-
1
-
-
0034490989
-
The expression, regulation and signal transduction pathways of the mammalian gonadotropin-releasing hormone receptor
-
Cheng, K. W., and Leung, P. C. (2000) The expression, regulation and signal transduction pathways of the mammalian gonadotropin-releasing hormone receptor, Can. J. Physiol. Pharmacol. 78, 1029-52.
-
(2000)
Can. J. Physiol. Pharmacol
, vol.78
, pp. 1029-1052
-
-
Cheng, K.W.1
Leung, P.C.2
-
2
-
-
0004270728
-
-
Knobil, E. N, Jr, Ed, pp, Raven Press, New York
-
Fink, G. (1988) in The Physiology of Reproduction (Knobil, E. N., Jr., Ed.) pp 1349-77, Raven Press, New York.
-
(1988)
The Physiology of Reproduction
, pp. 1349-1377
-
-
Fink, G.1
-
3
-
-
3843131055
-
Gonadotropin-releasing hormone receptors
-
Millar, R. P., Lu, Z. L., Pawson, A. J., Flanagan, C. A., Morgan, K., and Maudsley, S. R. (2004) Gonadotropin-releasing hormone receptors, Endocr. Rev. 25, 235-75.
-
(2004)
Endocr. Rev
, vol.25
, pp. 235-275
-
-
Millar, R.P.1
Lu, Z.L.2
Pawson, A.J.3
Flanagan, C.A.4
Morgan, K.5
Maudsley, S.R.6
-
4
-
-
0025294617
-
2+ mobilizing hormones: The case of gonadotropin-releasing hormone
-
2+ mobilizing hormones: The case of gonadotropin-releasing hormone, Endocr. Rev. 11, 326-53.
-
(1990)
Endocr. Rev
, vol.11
, pp. 326-353
-
-
Naor, Z.1
-
5
-
-
0028306250
-
Gonadotropin-releasing hormone and its analogs
-
Conn, P. M., and Crowley, W. F., Jr. (1994) Gonadotropin-releasing hormone and its analogs, Annu. Rev. Med. 45, 391-405.
-
(1994)
Annu. Rev. Med
, vol.45
, pp. 391-405
-
-
Conn, P.M.1
Crowley Jr., W.F.2
-
6
-
-
0036062668
-
Clinical use of GnRH analogs
-
Kiesel, L. A., Rody, A., Greb, R. R., and Szilagi, A. (2002) Clinical use of GnRH analogs, Clin. Endocrinol. 56, 677-87.
-
(2002)
Clin. Endocrinol
, vol.56
, pp. 677-687
-
-
Kiesel, L.A.1
Rody, A.2
Greb, R.R.3
Szilagi, A.4
-
8
-
-
0026501267
-
Hormone treatment of endometriosis: The estrogen threshold hypothesis
-
Barbieri, R. L. (1992) Hormone treatment of endometriosis: The estrogen threshold hypothesis, Am. J. Obstet. Gynecol. 166, 740-5.
-
(1992)
Am. J. Obstet. Gynecol
, vol.166
, pp. 740-745
-
-
Barbieri, R.L.1
-
9
-
-
0028235123
-
The use of leutenizing releasing hormone agonists and antagonists in gynaecological cancers
-
Emons, G., and Schally, A. V. (1994) The use of leutenizing releasing hormone agonists and antagonists in gynaecological cancers, Hum. Reprod. 9, 1364-79.
-
(1994)
Hum. Reprod
, vol.9
, pp. 1364-1379
-
-
Emons, G.1
Schally, A.V.2
-
10
-
-
0034511980
-
Progress towards the development of non-peptide orally-active gonadotropin-releasing hormone (GnRH) antagonists: Therapeutic implications
-
Millar, R. P., Zhu, Y. F., Chen, C., and Struthers, R. S. (2000) Progress towards the development of non-peptide orally-active gonadotropin-releasing hormone (GnRH) antagonists: Therapeutic implications, Br. Med. Bull. 56, 761-72.
-
(2000)
Br. Med. Bull
, vol.56
, pp. 761-772
-
-
Millar, R.P.1
Zhu, Y.F.2
Chen, C.3
Struthers, R.S.4
-
11
-
-
4344637399
-
Role of gonadotropin-releasing hormone (GnRH) in ovarian cancer
-
Grundker, C., and Emons, G. (2003) Role of gonadotropin-releasing hormone (GnRH) in ovarian cancer, Reprod. Biol. Endocrinol. 1, 65.
-
(2003)
Reprod. Biol. Endocrinol
, vol.1
, pp. 65
-
-
Grundker, C.1
Emons, G.2
-
12
-
-
0344444706
-
Gonadotropin-releasing hormone antagonists
-
Herbst, K. L. (2003) Gonadotropin-releasing hormone antagonists, Curr. Opin. Pharmacol. 3, 660-6.
-
(2003)
Curr. Opin. Pharmacol
, vol.3
, pp. 660-666
-
-
Herbst, K.L.1
-
13
-
-
0035944837
-
Gonadotropin-releasing-hormone- receptor antagonists
-
Huirne, J. A., and Lambalk, C. B. (2001) Gonadotropin-releasing-hormone- receptor antagonists, Lancet 358, 1793-803.
-
(2001)
Lancet
, vol.358
, pp. 1793-1803
-
-
Huirne, J.A.1
Lambalk, C.B.2
-
14
-
-
77956858305
-
Gonadotropin releasing hormone antagonists
-
Academic Press Inc, New York
-
Goulet, M. T. (1995) Gonadotropin releasing hormone antagonists, in Annual Reports in Medicinal Chemistry, pp 169-78, Academic Press Inc., New York.
-
(1995)
Annual Reports in Medicinal Chemistry
, pp. 169-178
-
-
Goulet, M.T.1
-
15
-
-
0035046991
-
The gonadotropin- releasing hormone antagonist abarelix depot versus luteinizing hormone releasing hormone agonists leuprolide or goserelin: Initial results of endocrinological and biochemical efficacies in patients with prostate cancer
-
Tomera, K., Gleason, D., Gittelman, M., Moseley, W., Zinner, N., Murdoch, M., Menon, M., Campion, M., and Garnick, M. B. (2001) The gonadotropin- releasing hormone antagonist abarelix depot versus luteinizing hormone releasing hormone agonists leuprolide or goserelin: Initial results of endocrinological and biochemical efficacies in patients with prostate cancer, J. Urol. 165, 1585-9.
-
(2001)
J. Urol
, vol.165
, pp. 1585-1589
-
-
Tomera, K.1
Gleason, D.2
Gittelman, M.3
Moseley, W.4
Zinner, N.5
Murdoch, M.6
Menon, M.7
Campion, M.8
Garnick, M.B.9
-
16
-
-
0033766116
-
Abarelix Depot, a GnRH antagonist, v LHRH superagonists in prostate cancer: Differential effects on follicle-stimulating hormone. Abarelix Depot study group
-
Garnick, M. B., and Campion, M. (2000) Abarelix Depot, a GnRH antagonist, v LHRH superagonists in prostate cancer: Differential effects on follicle-stimulating hormone. Abarelix Depot study group, Mol. Urol. 4, 275-7.
-
(2000)
Mol. Urol
, vol.4
, pp. 275-277
-
-
Garnick, M.B.1
Campion, M.2
-
17
-
-
0029865119
-
Down-regulation of pituitary receptors for luteinizing hormone-releasing hormone (LH-RH) in rats by LH-RH antagonist Cetrorelix
-
Halmos, G., Schally, A. V., Pinski, J., Vadillo-Buenfil, M., and Groot, K. (1996) Down-regulation of pituitary receptors for luteinizing hormone-releasing hormone (LH-RH) in rats by LH-RH antagonist Cetrorelix, Proc. Natl. Acad. Sci. U.S.A. 93, 2398-402.
-
(1996)
Proc. Natl. Acad. Sci. U.S.A
, vol.93
, pp. 2398-2402
-
-
Halmos, G.1
Schally, A.V.2
Pinski, J.3
Vadillo-Buenfil, M.4
Groot, K.5
-
18
-
-
2942550595
-
GnRH antagonists
-
Coccia, M. E., Comparetto, C., Bracco, G. L., and Scarselli, G. (2004) GnRH antagonists, Eur. J. Obstet. Gynecol. Reprod. Biol. 1158, S44-56.
-
(2004)
Eur. J. Obstet. Gynecol. Reprod. Biol
, vol.1158
-
-
Coccia, M.E.1
Comparetto, C.2
Bracco, G.L.3
Scarselli, G.4
-
19
-
-
5644242134
-
Non-Peptidic GnRH Receptor Antagonists
-
Armer, R. E., and Smelt, K. H. (2004) Non-Peptidic GnRH Receptor Antagonists, Curr. Med. Chem. 11, 3017-28.
-
(2004)
Curr. Med. Chem
, vol.11
, pp. 3017-3028
-
-
Armer, R.E.1
Smelt, K.H.2
-
20
-
-
33748510561
-
Nonpeptide Gonadotropin Releasing Hormone Antagonists
-
Zhu, Y. F., Chen, C., and Struthers, R. S. (2004) Nonpeptide Gonadotropin Releasing Hormone Antagonists, Annu. Rep. Med. Chem. 39, 99-110.
-
(2004)
Annu. Rep. Med. Chem
, vol.39
, pp. 99-110
-
-
Zhu, Y.F.1
Chen, C.2
Struthers, R.S.3
-
21
-
-
31544438603
-
Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor
-
Betz, S. F., Reinhart, G. J., Lio, F. M., Chen, C., and Struthers, R. S. (2006) Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor, J. Med. Chem. 49, 637-47.
-
(2006)
J. Med. Chem
, vol.49
, pp. 637-647
-
-
Betz, S.F.1
Reinhart, G.J.2
Lio, F.M.3
Chen, C.4
Struthers, R.S.5
-
22
-
-
33750132372
-
Determination of the Binding Mode of Thienopyrimidinedione Antagonists to the Human Gonadotropin Releasing Hormone Receptor Using SAR, Site-Directed Mutagenesis, and Homology Modeling
-
in press
-
Betz, S. F., Lio, F. M., Gao, Y., Reinhart, G. J., Guo, Z., Mesleh, M. F., Zhu, Y. F., and Struthers, R. S. (2006) Determination of the Binding Mode of Thienopyrimidinedione Antagonists to the Human Gonadotropin Releasing Hormone Receptor Using SAR, Site-Directed Mutagenesis, and Homology Modeling, J. Med. Chem. (in press).
-
(2006)
J. Med. Chem
-
-
Betz, S.F.1
Lio, F.M.2
Gao, Y.3
Reinhart, G.J.4
Guo, Z.5
Mesleh, M.F.6
Zhu, Y.F.7
Struthers, R.S.8
-
23
-
-
0036258990
-
G protein-coupled receptor allosterism and complexing
-
Christopoulos, A., and Kenakin, T. (2002) G protein-coupled receptor allosterism and complexing, Pharmacol. Rev. 54, 323-74.
-
(2002)
Pharmacol. Rev
, vol.54
, pp. 323-374
-
-
Christopoulos, A.1
Kenakin, T.2
-
24
-
-
3042557815
-
Allosteric Modulation of G protein-coupled receptors
-
May, L. T., Avlani, V. A., Sexton, P. M., and Christopoulos, A. (2004) Allosteric Modulation of G protein-coupled receptors, Curr. Pharm. Des. 10, 2003-13.
-
(2004)
Curr. Pharm. Des
, vol.10
, pp. 2003-2013
-
-
May, L.T.1
Avlani, V.A.2
Sexton, P.M.3
Christopoulos, A.4
-
25
-
-
0029126526
-
Detection, quantitation, and verification of allosteric interactions of agents with labeled and unlabeled ligands at G protein-coupled receptors: Interactions of strychnine and acetylcholine at muscarinic receptors
-
Lazareno, S., and Birdsall, N. J. (1995) Detection, quantitation, and verification of allosteric interactions of agents with labeled and unlabeled ligands at G protein-coupled receptors: Interactions of strychnine and acetylcholine at muscarinic receptors, Mol. Pharmacol. 48, 362-78.
-
(1995)
Mol. Pharmacol
, vol.48
, pp. 362-378
-
-
Lazareno, S.1
Birdsall, N.J.2
-
26
-
-
8744219619
-
G protein-coupled receptor allosterism: The promise and the problem(s)
-
Christopoulos, A., May, L. T., Avlani, V. A., and Sexton, P. M. (2004) G protein-coupled receptor allosterism: The promise and the problem(s), Biochem. Soc. Trans. 32, 873-7.
-
(2004)
Biochem. Soc. Trans
, vol.32
, pp. 873-877
-
-
Christopoulos, A.1
May, L.T.2
Avlani, V.A.3
Sexton, P.M.4
-
27
-
-
0025603686
-
Allosteric enhancement of adenosine Al receptor binding and function by 2-amino-3-benzoylthiophenes
-
Bruns, R. F., and Fergus, J. H. (1990) Allosteric enhancement of adenosine Al receptor binding and function by 2-amino-3-benzoylthiophenes, Mol. Pharmacol. 38, 939-49.
-
(1990)
Mol. Pharmacol
, vol.38
, pp. 939-949
-
-
Bruns, R.F.1
Fergus, J.H.2
-
28
-
-
0033539111
-
1 receptor. Synthesis and biological evaluation of novel 2-amino-3-benzoylthiophenes as allosteric enhancers of agonist binding
-
1 receptor. Synthesis and biological evaluation of novel 2-amino-3-benzoylthiophenes as allosteric enhancers of agonist binding, J. Med. Chem. 42, 3629-35.
-
(1999)
J. Med. Chem
, vol.42
, pp. 3629-3635
-
-
van der Klein, P.A.1
Kourounakis, A.P.2
IJzerman, A.P.3
-
29
-
-
0037122790
-
1 adenosine receptors
-
1 adenosine receptors, J. Med. Chem. 45, 382-9.
-
(2002)
J. Med. Chem
, vol.45
, pp. 382-389
-
-
Tranberg, C.E.1
Zickgraf, A.2
Giunta, B.N.3
Luetjens, H.4
Figler, H.5
Murphree, L.J.6
Falke, R.7
Fleischer, H.8
Linden, J.9
Scammells, P.J.10
Olsson, R.A.11
-
30
-
-
3142576214
-
2-Amino-3-benzoylthiophene allosteric enhancers of Al adenosine agonist binding: New 3, 4-, and 5-modifications
-
Lutjens, H., Zickgraf, A., Figler, H., Linden, J., Olsson, R. A., and Scammells, P. J. (2003) 2-Amino-3-benzoylthiophene allosteric enhancers of Al adenosine agonist binding: New 3, 4-, and 5-modifications, J. Med. Chem. 46, 1870-7.
-
(2003)
J. Med. Chem
, vol.46
, pp. 1870-1877
-
-
Lutjens, H.1
Zickgraf, A.2
Figler, H.3
Linden, J.4
Olsson, R.A.5
Scammells, P.J.6
-
31
-
-
0029776693
-
Activation of muscarinic acetylcholine receptors via their allosteric binding sites
-
Jakubik, J., Bacakova, L., Lisa, V., el-Fakahany, F. F., and Tucek, S. (1996) Activation of muscarinic acetylcholine receptors via their allosteric binding sites, Proc. Natl. Acad. Sci. U.S.A. 93, 8705-9.
-
(1996)
Proc. Natl. Acad. Sci. U.S.A
, vol.93
, pp. 8705-8709
-
-
Jakubik, J.1
Bacakova, L.2
Lisa, V.3
el-Fakahany, F.F.4
Tucek, S.5
-
33
-
-
0036232127
-
Allosteric modulation of muscarinic receptor signaling: Alcuronium-induced conversion of pilocarpine from an agonist into an antagonist
-
Zahn, K., Eckstein, N., Trankle, C., Sadee, W., and Mohr, K. (2002) Allosteric modulation of muscarinic receptor signaling: Alcuronium-induced conversion of pilocarpine from an agonist into an antagonist, J. Pharmacol. Exp. Ther. 301, 720-8.
-
(2002)
J. Pharmacol. Exp. Ther
, vol.301
, pp. 720-728
-
-
Zahn, K.1
Eckstein, N.2
Trankle, C.3
Sadee, W.4
Mohr, K.5
-
34
-
-
1342323325
-
Application of a kinetic model to the apparently complex behavior of negative and positive allosteric modulators of muscarinic acetylcholine receptors
-
Avlani, V., May, L. T., Sexton, P. M., and Christopoulos, A. (2004) Application of a kinetic model to the apparently complex behavior of negative and positive allosteric modulators of muscarinic acetylcholine receptors, J. Pharmacol. Exp. Ther. 308, 1062-72.
-
(2004)
J. Pharmacol. Exp. Ther
, vol.308
, pp. 1062-1072
-
-
Avlani, V.1
May, L.T.2
Sexton, P.M.3
Christopoulos, A.4
-
35
-
-
11844253226
-
Regulation of M2 muscarinic acetylcholine receptor expression and signaling by prolonged exposure to allosteric modulators
-
May, L. T., Lin, Y., Sexton, P. M., and Christopoulos, A. (2005) Regulation of M2 muscarinic acetylcholine receptor expression and signaling by prolonged exposure to allosteric modulators, J. Pharmacol. Exp. Ther. 312, 382-90.
-
(2005)
J. Pharmacol. Exp. Ther
, vol.312
, pp. 382-390
-
-
May, L.T.1
Lin, Y.2
Sexton, P.M.3
Christopoulos, A.4
-
37
-
-
9144251958
-
Pharmacodynamics of the type II calcimimetic compound cinacalcet HCl
-
Nemeth, E. F., Heaton, W. H., Miller, M., Fox, J., Balandrin, M. F., Van Wagenen, B. C., Colloton, M., Karbon, W., Scherrer, J., Shatzen, E., Rishton, G., Scully, S., Qi, M., Harris, R., Lacey, D., and Martin, D. (2004) Pharmacodynamics of the type II calcimimetic compound cinacalcet HCl, J. Pharmacol. Exp. Ther. 308, 627-35.
-
(2004)
J. Pharmacol. Exp. Ther
, vol.308
, pp. 627-635
-
-
Nemeth, E.F.1
Heaton, W.H.2
Miller, M.3
Fox, J.4
Balandrin, M.F.5
Van Wagenen, B.C.6
Colloton, M.7
Karbon, W.8
Scherrer, J.9
Shatzen, E.10
Rishton, G.11
Scully, S.12
Qi, M.13
Harris, R.14
Lacey, D.15
Martin, D.16
-
38
-
-
0035818605
-
Positive allosteric modulators of metabotropic glutamate 1 receptor: Characterization, mechanism of action, and binding site
-
Knoflach, F., Mutel, V., Jolidon, S., Kew, J. N., Malherbe, P., Vieira, E., Wichmann, J., and Kemp, J. A. (2001) Positive allosteric modulators of metabotropic glutamate 1 receptor: Characterization, mechanism of action, and binding site, Proc. Natl. Acad. Sci. U.S.A. 98, 13402-7.
-
(2001)
Proc. Natl. Acad. Sci. U.S.A
, vol.98
, pp. 13402-13407
-
-
Knoflach, F.1
Mutel, V.2
Jolidon, S.3
Kew, J.N.4
Malherbe, P.5
Vieira, E.6
Wichmann, J.7
Kemp, J.A.8
-
39
-
-
0142090782
-
-
Maj, M., Bruno, V., Dragic, Z., Yamamoto, R., Battaglia, G., Inderbitzin, W., Stoehr, N., Stein, T., Gasparini, F., Vranesic, I., Kuhn, R., Nicoletti, F., and Flor, P. J. (2003) (-)-PHCCC, a positive allosteric modulator of mGluR4: Characterization, mechanism of action, and neuroprotection, Neuropharmacology 45, 895-906.
-
Maj, M., Bruno, V., Dragic, Z., Yamamoto, R., Battaglia, G., Inderbitzin, W., Stoehr, N., Stein, T., Gasparini, F., Vranesic, I., Kuhn, R., Nicoletti, F., and Flor, P. J. (2003) (-)-PHCCC, a positive allosteric modulator of mGluR4: Characterization, mechanism of action, and neuroprotection, Neuropharmacology 45, 895-906.
-
-
-
-
40
-
-
11144354887
-
A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain
-
O'Brien, J. A., Lemaire, W., Wittmann, M., Jacobson, M. A., Ha, S. N., Wisnoski, D. D., Lindsley, C. W., Schaffhauser, H. J., Rowe, B., Sur, C., Duggan, M. E., Pettibone, D. J., Conn, P. J., and Williams, D. L. J. (2004) A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain, J. Pharmacol. Exp. Ther. 309, 568-77.
-
(2004)
J. Pharmacol. Exp. Ther
, vol.309
, pp. 568-577
-
-
O'Brien, J.A.1
Lemaire, W.2
Wittmann, M.3
Jacobson, M.A.4
Ha, S.N.5
Wisnoski, D.D.6
Lindsley, C.W.7
Schaffhauser, H.J.8
Rowe, B.9
Sur, C.10
Duggan, M.E.11
Pettibone, D.J.12
Conn, P.J.13
Williams, D.L.J.14
-
41
-
-
27844482134
-
A close structural analog of 2-methyl-6- (phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators
-
Rodriguez, A. L., Nong, Y., Sekaran, N. K., Alagille, D., Tamagnan, G. D., and Conn, P. J. (2005) A close structural analog of 2-methyl-6- (phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators, Mol. Pharmacol. 68, 1793-802.
-
(2005)
Mol. Pharmacol
, vol.68
, pp. 1793-1802
-
-
Rodriguez, A.L.1
Nong, Y.2
Sekaran, N.K.3
Alagille, D.4
Tamagnan, G.D.5
Conn, P.J.6
-
42
-
-
24044539957
-
Allosteric modulation of the cannabinoid CB1 receptor
-
Price, M. R., Baillie, G. L., Thomas, A., Stevenson, L. A., Easson, M., Goodwin, R., McLean, A., McIntosh, L., Goodwin, G., Walker, G., Westwood, P., Marrs, J., Thomson, F., Cowley, P., Christopoulos, A., Pertwee, R. G., and Ross, R. A. (2005) Allosteric modulation of the cannabinoid CB1 receptor, Mol. Pharmacol. 68, 1484-95.
-
(2005)
Mol. Pharmacol
, vol.68
, pp. 1484-1495
-
-
Price, M.R.1
Baillie, G.L.2
Thomas, A.3
Stevenson, L.A.4
Easson, M.5
Goodwin, R.6
McLean, A.7
McIntosh, L.8
Goodwin, G.9
Walker, G.10
Westwood, P.11
Marrs, J.12
Thomson, F.13
Cowley, P.14
Christopoulos, A.15
Pertwee, R.G.16
Ross, R.A.17
-
43
-
-
0037334023
-
Mechanism of corticotropin-releasing factor type I receptor regulation by nonpeptide antagonists
-
Hoare, S. R., Sullivan, S. K., Ling, N., Crowe, P. D., and Grigoriadis, D. E. (2003) Mechanism of corticotropin-releasing factor type I receptor regulation by nonpeptide antagonists, Mol. Pharmacol. 63, 151-65.
-
(2003)
Mol. Pharmacol
, vol.63
, pp. 151-165
-
-
Hoare, S.R.1
Sullivan, S.K.2
Ling, N.3
Crowe, P.D.4
Grigoriadis, D.E.5
-
44
-
-
15744391870
-
The CCR5 receptor-based mechanism of action of 873140, a potent allosteric noncompetitive HIV entry inhibitor
-
Watson, C., Jenkinson, S., Kazmierski, W., and Kenakin, T. (2005) The CCR5 receptor-based mechanism of action of 873140, a potent allosteric noncompetitive HIV entry inhibitor, Mol. Pharmacol. 67, 1268-82.
-
(2005)
Mol. Pharmacol
, vol.67
, pp. 1268-1282
-
-
Watson, C.1
Jenkinson, S.2
Kazmierski, W.3
Kenakin, T.4
-
45
-
-
0033028258
-
CPCCOEt, a noncompetitive metabotropic glutamate receptor 1 antagonist, inhibits receptor signaling without affecting glutamate binding
-
Litschig, S., Gasparini, F., Rueegg, D., Stoehr, N., Flor, P. J., Vranesic, I., Prezeau, L., Pin, J. P., Thomsen, C. P., and Kuhn, R. (1999) CPCCOEt, a noncompetitive metabotropic glutamate receptor 1 antagonist, inhibits receptor signaling without affecting glutamate binding, Mol. Pharmacol. 55, 453-61.
-
(1999)
Mol. Pharmacol
, vol.55
, pp. 453-461
-
-
Litschig, S.1
Gasparini, F.2
Rueegg, D.3
Stoehr, N.4
Flor, P.J.5
Vranesic, I.6
Prezeau, L.7
Pin, J.P.8
Thomsen, C.P.9
Kuhn, R.10
-
46
-
-
0034721795
-
The non-competitive antagonists 2-methyl-6-(phenylethynyl)pyridine and 7-hydroxyiminocyclopropan[b] criromen-1a-carboxylic acid ethyl ester interact with overlapping binding pockets in the transmembrane region of group I metabotropic glutamate receptors
-
Pagano, A., Ruegg, D., Litschig, S., Stoehr, N., Stierlin, C., Heinrich, M., Floersheim, P., Prezeau, L., Carroll, F., Pin, J. P., Cambria, A., Vranesic, I., Flor, P. J., Gasparini, F., and Kuhn, R. (2000) The non-competitive antagonists 2-methyl-6-(phenylethynyl)pyridine and 7-hydroxyiminocyclopropan[b] criromen-1a-carboxylic acid ethyl ester interact with overlapping binding pockets in the transmembrane region of group I metabotropic glutamate receptors, J. Biol. Chem. 275, 33750-8.
-
(2000)
J. Biol. Chem
, vol.275
, pp. 33750-33758
-
-
Pagano, A.1
Ruegg, D.2
Litschig, S.3
Stoehr, N.4
Stierlin, C.5
Heinrich, M.6
Floersheim, P.7
Prezeau, L.8
Carroll, F.9
Pin, J.P.10
Cambria, A.11
Vranesic, I.12
Flor, P.J.13
Gasparini, F.14
Kuhn, R.15
-
47
-
-
0036232127
-
Allosteric modulation of muscarinic receptor signaling: Alcuronium-induced conversion of pilocarpine from an agonist into an antagonist
-
Zahn, K., Eckstein, N., Trankle, C., Sadee, W., and Mohr, K. (2005) Allosteric modulation of muscarinic receptor signaling: Alcuronium-induced conversion of pilocarpine from an agonist into an antagonist, J. Pharmacol. Exp. Ther. 301, 720-8.
-
(2005)
J. Pharmacol. Exp. Ther
, vol.301
, pp. 720-728
-
-
Zahn, K.1
Eckstein, N.2
Trankle, C.3
Sadee, W.4
Mohr, K.5
-
48
-
-
0036591659
-
A model for the functioning of family 3 GPCRs
-
Parmentier, M. L., Prezeau, L., Bockert, J., and Pin, J. P. (2002) A model for the functioning of family 3 GPCRs, Trends Pharmacol. Sci. 23, 268-74.
-
(2002)
Trends Pharmacol. Sci
, vol.23
, pp. 268-274
-
-
Parmentier, M.L.1
Prezeau, L.2
Bockert, J.3
Pin, J.P.4
-
49
-
-
0037405120
-
Biological characterization of a novel, orally active small molecule gonadotropin-releasing hormone (GnRH) antagonist using castrated and intact rats
-
Anderes, K. L., Luthin, D. R., Castillo, R., Kraynov, E. A., Castro, M., Nared-Hood, K., Gregory, M. L., Pathak, V. P., Christie, L. C., Paderes, G., Vazir, H., Ye, Q., Anderson, M. B., and May, J. M. (2003) Biological characterization of a novel, orally active small molecule gonadotropin-releasing hormone (GnRH) antagonist using castrated and intact rats, J. Pharmacol. Exp. Ther. 305, 688-95.
-
(2003)
J. Pharmacol. Exp. Ther
, vol.305
, pp. 688-695
-
-
Anderes, K.L.1
Luthin, D.R.2
Castillo, R.3
Kraynov, E.A.4
Castro, M.5
Nared-Hood, K.6
Gregory, M.L.7
Pathak, V.P.8
Christie, L.C.9
Paderes, G.10
Vazir, H.11
Ye, Q.12
Anderson, M.B.13
May, J.M.14
-
50
-
-
18744366904
-
Characterization of mono- and diaminopyrimidine derivatives as novel, nonpeptide gonadotropin releasing hormone (GnRH) receptor antagonists
-
Luthin, D. R., Hong, Y., Tompkins, E., Anderes, K. L., Paderes, G., Kraynov, E. A., Castro, M. A., Nared-Hood, K. D., Castillo, R., Gregory, M., Vazir, H., May, J. M., and Anderson, M. B. (2002) Characterization of mono- and diaminopyrimidine derivatives as novel, nonpeptide gonadotropin releasing hormone (GnRH) receptor antagonists, Bioorg. Med. Chem. Lett. 12, 3635-9.
-
(2002)
Bioorg. Med. Chem. Lett
, vol.12
, pp. 3635-3639
-
-
Luthin, D.R.1
Hong, Y.2
Tompkins, E.3
Anderes, K.L.4
Paderes, G.5
Kraynov, E.A.6
Castro, M.A.7
Nared-Hood, K.D.8
Castillo, R.9
Gregory, M.10
Vazir, H.11
May, J.M.12
Anderson, M.B.13
-
51
-
-
18644378190
-
The discovery of novel small molecule non-peptide gonadotropin releasing hormone (GnRH) receptor antagonists
-
Luthin, D. R., Hong, Y., Pathak, V. P., Paderes, G., Nared-Hood, K. D., Castro, M. A., Vazir, H., Li, H., Tompkins, E., Christie, L., May, J. M., and Anderson, M. B. (2002) The discovery of novel small molecule non-peptide gonadotropin releasing hormone (GnRH) receptor antagonists, Bioorg. Med. Chem. Lett. 12, 3467-70.
-
(2002)
Bioorg. Med. Chem. Lett
, vol.12
, pp. 3467-3470
-
-
Luthin, D.R.1
Hong, Y.2
Pathak, V.P.3
Paderes, G.4
Nared-Hood, K.D.5
Castro, M.A.6
Vazir, H.7
Li, H.8
Tompkins, E.9
Christie, L.10
May, J.M.11
Anderson, M.B.12
-
52
-
-
10444219551
-
-
Tucci, F. C., Zhu, Y. F., Struthers, R. S., Guo, Z., Gross, T. D., Rowbottom, M. W., Acevedo, O., Gao, Y., Saunders, J., Xie, Q., Reinhart, G. J., Liu, X. J., Ling, N., Bonneville, A. K., Chen, T., Bozigian, H., and Chen, C. (2005) 3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3- methoxyphenyl)-6-methylpyrimidin-2,4-dione (NBI 42902) as a potent and orally active antagonist of the human gonadotropin-releasing hormone receptor. Design, synthesis, and in vitro and in vivo characterization, J. Med. Chem. 48, 1169-78.
-
Tucci, F. C., Zhu, Y. F., Struthers, R. S., Guo, Z., Gross, T. D., Rowbottom, M. W., Acevedo, O., Gao, Y., Saunders, J., Xie, Q., Reinhart, G. J., Liu, X. J., Ling, N., Bonneville, A. K., Chen, T., Bozigian, H., and Chen, C. (2005) 3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3- methoxyphenyl)-6-methylpyrimidin-2,4-dione (NBI 42902) as a potent and orally active antagonist of the human gonadotropin-releasing hormone receptor. Design, synthesis, and in vitro and in vivo characterization, J. Med. Chem. 48, 1169-78.
-
-
-
-
53
-
-
33845925084
-
Pharmacological Characterization of a Novel Nonpeptide Antagonist of the Human GnRH Receptor, NBI-42902
-
in press
-
Struthers, R. S., Xie, Q., Sullivan, S. K., Reinhart, G. J., Kohout, T. A., Zhu, Y. F., Chen, C., Liu, X. J., Ling, N., Yang, W., Maki, R., Bonneville, A. K., Chen, T., and Bozigian, H. Pharmacological Characterization of a Novel Nonpeptide Antagonist of the Human GnRH Receptor, NBI-42902, Endocrinology, in press.
-
Endocrinology
-
-
Struthers, R.S.1
Xie, Q.2
Sullivan, S.K.3
Reinhart, G.J.4
Kohout, T.A.5
Zhu, Y.F.6
Chen, C.7
Liu, X.J.8
Ling, N.9
Yang, W.10
Maki, R.11
Bonneville, A.K.12
Chen, T.13
Bozigian, H.14
-
54
-
-
33748074796
-
Kinetics of Nonpeptide Antagonist Binding to the Human Gonadotropin Releasing Hormone Receptor: Implications for Structure-Activity Relationships and Insurmountable Antagonism
-
in press
-
Sullivan, S. K., Hoare, S. R. J., Fleck, B. F., Zhu, Y. F., Heise, C. E., Struthers, R. S., and Crowe, P. D. (2006) Kinetics of Nonpeptide Antagonist Binding to the Human Gonadotropin Releasing Hormone Receptor: Implications for Structure-Activity Relationships and Insurmountable Antagonism, Biochem. Pharmacol. (in press).
-
(2006)
Biochem. Pharmacol
-
-
Sullivan, S.K.1
Hoare, S.R.J.2
Fleck, B.F.3
Zhu, Y.F.4
Heise, C.E.5
Struthers, R.S.6
Crowe, P.D.7
-
55
-
-
33749547640
-
Suppression of Serum Luteinizing Hormone in Postmenopausal Women by an Orally Administered Nonpeptide Antagonist of the Gonadotropin-Releasing Hormone Receptor (NBI-42902)
-
in press
-
Struthers, R. S., Chen, T., Campbell, B., Jimenez, R., Pan, H., Yen, S. C., and Bozigian, H. (2006) Suppression of Serum Luteinizing Hormone in Postmenopausal Women by an Orally Administered Nonpeptide Antagonist of the Gonadotropin-Releasing Hormone Receptor (NBI-42902), J. Clin. Endocrinol. Metab. (in press).
-
(2006)
J. Clin. Endocrinol. Metab
-
-
Struthers, R.S.1
Chen, T.2
Campbell, B.3
Jimenez, R.4
Pan, H.5
Yen, S.C.6
Bozigian, H.7
-
56
-
-
77957055780
-
Integrated methods for the construction of three dimensional models and computational probing of structure-function relations in G-protein coupled receptors
-
Ballasteros, J., and Weinstein, H. (1995) Integrated methods for the construction of three dimensional models and computational probing of structure-function relations in G-protein coupled receptors, Methods Neurosci. 25, 366-428.
-
(1995)
Methods Neurosci
, vol.25
, pp. 366-428
-
-
Ballasteros, J.1
Weinstein, H.2
-
57
-
-
0000390812
-
Non-peptide GnRH agents, methods and intermediates for their preparation
-
Anderson, M. B., Vazir, H. N., Luthin, D. R., Paderes, G. D., Pathak, V. P., Christie, L. C., Hong, Y., Tomkins, E. V., Li, H., and Faust, J. (2000) Non-peptide GnRH agents, methods and intermediates for their preparation, Chem. Abstr. 132, 279106.
-
(2000)
Chem. Abstr
, vol.132
, pp. 279106
-
-
Anderson, M.B.1
Vazir, H.N.2
Luthin, D.R.3
Paderes, G.D.4
Pathak, V.P.5
Christie, L.C.6
Hong, Y.7
Tomkins, E.V.8
Li, H.9
Faust, J.10
-
58
-
-
0031764251
-
A high affinity gonadotropin-releasing hormone (GnRH) tracer, radioiodinated at position 6, facilitates analysis of mutant GnRH receptors
-
Flanagan, C. A., Fromme, B. J., Davidson, J. S., and Millar, R. P. (1998) A high affinity gonadotropin-releasing hormone (GnRH) tracer, radioiodinated at position 6, facilitates analysis of mutant GnRH receptors, Endocrinology 139, 4115-9.
-
(1998)
Endocrinology
, vol.139
, pp. 4115-4119
-
-
Flanagan, C.A.1
Fromme, B.J.2
Davidson, J.S.3
Millar, R.P.4
-
59
-
-
4544377876
-
Species selectivity of nonpeptide antagonists of the gonadotropin-releasing hormone receptor is determined by residues in extracellular loops II and III and the amino terminus
-
Reinhart, G. J., Xie, Q., Liu, X. J., Zhu, Y. F., Fan, J., Chen, C., and Struthers, R. S. (2004) Species selectivity of nonpeptide antagonists of the gonadotropin-releasing hormone receptor is determined by residues in extracellular loops II and III and the amino terminus, J. Biol. Chem. 279, 34115-22.
-
(2004)
J. Biol. Chem
, vol.279
, pp. 34115-34122
-
-
Reinhart, G.J.1
Xie, Q.2
Liu, X.J.3
Zhu, Y.F.4
Fan, J.5
Chen, C.6
Struthers, R.S.7
-
60
-
-
0031785874
-
A single amino acid substitution in transmembrane helix VI results in overexpression of the human GnRH receptor
-
Myburgh, D. B., Pawson, A. J., Davidson, J. S., Flanagan, C. A., Millar, R. P., and Hapgood, J. P. (1998) A single amino acid substitution in transmembrane helix VI results in overexpression of the human GnRH receptor, Eur. J. Endocrinol. 139, 438-47.
-
(1998)
Eur. J. Endocrinol
, vol.139
, pp. 438-447
-
-
Myburgh, D.B.1
Pawson, A.J.2
Davidson, J.S.3
Flanagan, C.A.4
Millar, R.P.5
Hapgood, J.P.6
-
61
-
-
16544378561
-
A miniaturized column chromatography method for measuring receptor-mediated inositol phosphate accumulation
-
Benjamin, E. R., Haftl, S. L., Xanthos, D. N., Crumley, G., Hachicha, M., and Valenzano, K. J. (2004) A miniaturized column chromatography method for measuring receptor-mediated inositol phosphate accumulation, J. Biomol. Screening 9, 343-53.
-
(2004)
J. Biomol. Screening
, vol.9
, pp. 343-353
-
-
Benjamin, E.R.1
Haftl, S.L.2
Xanthos, D.N.3
Crumley, G.4
Hachicha, M.5
Valenzano, K.J.6
-
62
-
-
5544242529
-
MMFF VI. MMFF94s Option for Energy Minimization Studies
-
Halgren, T. A. (1999) MMFF VI. MMFF94s Option for Energy Minimization Studies, J. Comput. Chem. 20, 720-9.
-
(1999)
J. Comput. Chem
, vol.20
, pp. 720-729
-
-
Halgren, T.A.1
-
63
-
-
0001242234
-
MMFF VII. Characterization of MMFF94, MMFF94s, and Other Widely Available Force Fields for Conformational Energies and for Intermolecular-Interaction Energies and Geometries
-
Halgren, T. A. (1999) MMFF VII. Characterization of MMFF94, MMFF94s, and Other Widely Available Force Fields for Conformational Energies and for Intermolecular-Interaction Energies and Geometries, J. Comput. Chem. 20, 730-48.
-
(1999)
J. Comput. Chem
, vol.20
, pp. 730-748
-
-
Halgren, T.A.1
-
64
-
-
23844481788
-
Mutations remote from the human gonadotropin-releasing hormone (GnRH) receptor binding sites specifically increase binding affinity for GnRH II, but not GnRH I: Evidence for ligand-selective receptor active conformations
-
Lu, Z. L., Gallagher, R., Sellar, R., Coetsee, M., and Millar, R. R. (2005) Mutations remote from the human gonadotropin-releasing hormone (GnRH) receptor binding sites specifically increase binding affinity for GnRH II, but not GnRH I: Evidence for ligand-selective receptor active conformations, J. Biol. Chem. 280, 29796-803.
-
(2005)
J. Biol. Chem
, vol.280
, pp. 29796-29803
-
-
Lu, Z.L.1
Gallagher, R.2
Sellar, R.3
Coetsee, M.4
Millar, R.R.5
-
65
-
-
20544443426
-
Antagonist and agonist binding models of the human gonadotropin-releasing hormone receptor
-
Soderhall, J. A., Polymeropoulos, E. E., Paulini, K., Gunther, E., and Kuhne, R. (2005) Antagonist and agonist binding models of the human gonadotropin-releasing hormone receptor, Biochem. Biophys. Res. Commun. 333, 568-82.
-
(2005)
Biochem. Biophys. Res. Commun
, vol.333
, pp. 568-582
-
-
Soderhall, J.A.1
Polymeropoulos, E.E.2
Paulini, K.3
Gunther, E.4
Kuhne, R.5
-
66
-
-
0028100755
-
Glutamate 301 of the mouse gonadotropin-releasing hormone receptor confers specificity for arginine 8 of mammalian gonadotropin-releasing hormone
-
Flanagan, C. A., Becker, I. I., Davidson, J. S., Wakefield, I. K., Zhou, W., Sealfon, S. C., and Millar, R. P. (1994) Glutamate 301 of the mouse gonadotropin-releasing hormone receptor confers specificity for arginine 8 of mammalian gonadotropin-releasing hormone, J. Biol. Chem. 269, 22636-41.
-
(1994)
J. Biol. Chem
, vol.269
, pp. 22636-22641
-
-
Flanagan, C.A.1
Becker, I.I.2
Davidson, J.S.3
Wakefield, I.K.4
Zhou, W.5
Sealfon, S.C.6
Millar, R.P.7
-
67
-
-
0034747357
-
Role of aspartate 7.32 (302) of the human gonadotropin-releasing hormone receptor in stabilizing a high affinity ligand conformation
-
Fromme, B. J., Katz, A. A., Roeske, R. W., Millar, R. P., and Flanagan, C. A. (2001) Role of aspartate 7.32 (302) of the human gonadotropin-releasing hormone receptor in stabilizing a high affinity ligand conformation, Mol. Pharmacol. 60, 1280-7.
-
(2001)
Mol. Pharmacol
, vol.60
, pp. 1280-1287
-
-
Fromme, B.J.1
Katz, A.A.2
Roeske, R.W.3
Millar, R.P.4
Flanagan, C.A.5
-
68
-
-
15544365216
-
-
Elsevier Academic Press, San Diego
-
Kenakin, T. (2004) A Pharmacology Primer: Theory, Application, and Methods, pp 105-7, Elsevier Academic Press, San Diego.
-
(2004)
A Pharmacology Primer: Theory, Application, and Methods
, pp. 105-107
-
-
Kenakin, T.1
-
69
-
-
0033669603
-
Modeling the functional effects of allosteric modulators at pharmacological receptors: An extension of the two-state model of receptor activation
-
Hall, D. A. (2000) Modeling the functional effects of allosteric modulators at pharmacological receptors: An extension of the two-state model of receptor activation, Mol. Pharmacol. 58, 1412-23.
-
(2000)
Mol. Pharmacol
, vol.58
, pp. 1412-1423
-
-
Hall, D.A.1
-
70
-
-
9944263528
-
Searching for new allosteric sites in enzymes
-
Hardy, J. A., and Wells, J. A. (2004) Searching for new allosteric sites in enzymes, Curr. Opin. Struct. Biol. 14, 706-15.
-
(2004)
Curr. Opin. Struct. Biol
, vol.14
, pp. 706-715
-
-
Hardy, J.A.1
Wells, J.A.2
-
71
-
-
0031866950
-
On the unique binding and activating properties of xanomeline at the M1 muscarinic acetylcholine receptor
-
Christopoulos, A., Pierce, T. L., Sorman, J. L., and El-Fakahany, E. E. (1998) On the unique binding and activating properties of xanomeline at the M1 muscarinic acetylcholine receptor, Mol. Pharmacol. 53, 1120-30.
-
(1998)
Mol. Pharmacol
, vol.53
, pp. 1120-1130
-
-
Christopoulos, A.1
Pierce, T.L.2
Sorman, J.L.3
El-Fakahany, E.E.4
-
72
-
-
0036771048
-
Allosteric modulation of G protein-coupled receptors
-
Soudijn, W., van Wijngaarden, I., and Uzerman, A. P. (2002) Allosteric modulation of G protein-coupled receptors, Curr. Opin. Drug Discovery Dev. 5, 749-55.
-
(2002)
Curr. Opin. Drug Discovery Dev
, vol.5
, pp. 749-755
-
-
Soudijn, W.1
van Wijngaarden, I.2
Uzerman, A.P.3
|