-
1
-
-
84923141629
-
Methodological advances: the unsung heroes of the GPCR structural revolution
-
1 Ghosh, E., et al. Methodological advances: the unsung heroes of the GPCR structural revolution. Nat. Rev. Mol. Cell. Biol. 16 (2015), 69–81.
-
(2015)
Nat. Rev. Mol. Cell. Biol.
, vol.16
, pp. 69-81
-
-
Ghosh, E.1
-
2
-
-
84939818422
-
A molecular pharmacologist's guide to G protein-coupled receptor crystallography
-
2 Piscitelli, C.L., et al. A molecular pharmacologist's guide to G protein-coupled receptor crystallography. Mol. Pharmacol. 88 (2015), 536–551.
-
(2015)
Mol. Pharmacol.
, vol.88
, pp. 536-551
-
-
Piscitelli, C.L.1
-
3
-
-
84926623484
-
Large-scale production and protein engineering of G protein-coupled receptors for structural studies
-
3 Milic, D., Veprintsev, D.B., Large-scale production and protein engineering of G protein-coupled receptors for structural studies. Front. Pharmacol., 6, 2015, 66.
-
(2015)
Front. Pharmacol.
, vol.6
, pp. 66
-
-
Milic, D.1
Veprintsev, D.B.2
-
4
-
-
84995721452
-
Editorial: Orphan GPCRs as emerging drug targets
-
4 Fang, Y., et al. Editorial: Orphan GPCRs as emerging drug targets. Front. Pharmacol., 6, 2015, 295.
-
(2015)
Front. Pharmacol.
, vol.6
, pp. 295
-
-
Fang, Y.1
-
5
-
-
0038024615
-
The G-protein-coupled receptors in the human genome form five main families. Phylogenetic analysis, paralogon groups, and fingerprints
-
5 Fredriksson, R., et al. The G-protein-coupled receptors in the human genome form five main families. Phylogenetic analysis, paralogon groups, and fingerprints. Mol. Pharmacol. 63 (2003), 1256–1272.
-
(2003)
Mol. Pharmacol.
, vol.63
, pp. 1256-1272
-
-
Fredriksson, R.1
-
6
-
-
0034604451
-
Crystal structure of rhodopsin: a G protein-coupled receptor
-
6 Palczewski, K., et al. Crystal structure of rhodopsin: a G protein-coupled receptor. Science 289 (2000), 739–745.
-
(2000)
Science
, vol.289
, pp. 739-745
-
-
Palczewski, K.1
-
7
-
-
47049130668
-
Crystal structure of the ligand-free G-protein-coupled receptor opsin
-
7 Park, J.H., et al. Crystal structure of the ligand-free G-protein-coupled receptor opsin. Nature 454 (2008), 183–187.
-
(2008)
Nature
, vol.454
, pp. 183-187
-
-
Park, J.H.1
-
8
-
-
84861961427
-
Structural basis for allosteric regulation of GPCRs by sodium ions
-
8 Liu, W., et al. Structural basis for allosteric regulation of GPCRs by sodium ions. Science 337 (2012), 232–236.
-
(2012)
Science
, vol.337
, pp. 232-236
-
-
Liu, W.1
-
9
-
-
84893954062
-
Molecular control of delta-opioid receptor signalling
-
9 Fenalti, G., et al. Molecular control of delta-opioid receptor signalling. Nature 506 (2014), 191–196.
-
(2014)
Nature
, vol.506
, pp. 191-196
-
-
Fenalti, G.1
-
10
-
-
84897580006
-
Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator
-
10 Wu, H., et al. Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator. Science 344 (2014), 58–64.
-
(2014)
Science
, vol.344
, pp. 58-64
-
-
Wu, H.1
-
11
-
-
84890744445
-
Kinetics and mechanism of G protein-coupled receptor activation
-
11 Lohse, M.J., et al. Kinetics and mechanism of G protein-coupled receptor activation. Curr. Opin. Cell Biol. 27 (2014), 87–93.
-
(2014)
Curr. Opin. Cell Biol.
, vol.27
, pp. 87-93
-
-
Lohse, M.J.1
-
12
-
-
47949129742
-
Structure of a beta1-adrenergic G-protein-coupled receptor
-
486–391
-
12 Warne, T., et al. Structure of a beta1-adrenergic G-protein-coupled receptor. Nature, 454, 2008 486–391.
-
(2008)
Nature
, vol.454
-
-
Warne, T.1
-
13
-
-
40049099087
-
Microscale fluorescent thermal stability assay for membrane proteins
-
13 Alexandrov, A.I., et al. Microscale fluorescent thermal stability assay for membrane proteins. Structure 16 (2008), 351–359.
-
(2008)
Structure
, vol.16
, pp. 351-359
-
-
Alexandrov, A.I.1
-
14
-
-
84938359988
-
Crystal structure of rhodopsin bound to arrestin by femtosecond X-ray laser
-
14 Kang, Y., et al. Crystal structure of rhodopsin bound to arrestin by femtosecond X-ray laser. Nature 523 (2015), 561–567.
-
(2015)
Nature
, vol.523
, pp. 561-567
-
-
Kang, Y.1
-
15
-
-
78651405537
-
The structural basis for agonist and partial agonist action on a beta(1)-adrenergic receptor
-
15 Warne, T., et al. The structural basis for agonist and partial agonist action on a beta(1)-adrenergic receptor. Nature 469 (2011), 241–244.
-
(2011)
Nature
, vol.469
, pp. 241-244
-
-
Warne, T.1
-
16
-
-
84939795137
-
Structural insights into mu-opioid receptor activation
-
16 Huang, W., et al. Structural insights into mu-opioid receptor activation. Nature 524 (2015), 315–321.
-
(2015)
Nature
, vol.524
, pp. 315-321
-
-
Huang, W.1
-
17
-
-
84867840947
-
Structure of the agonist-bound neurotensin receptor
-
17 White, J.F., et al. Structure of the agonist-bound neurotensin receptor. Nature 490 (2012), 508–513.
-
(2012)
Nature
, vol.490
, pp. 508-513
-
-
White, J.F.1
-
18
-
-
79954782236
-
Structure of an agonist-bound human A2A adenosine receptor
-
18 Xu, F., et al. Structure of an agonist-bound human A2A adenosine receptor. Science 332 (2011), 322–327.
-
(2011)
Science
, vol.332
, pp. 322-327
-
-
Xu, F.1
-
19
-
-
79959564813
-
Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation
-
19 Lebon, G., et al. Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation. Nature 474 (2011), 521–525.
-
(2011)
Nature
, vol.474
, pp. 521-525
-
-
Lebon, G.1
-
20
-
-
80051658642
-
Crystal structure of the beta2 adrenergic receptor-Gs protein complex
-
20 Rasmussen, S.G., et al. Crystal structure of the beta2 adrenergic receptor-Gs protein complex. Nature 477 (2011), 549–555.
-
(2011)
Nature
, vol.477
, pp. 549-555
-
-
Rasmussen, S.G.1
-
21
-
-
84886947656
-
Adrenaline-activated structure of beta2-adrenoceptor stabilized by an engineered nanobody
-
21 Ring, A.M., et al. Adrenaline-activated structure of beta2-adrenoceptor stabilized by an engineered nanobody. Nature 502 (2013), 575–579.
-
(2013)
Nature
, vol.502
, pp. 575-579
-
-
Ring, A.M.1
-
22
-
-
84877607189
-
Structural basis for molecular recognition at serotonin receptors
-
22 Wang, C., et al. Structural basis for molecular recognition at serotonin receptors. Science 340 (2013), 610–614.
-
(2013)
Science
, vol.340
, pp. 610-614
-
-
Wang, C.1
-
23
-
-
84877631485
-
Structural features for functional selectivity at serotonin receptors
-
23 Wacker, D., et al. Structural features for functional selectivity at serotonin receptors. Science 340 (2013), 615–619.
-
(2013)
Science
, vol.340
, pp. 615-619
-
-
Wacker, D.1
-
24
-
-
84889564886
-
Activation and allosteric modulation of a muscarinic acetylcholine receptor
-
24 Kruse, A.C., et al. Activation and allosteric modulation of a muscarinic acetylcholine receptor. Nature 504 (2013), 101–106.
-
(2013)
Nature
, vol.504
, pp. 101-106
-
-
Kruse, A.C.1
-
25
-
-
84899751079
-
Agonist-bound structure of the human P2Y12 receptor
-
25 Zhang, J., et al. Agonist-bound structure of the human P2Y12 receptor. Nature 509 (2014), 119–122.
-
(2014)
Nature
, vol.509
, pp. 119-122
-
-
Zhang, J.1
-
26
-
-
84907221192
-
High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875
-
26 Srivastava, A., et al. High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875. Nature 513 (2014), 124–127.
-
(2014)
Nature
, vol.513
, pp. 124-127
-
-
Srivastava, A.1
-
27
-
-
84904325982
-
Structural basis for Smoothened receptor modulation and chemoresistance to anticancer drugs
-
27 Wang, C., et al. Structural basis for Smoothened receptor modulation and chemoresistance to anticancer drugs. Nat. Commun., 5, 2014, 4355.
-
(2014)
Nat. Commun.
, vol.5
, pp. 4355
-
-
Wang, C.1
-
28
-
-
84861984672
-
Fusion partner toolchest for the stabilization and crystallization of G protein-coupled receptors
-
28 Chun, E., et al. Fusion partner toolchest for the stabilization and crystallization of G protein-coupled receptors. Structure 20 (2012), 967–976.
-
(2012)
Structure
, vol.20
, pp. 967-976
-
-
Chun, E.1
-
29
-
-
84884673669
-
Structure of the CCR5 chemokine receptor-HIV entry inhibitor maraviroc complex
-
29 Tan, Q., et al. Structure of the CCR5 chemokine receptor-HIV entry inhibitor maraviroc complex. Science 341 (2013), 1387–1390.
-
(2013)
Science
, vol.341
, pp. 1387-1390
-
-
Tan, Q.1
-
30
-
-
84928469118
-
Two disparate ligand-binding sites in the human P2Y1 receptor
-
30 Zhang, D., et al. Two disparate ligand-binding sites in the human P2Y1 receptor. Nature 520 (2015), 317–321.
-
(2015)
Nature
, vol.520
, pp. 317-321
-
-
Zhang, D.1
-
31
-
-
84925506175
-
Crystal structure of the human OX2 orexin receptor bound to the insomnia drug suvorexant
-
31 Yin, J., et al. Crystal structure of the human OX2 orexin receptor bound to the insomnia drug suvorexant. Nature 519 (2015), 247–250.
-
(2015)
Nature
, vol.519
, pp. 247-250
-
-
Yin, J.1
-
32
-
-
84960155005
-
Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors
-
32 Yin, J., et al. Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors. Nat. Struct. Mol. Biol. 23 (2016), 293–299.
-
(2016)
Nat. Struct. Mol. Biol.
, vol.23
, pp. 293-299
-
-
Yin, J.1
-
33
-
-
84982308386
-
Crystal structures of the M1 and M4 muscarinic acetylcholine receptors
-
33 Thal, D.M., et al. Crystal structures of the M1 and M4 muscarinic acetylcholine receptors. Nature 531 (2016), 335–340.
-
(2016)
Nature
, vol.531
, pp. 335-340
-
-
Thal, D.M.1
-
34
-
-
84861075468
-
Structure of the delta-opioid receptor bound to naltrindole
-
34 Granier, S., et al. Structure of the delta-opioid receptor bound to naltrindole. Nature 485 (2012), 400–404.
-
(2012)
Nature
, vol.485
, pp. 400-404
-
-
Granier, S.1
-
35
-
-
84861019261
-
Structure of the nociceptin/orphanin FQ receptor in complex with a peptide mimetic
-
35 Thompson, A.A., et al. Structure of the nociceptin/orphanin FQ receptor in complex with a peptide mimetic. Nature 485 (2012), 395–399.
-
(2012)
Nature
, vol.485
, pp. 395-399
-
-
Thompson, A.A.1
-
36
-
-
36448995359
-
High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor
-
36 Cherezov, V., et al. High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor. Science 318 (2007), 1258–1265.
-
(2007)
Science
, vol.318
, pp. 1258-1265
-
-
Cherezov, V.1
-
37
-
-
84871411930
-
High-resolution crystal structure of human protease-activated receptor 1
-
37 Zhang, C., et al. High-resolution crystal structure of human protease-activated receptor 1. Nature 492 (2012), 387–392.
-
(2012)
Nature
, vol.492
, pp. 387-392
-
-
Zhang, C.1
-
38
-
-
84862777742
-
Structure of the human kappa-opioid receptor in complex with JDTic
-
38 Wu, H., et al. Structure of the human kappa-opioid receptor in complex with JDTic. Nature 485 (2012), 327–332.
-
(2012)
Nature
, vol.485
, pp. 327-332
-
-
Wu, H.1
-
39
-
-
84899755031
-
Structure of the human P2Y12 receptor in complex with an antithrombotic drug
-
39 Zhang, K., et al. Structure of the human P2Y12 receptor in complex with an antithrombotic drug. Nature 509 (2014), 115–118.
-
(2014)
Nature
, vol.509
, pp. 115-118
-
-
Zhang, K.1
-
40
-
-
84876197291
-
Crystal structure of oligomeric beta1-adrenergic G protein-coupled receptors in ligand-free basal state
-
40 Huang, J., et al. Crystal structure of oligomeric beta1-adrenergic G protein-coupled receptors in ligand-free basal state. Nat. Struct. Mol. Biol. 20 (2013), 419–425.
-
(2013)
Nat. Struct. Mol. Biol.
, vol.20
, pp. 419-425
-
-
Huang, J.1
-
41
-
-
85027927015
-
Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists
-
41 Wu, B., et al. Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists. Science 330 (2010), 1066–1071.
-
(2010)
Science
, vol.330
, pp. 1066-1071
-
-
Wu, B.1
-
42
-
-
78449305788
-
Structure of the human dopamine D3 receptor in complex with a D2/D3 selective antagonist
-
42 Chien, E.Y., et al. Structure of the human dopamine D3 receptor in complex with a D2/D3 selective antagonist. Science 330 (2010), 1091–1095.
-
(2010)
Science
, vol.330
, pp. 1091-1095
-
-
Chien, E.Y.1
-
43
-
-
84881173408
-
Structure of class B GPCR corticotropin-releasing factor receptor 1
-
43 Hollenstein, K., et al. Structure of class B GPCR corticotropin-releasing factor receptor 1. Nature 499 (2013), 438–443.
-
(2013)
Nature
, vol.499
, pp. 438-443
-
-
Hollenstein, K.1
-
44
-
-
36248970132
-
Crystal structure of the human beta2 adrenergic G-protein-coupled receptor
-
44 Rasmussen, S.G., et al. Crystal structure of the human beta2 adrenergic G-protein-coupled receptor. Nature 450 (2007), 383–387.
-
(2007)
Nature
, vol.450
, pp. 383-387
-
-
Rasmussen, S.G.1
-
45
-
-
84924561288
-
Structural biology. Structural basis for chemokine recognition and activation of a viral G protein-coupled receptor
-
45 Burg, J.S., et al. Structural biology. Structural basis for chemokine recognition and activation of a viral G protein-coupled receptor. Science 347 (2015), 1113–1137.
-
(2015)
Science
, vol.347
, pp. 1113-1137
-
-
Burg, J.S.1
-
46
-
-
79960070651
-
Structure of the human histamine H1 receptor complex with doxepin
-
46 Shimamura, T., et al. Structure of the human histamine H1 receptor complex with doxepin. Nature 475 (2011), 65–70.
-
(2011)
Nature
, vol.475
, pp. 65-70
-
-
Shimamura, T.1
-
47
-
-
84893854581
-
Structure of signaling-competent neurotensin receptor 1 obtained by directed evolution in Escherichia coli
-
47 Egloff, P., et al. Structure of signaling-competent neurotensin receptor 1 obtained by directed evolution in Escherichia coli. Proc. Natl. Acad. Sci. U. S. A. 111 (2014), E655–E662.
-
(2014)
Proc. Natl. Acad. Sci. U. S. A.
, vol.111
, pp. E655-E662
-
-
Egloff, P.1
-
48
-
-
40349088827
-
G-protein-coupled receptor phosphorylation: where, when and by whom
-
48 Tobin, A.B., G-protein-coupled receptor phosphorylation: where, when and by whom. Br. J. Pharmacol. 153:Suppl 1 (2008), S167–S176.
-
(2008)
Br. J. Pharmacol.
, vol.153
, pp. S167-S176
-
-
Tobin, A.B.1
-
49
-
-
80051616441
-
Distinct phosphorylation sites on the beta(2)-adrenergic receptor establish a barcode that encodes differential functions of beta-arrestin
-
49 Nobles, K.N., et al. Distinct phosphorylation sites on the beta(2)-adrenergic receptor establish a barcode that encodes differential functions of beta-arrestin. Sci. Signal., 4, 2011, ra51.
-
(2011)
Sci. Signal.
, vol.4
, pp. ra51
-
-
Nobles, K.N.1
-
50
-
-
79956295210
-
Differential regulation of two palmitoylation sites in the cytoplasmic tail of the beta1-adrenergic receptor
-
50 Zuckerman, D.M., et al. Differential regulation of two palmitoylation sites in the cytoplasmic tail of the beta1-adrenergic receptor. J. Biol. Chem. 286 (2011), 19014–19023.
-
(2011)
J. Biol. Chem.
, vol.286
, pp. 19014-19023
-
-
Zuckerman, D.M.1
-
51
-
-
0030451745
-
Deglycosylation of proteins for crystallization using recombinant fusion protein glycosidases
-
51 Grueninger-Leitch, F., et al. Deglycosylation of proteins for crystallization using recombinant fusion protein glycosidases. Protein Sci. 5 (1996), 2617–2622.
-
(1996)
Protein Sci.
, vol.5
, pp. 2617-2622
-
-
Grueninger-Leitch, F.1
-
52
-
-
80055115291
-
Crystallization of membrane proteins in lipidic mesophases
-
52 Liu, W., Cherezov, V., Crystallization of membrane proteins in lipidic mesophases. J. Vis. Exp., 2011, e2501.
-
(2011)
J. Vis. Exp.
, pp. e2501
-
-
Liu, W.1
Cherezov, V.2
-
53
-
-
84921728247
-
A comprehensive review of the lipid cubic phase or in meso method for crystallizing membrane and soluble proteins and complexes
-
53 Caffrey, M., A comprehensive review of the lipid cubic phase or in meso method for crystallizing membrane and soluble proteins and complexes. Acta Crystallogr. F Struct. Biol. Commun. 71:Pt 1 (2015), 3–18.
-
(2015)
Acta Crystallogr. F Struct. Biol. Commun.
, vol.71
, pp. 3-18
-
-
Caffrey, M.1
-
54
-
-
84940007958
-
Fluorescence recovery after photobleaching in lipidic cubic phase (LCP-FRAP): a precrystallization assay for membrane proteins
-
54 Fenalti, G., et al. Fluorescence recovery after photobleaching in lipidic cubic phase (LCP-FRAP): a precrystallization assay for membrane proteins. Methods Enzymol. 557 (2015), 417–437.
-
(2015)
Methods Enzymol.
, vol.557
, pp. 417-437
-
-
Fenalti, G.1
-
55
-
-
84857254248
-
Crystal structure of a lipid G protein-coupled receptor
-
55 Hanson, M.A., et al. Crystal structure of a lipid G protein-coupled receptor. Science 335 (2012), 851–855.
-
(2012)
Science
, vol.335
, pp. 851-855
-
-
Hanson, M.A.1
-
56
-
-
0034961077
-
Crystallization screens: compatibility with the lipidic cubic phase for in meso crystallization of membrane proteins
-
56 Cherezov, V., et al. Crystallization screens: compatibility with the lipidic cubic phase for in meso crystallization of membrane proteins. Biophys J. 81 (2001), 225–242.
-
(2001)
Biophys J.
, vol.81
, pp. 225-242
-
-
Cherezov, V.1
-
57
-
-
84863115467
-
Structure and dynamics of the M3 muscarinic acetylcholine receptor
-
57 Kruse, A.C., et al. Structure and dynamics of the M3 muscarinic acetylcholine receptor. Nature 482 (2012), 552–556.
-
(2012)
Nature
, vol.482
, pp. 552-556
-
-
Kruse, A.C.1
-
58
-
-
84862777405
-
Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist
-
58 Haga, K., et al. Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist. Nature 482 (2012), 547–551.
-
(2012)
Nature
, vol.482
, pp. 547-551
-
-
Haga, K.1
-
59
-
-
84907020020
-
Preparation of microcrystals in lipidic cubic phase for serial femtosecond crystallography
-
59 Liu, W., et al. Preparation of microcrystals in lipidic cubic phase for serial femtosecond crystallography. Nat. Protoc. 9 (2014), 2123–2134.
-
(2014)
Nat. Protoc.
, vol.9
, pp. 2123-2134
-
-
Liu, W.1
-
60
-
-
84890840505
-
Serial femtosecond crystallography of G protein-coupled receptors
-
60 Liu, W., et al. Serial femtosecond crystallography of G protein-coupled receptors. Science 342 (2013), 1521–1524.
-
(2013)
Science
, vol.342
, pp. 1521-1524
-
-
Liu, W.1
-
61
-
-
0028245619
-
Molecular biology of 5-HT receptors
-
61 Boess, F.G., Martin, I.L., Molecular biology of 5-HT receptors. Neuropharmacology 33 (1994), 275–317.
-
(1994)
Neuropharmacology
, vol.33
, pp. 275-317
-
-
Boess, F.G.1
Martin, I.L.2
-
62
-
-
12944284419
-
Kinetic and functional properties of [3H]ZM241385, a high affinity antagonist for adenosine A2A receptors
-
62 Uustare, A., et al. Kinetic and functional properties of [3H]ZM241385, a high affinity antagonist for adenosine A2A receptors. Life Sci. 76 (2005), 1513–1526.
-
(2005)
Life Sci.
, vol.76
, pp. 1513-1526
-
-
Uustare, A.1
-
63
-
-
0030053138
-
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy
-
63 Wexler, R.R., et al. Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy. J. Med. Chem. 39 (1996), 625–656.
-
(1996)
J. Med. Chem.
, vol.39
, pp. 625-656
-
-
Wexler, R.R.1
-
64
-
-
79953147162
-
New insights into the mechanisms whereby low molecular weight CCR5 ligands inhibit HIV-1 infection
-
64 Garcia-Perez, J., et al. New insights into the mechanisms whereby low molecular weight CCR5 ligands inhibit HIV-1 infection. J. Biol. Chem. 286 (2011), 4978–4990.
-
(2011)
J. Biol. Chem.
, vol.286
, pp. 4978-4990
-
-
Garcia-Perez, J.1
-
65
-
-
58149089159
-
Orally bioavailable isothioureas block function of the chemokine receptor CXCR4 in vitro and in vivo
-
65 Thoma, G., et al. Orally bioavailable isothioureas block function of the chemokine receptor CXCR4 in vitro and in vivo. J. Med. Chem. 51 (2008), 7915–7920.
-
(2008)
J. Med. Chem.
, vol.51
, pp. 7915-7920
-
-
Thoma, G.1
-
66
-
-
0030610305
-
The D3 dopamine receptor: neurobiology and potential clinical relevance
-
66 Levant, B., The D3 dopamine receptor: neurobiology and potential clinical relevance. Pharmacol. Rev. 49 (1997), 231–252.
-
(1997)
Pharmacol. Rev.
, vol.49
, pp. 231-252
-
-
Levant, B.1
-
67
-
-
84881193006
-
Structure of the human glucagon class B G-protein-coupled receptor
-
67 Siu, F.Y., et al. Structure of the human glucagon class B G-protein-coupled receptor. Nature 499 (2013), 444–449.
-
(2013)
Nature
, vol.499
, pp. 444-449
-
-
Siu, F.Y.1
-
68
-
-
0029847231
-
Impaired locomotor activity and exploratory behavior in mice lacking histamine H1 receptors
-
68 Inoue, I., et al. Impaired locomotor activity and exploratory behavior in mice lacking histamine H1 receptors. Proc. Natl. Acad. Sci. U. S. A. 93 (1996), 13316–13320.
-
(1996)
Proc. Natl. Acad. Sci. U. S. A.
, vol.93
, pp. 13316-13320
-
-
Inoue, I.1
-
69
-
-
79953684895
-
Muscarinic receptor antagonists, from folklore to pharmacology; finding drugs that actually work in asthma and COPD
-
69 Moulton, B.C., Fryer, A.D., Muscarinic receptor antagonists, from folklore to pharmacology; finding drugs that actually work in asthma and COPD. Br. J. Pharmacol. 163 (2011), 44–52.
-
(2011)
Br. J. Pharmacol.
, vol.163
, pp. 44-52
-
-
Moulton, B.C.1
Fryer, A.D.2
-
70
-
-
0023661365
-
Distinct primary structures, ligand-binding properties and tissue-specific expression of four human muscarinic acetylcholine receptors
-
70 Peralta, E.G., et al. Distinct primary structures, ligand-binding properties and tissue-specific expression of four human muscarinic acetylcholine receptors. EMBO J. 6 (1987), 3923–3929.
-
(1987)
EMBO J.
, vol.6
, pp. 3923-3929
-
-
Peralta, E.G.1
-
71
-
-
33749358578
-
Quantifying the association and dissociation rates of unlabelled antagonists at the muscarinic M3 receptor
-
71 Dowling, M.R., Charlton, S.J., Quantifying the association and dissociation rates of unlabelled antagonists at the muscarinic M3 receptor. Br. J. Pharmacol. 148 (2006), 927–937.
-
(2006)
Br. J. Pharmacol.
, vol.148
, pp. 927-937
-
-
Dowling, M.R.1
Charlton, S.J.2
-
72
-
-
79955556415
-
Radiosynthesis and preliminary evaluation of 4-[18F]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylb enzamide as a new positron emission tomography ligand for metabotropic glutamate receptor subtype 1
-
72 Yamasaki, T., et al. Radiosynthesis and preliminary evaluation of 4-[18F]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylb enzamide as a new positron emission tomography ligand for metabotropic glutamate receptor subtype 1. Bioorg. Med. Chem. Lett. 21 (2011), 2998–3001.
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 2998-3001
-
-
Yamasaki, T.1
-
73
-
-
84904994581
-
Structure of class C GPCR metabotropic glutamate receptor 5 transmembrane domain
-
73 Dore, A.S., et al. Structure of class C GPCR metabotropic glutamate receptor 5 transmembrane domain. Nature 511 (2014), 557–562.
-
(2014)
Nature
, vol.511
, pp. 557-562
-
-
Dore, A.S.1
-
74
-
-
67349192597
-
Pharmacological characterization of the nociceptin/orphanin FQ receptor non peptide antagonist Compound 24
-
74 Fischetti, C., et al. Pharmacological characterization of the nociceptin/orphanin FQ receptor non peptide antagonist Compound 24. Eur. J. Pharmacol. 614 (2009), 50–57.
-
(2009)
Eur. J. Pharmacol.
, vol.614
, pp. 50-57
-
-
Fischetti, C.1
-
75
-
-
0041341923
-
Differential involvement of intracellular domains of the rat NTS1 neurotensin receptor in coupling to G proteins: a molecular basis for agonist-directed trafficking of receptor stimulus
-
75 Skrzydelski, D., et al. Differential involvement of intracellular domains of the rat NTS1 neurotensin receptor in coupling to G proteins: a molecular basis for agonist-directed trafficking of receptor stimulus. Mol. Pharmacol. 64 (2003), 421–429.
-
(2003)
Mol. Pharmacol.
, vol.64
, pp. 421-429
-
-
Skrzydelski, D.1
-
76
-
-
77954731181
-
Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H -1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia
-
76 Cox, C.D., et al. Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H -1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. J. Med. Chem. 53 (2010), 5320–5332.
-
(2010)
J. Med. Chem.
, vol.53
, pp. 5320-5332
-
-
Cox, C.D.1
-
77
-
-
84887945666
-
5-alkyl-1,3-oxazole derivatives of 6-amino-nicotinic acids as alkyl ester bioisosteres are antagonists of the P2Y12 receptor
-
77 Bach, P., et al. 5-alkyl-1,3-oxazole derivatives of 6-amino-nicotinic acids as alkyl ester bioisosteres are antagonists of the P2Y12 receptor. Future Med. Chem. 5 (2013), 2037–2056.
-
(2013)
Future Med. Chem.
, vol.5
, pp. 2037-2056
-
-
Bach, P.1
-
78
-
-
84874618577
-
Discovery of 2-(phenoxypyridine)-3-phenylureas as small molecule P2Y1 antagonists
-
78 Chao, H., et al. Discovery of 2-(phenoxypyridine)-3-phenylureas as small molecule P2Y1 antagonists. J. Med. Chem. 56 (2013), 1704–1714.
-
(2013)
J. Med. Chem.
, vol.56
, pp. 1704-1714
-
-
Chao, H.1
-
79
-
-
44949114152
-
Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity
-
79 Chackalamannil, S., et al. Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity. J. Med. Chem. 51 (2008), 3061–3064.
-
(2008)
J. Med. Chem.
, vol.51
, pp. 3061-3064
-
-
Chackalamannil, S.1
-
80
-
-
33746365908
-
Enhancement of capillary leakage and restoration of lymphocyte egress by a chiral S1P1 antagonist in vivo
-
80 Sanna, M.G., et al. Enhancement of capillary leakage and restoration of lymphocyte egress by a chiral S1P1 antagonist in vivo. Nat. Chem. Biol. 2 (2006), 434–441.
-
(2006)
Nat. Chem. Biol.
, vol.2
, pp. 434-441
-
-
Sanna, M.G.1
-
81
-
-
84932607395
-
MRT-92 inhibits Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor
-
81 Hoch, L., et al. MRT-92 inhibits Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor. FASEB J. 29 (2015), 1817–1829.
-
(2015)
FASEB J.
, vol.29
, pp. 1817-1829
-
-
Hoch, L.1
-
82
-
-
84876875551
-
Substituted 7-amino-5-thio-thiazolo[4,5-d]pyrimidines as potent and selective antagonists of the fractalkine receptor (CX3CR1)
-
82 Karlstrom, S., et al. Substituted 7-amino-5-thio-thiazolo[4,5-d]pyrimidines as potent and selective antagonists of the fractalkine receptor (CX3CR1). J. Med. Chem. 56 (2013), 3177–3190.
-
(2013)
J. Med. Chem.
, vol.56
, pp. 3177-3190
-
-
Karlstrom, S.1
-
83
-
-
0029134812
-
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification
-
83 Hieble, J.P., et al. Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification. J. Med. Chem. 38 (1995), 3415–3444.
-
(1995)
J. Med. Chem.
, vol.38
, pp. 3415-3444
-
-
Hieble, J.P.1
-
84
-
-
53349102957
-
Use of the X-ray structure of the beta2-adrenergic receptor for drug discovery. Part 2: identification of active compounds
-
84 Sabio, M., et al. Use of the X-ray structure of the beta2-adrenergic receptor for drug discovery. Part 2: identification of active compounds. Bioorg. Med. Chem. Lett. 18 (2008), 5391–5395.
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 5391-5395
-
-
Sabio, M.1
-
85
-
-
0028006303
-
Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors
-
85 Raynor, K., et al. Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors. Mol. Pharmacol. 45 (1994), 330–334.
-
(1994)
Mol. Pharmacol.
, vol.45
, pp. 330-334
-
-
Raynor, K.1
-
86
-
-
0036177994
-
Involvement of mu- and kappa-, but not delta-, opioid receptors in the peristaltic motor depression caused by endogenous and exogenous opioids in the guinea-pig intestine
-
86 Shahbazian, A., et al. Involvement of mu- and kappa-, but not delta-, opioid receptors in the peristaltic motor depression caused by endogenous and exogenous opioids in the guinea-pig intestine. Br. J. Pharmacol. 135 (2002), 741–750.
-
(2002)
Br. J. Pharmacol.
, vol.135
, pp. 741-750
-
-
Shahbazian, A.1
-
87
-
-
80053928946
-
Ligand-directed functional selectivity at the mu opioid receptor revealed by label-free integrative pharmacology on-target
-
87 Morse, M., et al. Ligand-directed functional selectivity at the mu opioid receptor revealed by label-free integrative pharmacology on-target. PLoS One, 6, 2011, e25643.
-
(2011)
PLoS One
, vol.6
, pp. e25643
-
-
Morse, M.1
|