Supplementary Table 1: References Receptor Citation
ADRB1 Baker JG, Proudman RG, Hawley NC, Fischer PM, Hill SJ. Role of key transmembrane residues in agonist and antagonist actions at the two conformations of the human beta1-adrenoceptor. Mol Pharmacol 2008; 74(5): 1246-1260.
Baker JG, Proudman RG, Hill SJ. Salmeterol's extreme beta2 selectivity is due to residues in both extracellular loops and
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Behr B, Hoffmann C, Ottolina G, Klotz KN. Novel mutants of the human beta1-adrenergic receptor reveal amino acids relevant for receptor activation. J Biol Chem 2006; 281(26): 18120-18125.
Isogaya M, Sugimoto Y, Tanimura R, Tanaka R, Kikkawa H, Nagao T, et al. Binding pockets of the beta(1)- and beta(2)-adrenergic receptors for subtype-selective agonists. Mol
Pharmacol 1999; 56(5): 875-885.
Rathz DA, Brown KM, Kramer LA, Liggett SB. Amino acid 49 polymorphisms of the human beta1-adrenergic receptor affect agonist-promoted trafficking. J Cardiovasc
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Rezmann-Vitti LA, Louis SN, Nero TL, Jackman GP, Iakovidis D, Machida CA, et al. Agonist binding and activation of the rat beta(1)-adrenergic receptor: role of Trp(134(3.28)),
Ser(190(4.57)) and Tyr(356(7.43)). Biochem Pharmacol 2004; 68(4): 675-688.
Rezmann-Vitti LA, Louis SN, Nero TL, Jackman GP, Machida CA, Louis WJ. Site-directed mutagenesis of the rat beta1-
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)cyanopindolol but not (+/-)[125Iodo]cyanopindolol binding. Eur J Med Chem 2004; 39(7): 625-631.
Rezmann-Vitti LA, Nero TL, Jackman GP, Machida CA, Duke BJ, Louis WJ, et al. Role of Tyr(356(7.43)) and Ser(190(4.57)) in antagonist binding in the rat beta1-adrenergic receptor. J Med Chem 2006; 49(12): 3467-3477.
ADRB2 Arakawa M, Chakraborty R, Upadhyaya J, Eilers M, Reeves PJ, Smith SO, et al. Structural and functional roles of small group- conserved amino acids present on helix-H7 in the beta(2)-
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Baker JG, Proudman RG, Hill SJ. Salmeterol's extreme beta2 selectivity is due to residues in both extracellular loops and
transmembrane domains. Mol Pharmacol 2015; 87(1): 103-120.
Chung FZ, Wang CD, Potter PC, Venter JC, Fraser CM. Site- directed mutagenesis and continuous expression of human beta- adrenergic receptors. Identification of a conserved aspartate residue involved in agonist binding and receptor activation. J Biol Chem 1988; 263(9): 4052-4055.
Del Carmine R, Molinari P, Sbraccia M, Ambrosio C, Costa T.
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Fraser CM, Chung FZ, Wang CD, Venter JC. Site-directed
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Green SA, Cole G, Jacinto M, Innis M, Liggett SB. A polymorphism of the human beta 2-adrenergic receptor within the fourth
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Green SA, Rathz DA, Schuster AJ, Liggett SB. The Ile164 beta(2)- adrenoceptor polymorphism alters salmeterol exosite binding and conventional agonist coupling to G(s). Eur J
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Isogaya M, Sugimoto Y, Tanimura R, Tanaka R, Kikkawa H, Nagao T, et al. Binding pockets of the beta(1)- and beta(2)-adrenergic receptors for subtype-selective agonists. Mol
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Kikkawa H, Isogaya M, Nagao T, Kurose H. The role of the
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Noda K, Saad Y, Graham RM, Karnik SS. The high affinity state of the beta 2-adrenergic receptor requires unique interaction
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Ericksen SS, Cummings DF, Teer ME, Amdani S, Schetz JA. Ring substituents on substituted benzamide ligands indirectly mediate interactions with position 7.39 of transmembrane helix 7 of the D4 dopamine receptor. J Pharmacol Exp Ther 2012; 342(2): 472- 485.
Ericksen SS, Cummings DF, Weinstein H, Schetz JA. Ligand selectivity of D2 dopamine receptors is modulated by changes in local dynamics produced by sodium binding. J Pharmacol Exp Ther 2009; 328(1): 40-54.
Fowler JC, Bhattacharya S, Urban JD, Vaidehi N, Mailman RB.
Receptor conformations involved in dopamine D(2L) receptor functional selectivity induced by selected transmembrane-5 serine mutations. Mol Pharmacol 2012; 81(6): 820-831.
Lan H, Durand CJ, Teeter MM, Neve KA. Structural determinants of pharmacological specificity between D(1) and D(2) dopamine receptors. Mol Pharmacol 2006; 69(1): 185-194.
Mansour A, Meng F, Meador-Woodruff JH, Taylor LP, Civelli O, Akil H. Site-directed mutagenesis of the human dopamine D2
receptor. Eur J Pharmacol 1992; 227(2): 205-214.
Michino M, Donthamsetti P, Beuming T, Banala A, Duan L, Roux T, et al. A single glycine in extracellular loop 1 is the critical determinant for pharmacological specificity of dopamine D2 and D3 receptors. Mol Pharmacol 2013; 84(6): 854-864.
Simpson MM, Ballesteros JA, Chiappa V, Chen J, Suehiro M, Hartman DS, et al. Dopamine D4/D2 receptor selectivity is determined by A divergent aromatic microdomain contained within the second, third, and seventh membrane-spanning segments. Mol Pharmacol 1999; 56(6): 1116-1126.
Tschammer N, Bollinger S, Kenakin T, Gmeiner P. Histidine 6.55 is a major determinant of ligand-biased signaling in dopamine D2L receptor. Mol Pharmacol 2011; 79(3): 575-585.
Tschammer N, Dorfler M, Hubner H, Gmeiner P. Engineering a GPCR-ligand pair that simulates the activation of D(2L) by Dopamine. ACS Chem Neurosci 2010; 1(1): 25-35.
Wilcox RE, Huang WH, Brusniak MY, Wilcox DM, Pearlman RS, Teeter MM, et al. CoMFA-based prediction of agonist affinities at recombinant wild type versus serine to alanine point mutated D2 dopamine receptors. J Med Chem 2000; 43(16): 3005-3019.
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Investigation of the role of conserved serine residues in the long form of the rat D2 dopamine receptor using site-directed
mutagenesis. J Neurochem 1996; 66(1): 394-402.
Woodward R, Daniell SJ, Strange PG, Naylor LH. Structural
studies on D2 dopamine receptors: mutation of a histidine residue specifically affects the binding of a subgroup of substituted
benzamide drugs. J Neurochem 1994; 62(5): 1664-1669.
AGTR1 Bhuiyan MA, Hossain M, Ishiguro M, Nakamura T, Nagatomo T.
Engineered mutation of some important amino acids in
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Fierens FL, Vanderheyden PM, Gaborik Z, Minh TL, Backer JP, Hunyady L, et al. Lys(199) mutation of the human angiotensin type 1 receptor differentially affects the binding of surmountable and insurmountable non-peptide antagonists. J Renin Angiotensin Aldosterone Syst 2000; 1(3): 283-288.
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Residues Val254, His256, and Phe259 of the angiotensin II AT1 receptor are not involved in ligand binding but participate in signal transduction. Mol Endocrinol 1998; 12(6): 810-814.
Hunyady L, Ji H, Jagadeesh G, Zhang M, Gaborik Z, Mihalik B, et al. Dependence of AT1 angiotensin receptor function on adjacent asparagine residues in the seventh transmembrane helix. Mol Pharmacol 1998; 54(2): 427-434.
Ji H, Leung M, Zhang Y, Catt KJ, Sandberg K. Differential structural requirements for specific binding of nonpeptide and peptide antagonists to the AT1 angiotensin receptor.
Identification of amino acid residues that determine binding of the antihypertensive drug losartan. J Biol
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Le MT, Vanderheyden PM, Szaszak M, Hunyady L, Kersemans V, Vauquelin G. Peptide and nonpeptide antagonist interaction with constitutively active human AT1 receptors. Biochem
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Miura S, Kiya Y, Kanazawa T, Imaizumi S, Fujino M, Matsuo Y, et al. Differential bonding interactions of inverse agonists of
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Monnot C, Bihoreau C, Conchon S, Curnow KM, Corvol P, Clauser E. Polar residues in the transmembrane domains of the type 1 angiotensin II receptor are required for binding and coupling.
Reconstitution of the binding site by co-expression of two deficient mutants. J Biol Chem 1996; 271(3): 1507-1513.
Nirula V, Zheng W, Sothinathan R, Sandberg K. Interaction of biphenylimidazole and imidazoleacrylic acid nonpeptide
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Noda K, Feng YH, Liu XP, Saad Y, Husain A, Karnik SS. The active state of the AT1 angiotensin receptor is generated by angiotensin II induction. Biochemistry 1996; 35(51): 16435-16442.
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Ohyama K, Yamano Y, Sano T, Nakagomi Y, Hamakubo T, Morishima I, et al. Disulfide bridges in extracellular domains of angiotensin II receptor type IA. Regul Pept 1995; 57(2): 141- 147.
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Perlman S, Schambye HT, Rivero RA, Greenlee WJ, Hjorth SA, Schwartz TW. Non-peptide angiotensin agonist. Functional and molecular interaction with the AT1 receptor. J Biol
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Schambye HT, Hjorth SA, Bergsma DJ, Sathe G, Schwartz TW.
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OPRM1 Beyer A, Koch T, Schroder H, Schulz S, Hollt V. Effect of the A118G polymorphism on binding affinity, potency and agonist- mediated endocytosis, desensitization, and resensitization of the human mu-opioid receptor. J Neurochem 2004; 89(3): 553-560.
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Bot G, Blake AD, Li S, Reisine T. Mutagenesis of a single amino acid in the rat mu-opioid receptor discriminates ligand binding. J Neurochem 1998; 70(1): 358-365.
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