title: Progress in structure based drug design for G protein-coupled receptors.
authors: Heptares Therapeutics Limited, BioPark, Welwyn Garden City, Hertfordshire, UK. miles.congreve@heptares.com
authors: Miles
authors: M
authors: Congreve
authors: Christopher J
authors: CJ
authors: Langmead
authors: Jonathan S
authors: JS
authors: Mason
authors: Fiona H
authors: FH
authors: Marshall
references: Trends Pharmacol Sci. 1999 May;20(5):184-7
references: 10354609
references: J Med Chem. 2008 Feb 14;51(3):581-8
references: 18198821
references: J Med Chem. 2010 Feb 11;53(3):1357-69
references: 20078106
references: Mini Rev Med Chem. 2005 Jun;5(6):555-61
references: 15974933
references: J Med Chem. 2009 Aug 27;52(16):5207-16
references: 19627087
references: Nature. 2011 Jan 13;469(7329):236-40
references: 21228876
references: Neuropharmacology. 2011 Jan;60(1):24-35
references: 20637785
references: Curr Top Med Chem. 2010;10(10):993-1018
references: 20370656
references: J Biol Chem. 2002 May 24;277(21):19056-63
references: 11891221
references: J Med Chem. 1997 Feb 14;40(4):528-37
references: 9046344
references: Trends Pharmacol Sci. 2008 Feb;29(2):79-83
references: 18194818
references: J Am Chem Soc. 2010 Aug 25;132(33):11443-5
references: 20669948
references: Br J Pharmacol. 2010 Apr;159(7):1429-39
references: 20233217
references: Proc Natl Acad Sci U S A. 2009 Apr 21;106(16):6843-8
references: 19342484
references: J Med Chem. 2005 Jul 28;48(15):4842-50
references: 16033264
references: J Med Chem. 2005 Jun 30;48(13):4312-31
references: 15974585
references: J Med Chem. 2008 Mar 27;51(6):1824-30
references: 18293909
references: Sci Signal. 2008 Sep 16;1(37):ra4
references: 18799424
references: J Med Chem. 2008 Aug 28;51(16):4978-85
references: 18680279
references: Nature. 2008 Jul 10;454(7201):183-7
references: 18563085
references: Science. 2011 Apr 15;332(6027):322-7
references: 21393508
references: Trends Biochem Sci. 2009 Jun;34(6):303-10
references: 19446460
references: J Med Chem. 2009 May 28;52(10):3284-92
references: 19402631
references: J Med Chem. 2009 Dec 10;52(23):7640-52
references: 19743865
references: Trends Pharmacol Sci. 1989 Jun;10(6):230-5
references: 2549665
references: Curr Top Med Chem. 2010;10(6):638-56
references: 20337589
references: J Comput Aided Mol Des. 2010 Aug;24(8):659-74
references: 20512399
references: J Am Chem Soc. 2008 Apr 16;130(15):5115-23
references: 18357984
references: J Med Chem. 2006 Jul 27;49(15):4470-6
references: 16854052
references: Br J Pharmacol. 1993 Aug;109(4):1169-77
references: 8401927
references: Curr Med Chem. 2006;13(14):1667-91
references: 16787212
references: Eur J Med Chem. 2010 Aug;45(8):3459-71
references: 20537438
references: J Med Chem. 2004 Oct 21;47(22):5393-404
references: 15481977
references: Br J Hosp Med. 1993 Feb 17-Mar 2;49(4):262-7
references: 8443626
references: Trends Neurosci. 2008 May;31(5):234-42
references: 18395805
references: Nat Rev Drug Discov. 2009 Jun;8(6):455-63
references: 19461661
references: Nat Med. 2007 Sep;13(9):1102-7
references: 17767166
references: J Med Chem. 2006 Jul 13;49(14):4008-16
references: 16821760
references: J Med Chem. 2004 Feb 12;47(4):888-99
references: 14761190
references: J Mol Recognit. 2005 Jan-Feb;18(1):60-72
references: 15386622
references: Nature. 2007 Nov 15;450(7168):383-7
references: 17952055
references: J Med Chem. 2006 Feb 9;49(3):984-94
references: 16451064
references: Proc Natl Acad Sci U S A. 2002 Apr 30;99(9):5982-7
references: 11972040
references: Science. 2010 Nov 19;330(6007):1066-71
references: 20929726
references: J Med Chem. 1998 Jul 30;41(16):2911-27
references: 9685229
references: Neuropharmacology. 1998 Aug;37(8):1043-51
references: 9833633
references: Trends Pharmacol Sci. 2006 Sep;27(9):475-81
references: 16889837
references: Drug Discov Today. 2009 Mar;14(5-6):291-7
references: 19121409
references: Bioorg Med Chem Lett. 2007 Oct 15;17(20):5552-7
references: 17765542
references: J Med Chem. 2010 May 13;53(9):3748-55
references: 20405927
references: Trends Biochem Sci. 2008 Oct;33(10):491-500
references: 18789697
references: Bioorg Med Chem Lett. 2010 Dec 15;20(24):7259-64
references: 21074436
references: Neuropsychopharmacology. 2010 Mar;35(4):855-69
references: 19940843
references: Structure. 2010 Sep 8;18(9):1083-93
references: 20826335
references: Nature. 2008 May 15;453(7193):363-7
references: 18480818
references: Curr Med Chem. 2010;17(12):1167-80
references: 20158474
references: Mol Pharmacol. 2009 Feb;75(2):331-41
references: 19001633
references: Pharmacol Ther. 2003 Jun;98(3):325-54
references: 12782243
references: Curr Opin Struct Biol. 2010 Aug;20(4):401-14
references: 20538452
references: Trends Pharmacol Sci. 2009 Mar;30(3):148-55
references: 19201489
references: Proc Natl Acad Sci U S A. 2009 Sep 15;106(37):15950-5
references: 19717450
references: Science. 2008 Nov 21;322(5905):1211-7
references: 18832607
references: Trends Pharmacol Sci. 2009 May;30(5):249-59
references: 19375807
references: Bioorg Med Chem. 2008 Apr 15;16(8):4378-89
references: 18342519
references: Bioorg Med Chem. 2008 Oct 15;16(20):9359-68
references: 18809332
references: J Mol Biol. 2007 Oct 5;372(5):1179-88
references: 17825322
references: Curr Opin Pharmacol. 2009 Oct;9(5):615-21
references: 19477685
references: Proc Natl Acad Sci U S A. 2008 Apr 1;105(13):5034-9
references: 18375760
references: Proc Natl Acad Sci U S A. 2006 Oct 31;103(44):16123-8
references: 17060607
references: J Med Chem. 2009 Aug 13;52(15):4923-35
references: 19606869
references: Biophys J. 2010 Oct 6;99(7):2366-73
references: 20923672
references: Bioorg Med Chem. 2009 Dec 1;17(23):7987-92
references: 19857969
references: Science. 2000 Aug 4;289(5480):739-45
references: 10926528
references: Adv Drug Deliv Rev. 2001 Mar 1;46(1-3):3-26
references: 11259830
references: ACS Chem Biol. 2008 Sep 19;3(9):530-41
references: 18652471
references: Mol Interv. 2009 Jun;9(3):125-35
references: 19592673
references: Proc Natl Acad Sci U S A. 2007 Mar 6;104(10):3759-64
references: 17360426
references: J Biol Chem. 2004 Jul 9;279(28):29085-91
references: 15126507
references: Drug Discov Today. 2009 Jul;14(13-14):668-75
references: 19427404
references: Science. 2007 Nov 23;318(5854):1258-65
references: 17962520
references: Nature. 2011 Jan 13;469(7329):241-4
references: 21228877
references: Science. 2010 Nov 19;330(6007):1091-5
references: 21097933
references: J Mol Model. 2009 Oct;15(10):1203-11
references: 19263094
references: J Biol Chem. 2008 Nov 21;283(47):32900-12
references: 18801728
references: Mol Pharmacol. 2006 Jan;69(1):236-46
references: 16207821
references: Trends Pharmacol Sci. 2010 Dec;31(12):567-74
references: 20870300
references: Trends Biochem Sci. 2009 Nov;34(11):540-52
references: 19836958
references: Methods Enzymol. 2011;493:115-36
references: 21371589
references: Nature. 2011 Jan 13;469(7329):175-80
references: 21228869
references: Annu Rev Pharmacol Toxicol. 2007;47:1-51
references: 17009927
references: Curr Top Med Chem. 2007;7(16):1600-29
references: 17979771
references: J Med Chem. 2010 Aug 12;53(15):5383-99
references: 20369879
references: Bioorg Med Chem Lett. 2008 Oct 15;18(20):5391-5
references: 18829308
references: Structure. 2008 Jun;16(6):897-905
references: 18547522
references: ChemMedChem. 2010 Aug 2;5(8):1300-17
references: 20544783
references: J Biol Chem. 2008 Jun 27;283(26):17753-6
references: 18463093
references: Neuropharmacology. 2011 Jan;60(1):36-44
references: 20624408
references: Bioorg Med Chem. 2010 Apr 1;18(7):2524-36
references: 20304654
references: J Mol Biol. 2004 Nov 5;343(5):1409-38
references: 15491621
references: J Med Chem. 2009 Jan 22;52(2):433-44
references: 19115816
references: Proc Natl Acad Sci U S A. 2004 Aug 31;101(35):12836-41
references: 15326300
references: Mol Pharmacol. 2003 Oct;64(4):798-810
references: 14500736
references: J Chem Inf Model. 2010 Jan;50(1):155-69
references: 19919042
references: J Biol Chem. 1994 Sep 2;269(35):22054-8
references: 7520910
references: Int J Clin Pract. 2009 Aug;63(8):1154-60
references: 19624785
references: Nat Rev Drug Discov. 2009 Jan;8(1):41-54
references: 19116626
references: Mol Pharmacol. 2000 Jul;58(1):194-207
references: 10860942
references: Nature. 2000 Oct 26;407(6807):971-7
references: 11069170
references: Mol Pharmacol. 2008 Nov;74(5):1193-202
references: 18676678
references: J Med Chem. 2009 May 14;52(9):2923-32
references: 19374402
references: Curr Top Med Chem. 2010;10(10):976-92
references: 20370657
references: Bioorg Med Chem Lett. 2009 Jul 1;19(13):3471-5
references: 19457667
references: J Med Chem. 2009 Apr 23;52(8):2407-19
references: 19301821
references: J Med Chem. 1985 Jul;28(7):849-57
references: 3892003
references: Bioorg Med Chem Lett. 2010 Jun 15;20(12):3545-9
references: 20483599
references: Curr Top Med Chem. 2007;7(10):991-8
references: 17508932
references: J Mol Biol. 2004 Sep 10;342(2):571-83
references: 15327956
references: Nature. 1993 Apr 22;362(6422):770-2
references: 8469290
references: Structure. 2009 Jan 14;17(1):8-14
references: 19141277
references: J Med Chem. 2010 Nov 25;53(22):7918-31
references: 20979417
references: Curr Opin Drug Discov Devel. 2010 May;13(3):317-25
references: 20443165
references: Nature. 2011 Mar 31;471(7340):651-5
references: 21389988
references: J Med Chem. 2008 Feb 14;51(3):603-11
references: 18201064
references: J Med Chem. 2006 Oct 19;49(21):6170-6
references: 17034124
references: Nature. 2010 Jan 7;463(7277):108-12
references: 20054398
references: Annu Rev Biophys. 2010;39:309-28
references: 20192770
references: Expert Opin Pharmacother. 2006 Jun;7(8):1055-64
references: 16722815
references: J Med Chem. 2007 Jan 25;50(2):233-40
references: 17228865
references: Bioorg Med Chem. 2009 Jul 15;17(14):5259-74
references: 19501513
references: Nature. 2008 Jul 24;454(7203):486-91
references: 18594507
references: Curr Opin Struct Biol. 2008 Dec;18(6):734-40
references: 18957321
references: IDrugs. 2010 Dec;13(12):869-73
references: 21154145
references: J Mol Biol. 2008 Jul 18;380(4):648-55
references: 18554610
references: Bioorg Med Chem. 2010 Aug 1;18(15):5562-75
references: 20621490
references: Nat Rev Drug Discov. 2002 Sep;1(9):727-30
references: 12209152
references: J Med Chem. 1999 Mar 25;42(6):1027-40
references: 10090786
references: Bioorg Med Chem Lett. 2009 Aug 15;19(16):4679-83
references: 19608416
references: Mol Pharmacol. 2008 Mar;73(3):855-67
references: 18042736
references: J Biol Chem. 2008 Oct 24;283(43):29312-21
references: 18723515
references: Expert Opin Emerg Drugs. 2009 Mar;14(1):129-44
references: 19249985
references: Nature. 2009 May 21;459(7245):356-63
references: 19458711
references: Annu Rev Pharmacol Toxicol. 2008;48:107-41
references: 17848137
references: J Med Chem. 2003 Nov 6;46(23):4847-59
references: 14584936
references: Mol Pharmacol. 2002 Jun;61(6):1297-302
references: 12021390
references: IDrugs. 2003 Jun;6(6):587-92
references: 12811682
references: J Pharmacol Exp Ther. 2004 Feb;308(2):627-35
references: 14593085
references: J Chem Inf Model. 2008 May;48(5):1104-17
references: 18442221
references: Nat Rev Neurol. 2010 Oct;6(10):573-82
references: 20820195
references: Proteins. 2010 Jan;78(1):197-211
references: 20063437
references: Drug Discov Today. 2004 May 15;9(10):430-1
references: 15109945
references: J Biol Chem. 2000 Oct 27;275(43):33750-8
references: 10934211
references: J Med Chem. 2008 Jul 10;51(13):3661-80
references: 18457385
references: Angew Chem Int Ed Engl. 2010 Feb 15;49(8):1426-9
references: 20084646
references: Nature. 2011 May 18;474(7352):521-5
references: 21593763
references: Bioorg Med Chem Lett. 2006 May 15;16(10):2791-5
references: 16529929
references: Bioorg Med Chem Lett. 2008 Sep 15;18(18):4963-7
references: 18760600
references: ACS Med Chem Lett. 2010 May 10;1(4):160-4
references: 24900189
references: J Med Chem. 2011 Jul 14;54(13):4312-23
references: 21661720
references: J Med Chem. 2009 May 28;52(10):3166-73
references: 19397376
references: J Med Chem. 2008 Dec 25;51(24):7653-62
references: 18983141
references: J Biol Chem. 2010 Feb 5;285(6):3973-3985
references: 19920139
references: Mol Pharmacol. 1998 Jan;53(1):128-34
references: 9443940
references: Curr Pharm Des. 2009;15(35):4049-68
references: 20028321
references: J Med Chem. 2008 Apr 10;51(7):2108-14
references: 18333607
references: Bioorg Med Chem Lett. 2008 Mar 1;18(5):1598-602
references: 18243704
references: J Med Chem. 2010 Apr 22;53(8):3361-75
references: 20307065
references: Curr Opin Pharmacol. 2009 Oct;9(5):629-35
references: 19443270
references: Nat Rev Drug Discov. 2008 Apr;7(4):339-57
references: 18382464
references: Nat Rev Drug Discov. 2007 Nov;6(11):881-90
references: 17971784
references: J Med Chem. 2010 Feb 11;53(3):1338-46
references: 20047331
references: Pharmacol Rev. 2011 Mar;63(1):59-126
references: 21228259
references: Nature. 2011 Mar 31;471(7340):656-60
references: 21389983
references: Neuropharmacology. 2011 Jan;60(1):93-101
references: 20705075
references: J Leukoc Biol. 1995 May;57(5):703-11
references: 7759949
references: J Am Chem Soc. 2003 Jun 25;125(25):7516-7
references: 12812482
references: Structure. 2011 Sep 7;19(9):1283-93
references: 21885291
references: Philos Trans R Soc Lond B Biol Sci. 1990 Jan 30;326(1236):379-89
references: 1970644
references: Nature. 2008 Sep 25;455(7212):497-502
references: 18818650
references: Trends Pharmacol Sci. 2004 Apr;25(4):186-92
references: 15063082
references: J Med Chem. 2008 May 22;51(10):2907-14
references: 18442228
references: J Chem Inf Model. 2010 Apr 26;50(4):626-37
references: 20187660