nonpeptide antagonist into the V1a vasopressin receptor using sulfydryl-reactive ligands and cysteine mutants as chemical sensors
-
Tahtaoui, C., Balestre, M. N., Klotz, P., Rognan, D., Barberis, C., Mouillac, B., and Hibert, M. (2003) Identification of the binding sites of the SR49059 nonpeptide antagonist into the V1a vasopressin receptor using sulfydryl-reactive ligands and cysteine mutants as chemical sensors J. Biol. Chem. 278, 40010-40019
-
(2003)
J. Biol. Chem.
, vol.278
, pp. 40010-40019
-
-
Tahtaoui, C.1
Balestre, M.N.2
Klotz, P.3
Rognan, D.4
Barberis, C.5
Mouillac, B.6
Hibert, M.7
-
82
-
-
84909953243
-
Covalent protein modification: The current landscape of residue-specific electrophiles
-
Shannon, D. A. and Weerapana, E. (2015) Covalent protein modification: the current landscape of residue-specific electrophiles Curr. Opin. Chem. Biol. 24, 18-26
-
(2015)
Curr. Opin. Chem. Biol.
, vol.24
, pp. 18-26
-
-
Shannon, D.A.1
Weerapana, E.2
-
83
-
-
84883445935
-
Adding an unnatural covalent bond to proteins through proximity-enhanced bioreactivity
-
Xiang, Z., Ren, H., Hu, Y. S., Coin, I., Wei, J., Cang, H., and Wang, L. (2013) Adding an unnatural covalent bond to proteins through proximity-enhanced bioreactivity Nat. Methods. 10, 885-888
-
(2013)
Nat. Methods.
, vol.10
, pp. 885-888
-
-
Xiang, Z.1
Ren, H.2
Hu, Y.S.3
Coin, I.4
Wei, J.5
Cang, H.6
Wang, L.7
-
84
-
-
0019131621
-
Potent beta-adrenergic antagonist possessing chemically reactive group
-
Pitha, J., Zjawiony, J., Nasrin, N., Lefkowitz, R. J., and Caron, M. G. (1980) Potent beta-adrenergic antagonist possessing chemically reactive group Life Sci. 27, 1791-1798
-
(1980)
Life Sci.
, vol.27
, pp. 1791-1798
-
-
Pitha, J.1
Zjawiony, J.2
Nasrin, N.3
Lefkowitz, R.J.4
Caron, M.G.5
-
85
-
-
0021965692
-
Irreversible blockade of β-adrenergic receptors with a bromoacetyl derivative of pindolol
-
Homburger, V., Gozlan, H., Bouhelal, R., Lucas, M., and Bockaert, J. (1985) Irreversible blockade of β-adrenergic receptors with a bromoacetyl derivative of pindolol Naunyn-Schmiedebergs Arch. Pharmacol. 328, 279-287
-
(1985)
Naunyn-Schmiedebergs Arch. Pharmacol.
, vol.328
, pp. 279-287
-
-
Homburger, V.1
Gozlan, H.2
Bouhelal, R.3
Lucas, M.4
Bockaert, J.5
-
86
-
-
0021949426
-
Covalent labeling of the beta-adrenergic ligand-binding site with para-(bromoacetamidyl)benzylcarazolol. A highly potent beta-adrenergic affinity label
-
Dickinson, K. E., Heald, S. L., Jeffs, P. W., Lefkowitz, R. J., and Caron, M. G. (1985) Covalent labeling of the beta-adrenergic ligand-binding site with para-(bromoacetamidyl)benzylcarazolol. A highly potent beta-adrenergic affinity label Mol. Pharmacol. 27, 499-506
-
(1985)
Mol. Pharmacol.
, vol.27
, pp. 499-506
-
-
Dickinson, K.E.1
Heald, S.L.2
Jeffs, P.W.3
Lefkowitz, R.J.4
Caron, M.G.5
-
87
-
-
0022367060
-
Irreversible inactivation of the β-adrenoreceptor by a partial agonist. Evidence for selective loss of the agonist high affinity binding sites
-
Baker, S. P., Liptak, A., and Pitha, J. (1985) Irreversible inactivation of the β-adrenoreceptor by a partial agonist. Evidence for selective loss of the agonist high affinity binding sites J. Biol. Chem. 260, 15820-15828
-
(1985)
J. Biol. Chem.
, vol.260
, pp. 15820-15828
-
-
Baker, S.P.1
Liptak, A.2
Pitha, J.3
-
88
-
-
0023258258
-
Carbostyril derivatives having potent β-adrenergic agonist properties
-
Milecki, J., Baker, S. P., Standifer, K. M., Ishizu, T., Chida, Y., Kusiak, J. W., and Pitha, J. (1987) Carbostyril derivatives having potent β-adrenergic agonist properties J. Med. Chem. 30, 1563-1566
-
(1987)
J. Med. Chem.
, vol.30
, pp. 1563-1566
-
-
Milecki, J.1
Baker, S.P.2
Standifer, K.M.3
Ishizu, T.4
Chida, Y.5
Kusiak, J.W.6
Pitha, J.7
-
89
-
-
0024498148
-
Carbostyril-based beta-adrenergic agonists: Evidence for long lasting or apparent irreversible receptor binding and activation of adenylate cyclase activity in vitro
-
Standifer, K. M., Pitha, J., and Baker, S. P. (1989) Carbostyril-based beta-adrenergic agonists: evidence for long lasting or apparent irreversible receptor binding and activation of adenylate cyclase activity in vitro Naunyn-Schmiedebergs Arch. Pharmacol. 339, 129-137
-
(1989)
Naunyn-Schmiedebergs Arch. Pharmacol.
, vol.339
, pp. 129-137
-
-
Standifer, K.M.1
Pitha, J.2
Baker, S.P.3
-
90
-
-
0031897217
-
Irreversible binding of a carbostyril-based agonist and antagonist to the β-adrenoceptor in DDT1MF-2 cells and rat aorta
-
Deyrup, M. D., Greco, P. G., Otero, D. H., Dennis, D. M., Gelband, C. H., and Baker, S. P. (1998) Irreversible binding of a carbostyril-based agonist and antagonist to the β-adrenoceptor in DDT1MF-2 cells and rat aorta Br. J. Pharmacol. 124, 165-175
-
(1998)
Br. J. Pharmacol.
, vol.124
, pp. 165-175
-
-
Deyrup, M.D.1
Greco, P.G.2
Otero, D.H.3
Dennis, D.M.4
Gelband, C.H.5
Baker, S.P.6
-
91
-
-
0031578626
-
Development of a high-affinity ligand that binds rrreversibly to Mel1b melatonin receptors
-
Witt-Enderby, P. A., Chu, G.-H., Gillen, M. L., and Li, P.-K. (1997) Development of a high-affinity ligand that binds rrreversibly to Mel1b melatonin receptors J. Med. Chem. 40, 4195-4198
-
(1997)
J. Med. Chem.
, vol.40
, pp. 4195-4198
-
-
Witt-Enderby, P.A.1
Chu, G.-H.2
Gillen, M.L.3
Li, P.-K.4
-
92
-
-
0026357735
-
Irreversible ligands as probes for drug receptors
-
Newman, A. H. (1991) Irreversible ligands as probes for drug receptors NIDA Res. Monogr. 112, 256-283
-
(1991)
NIDA Res. Monogr.
, vol.112
, pp. 256-283
-
-
Newman, A.H.1
-
93
-
-
84931275605
-
Fluoro-substituted phenylazocarboxamides: Dopaminergic behavior and N-arylating properties for irreversible binding
-
DOI
-
Bartuschat, A. L., Schellhorn, T., Hübner, H., Gmeiner, P., and Heinrich, M. R. (2015) Fluoro-substituted phenylazocarboxamides: Dopaminergic behavior and N-arylating properties for irreversible binding, Bioorg. Med. Chem., 14, DOI: 10.1016/j.bmc.2014.12.012.
-
(2015)
Bioorg. Med. Chem.
, vol.14
-
-
Bartuschat, A.L.1
Schellhorn, T.2
Hübner, H.3
Gmeiner, P.4
Heinrich, M.R.5
-
94
-
-
84906823958
-
Sulfur(VI) fluoride exchange (SuFEx): Another good reaction for click chemistry
-
Dong, J., Krasnova, L., Finn, M. G., and Sharpless, K. B. (2014) Sulfur(VI) fluoride exchange (SuFEx): Another good reaction for click chemistry Angew. Chem., Int. Ed. 53, 9430-9448
-
(2014)
Angew. Chem., Int. Ed.
, vol.53
, pp. 9430-9448
-
-
Dong, J.1
Krasnova, L.2
Finn, M.G.3
Sharpless, K.B.4
-
95
-
-
0037020759
-
New irreversible adenosine A1 antagonists based on FSCPX
-
Beauglehole, A. R., Baker, S. P., and Scammells, P. J. (2002) New irreversible adenosine A1 antagonists based on FSCPX Bioorg. Med. Chem. Lett. 12, 3179-3182
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 3179-3182
-
-
Beauglehole, A.R.1
Baker, S.P.2
Scammells, P.J.3
-
96
-
-
0034727862
-
Fluorosulfonyl-substituted xanthines as selective irreversible antagonists for the A1-adenosine receptor
-
Beauglehole, A. R., Baker, S. P., and Scammells, P. J. (2000) Fluorosulfonyl-substituted xanthines as selective irreversible antagonists for the A1-adenosine receptor J. Med. Chem. 43, 4973-4980
-
(2000)
J. Med. Chem.
, vol.43
, pp. 4973-4980
-
-
Beauglehole, A.R.1
Baker, S.P.2
Scammells, P.J.3
-
97
-
-
0030008733
-
A novel irreversible antagonist of the A1-adenosine receptor
-
Srinivas, M., Shryock, J. C., Scammells, P. J., Ruble, J., Baker, S. P., and Belardinelli, L. (1996) A novel irreversible antagonist of the A1-adenosine receptor Mol. Pharmacol. 50, 196-205
-
(1996)
Mol. Pharmacol.
, vol.50
, pp. 196-205
-
-
Srinivas, M.1
Shryock, J.C.2
Scammells, P.J.3
Ruble, J.4
Baker, S.P.5
Belardinelli, L.6
-
98
-
-
0034729789
-
Reporter affinity labels: An o-phthalaldehyde derivative of β-naltrexamine as a fluorogenic ligand for opioid receptors
-
Le Bourdonnec, B., Kouhen, R. E., Lunzer, M. M., Law, P. Y., Loh, H. H., and Portoghese, P. S. (2000) Reporter affinity labels: An o-phthalaldehyde derivative of β-naltrexamine as a fluorogenic ligand for opioid receptors J. Med. Chem. 43, 2489-2492
-
(2000)
J. Med. Chem.
, vol.43
, pp. 2489-2492
-
-
Le Bourdonnec, B.1
Kouhen, R.E.2
Lunzer, M.M.3
Law, P.Y.4
Loh, H.H.5
Portoghese, P.S.6
-
99
-
-
0037019276
-
Naphthalene dicarboxaldehyde as an electrophilic fluorogenic moiety for affinity labeling: Application to opioid receptor affinity labels with greatly improved fluorogenic properties
-
McCurdy, C. R., Le Bourdonnec, B., Metzger, T. G., Kouhen, R. E., Zhang, Y., Law, P. Y., and Portoghese, P. S. (2002) Naphthalene dicarboxaldehyde as an electrophilic fluorogenic moiety for affinity labeling: application to opioid receptor affinity labels with greatly improved fluorogenic properties J. Med. Chem. 45, 2887-2890
-
(2002)
J. Med. Chem.
, vol.45
, pp. 2887-2890
-
-
McCurdy, C.R.1
Le Bourdonnec, B.2
Metzger, T.G.3
Kouhen, R.E.4
Zhang, Y.5
Law, P.Y.6
Portoghese, P.S.7
-
100
-
-
0035304607
-
Affinity labels as tools for the identification of opioid receptor recognition sites
-
Portoghese, P. S., El Kouhen, R., Law, P. Y., Loh, H. H., and Le Bourdonnec, B. (2001) Affinity labels as tools for the identification of opioid receptor recognition sites Farmaco 56, 191-196
-
(2001)
Farmaco
, vol.56
, pp. 191-196
-
-
Portoghese, P.S.1
El Kouhen, R.2
Law, P.Y.3
Loh, H.H.4
Le Bourdonnec, B.5
|