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Small-Molecule Positive Allosteric Modulators of the β2-Adrenoceptor Isolated from DNA-Encoded Libraries.
Ahn S, Pani B, Kahsai AW, Olsen EK, Husemoen G, Vestergaard M, Jin L, Zhao S, Wingler LM, Rambarat PK, Simhal RK, Xu TT, Sun LD, Shim PJ, Staus DP, Huang LY, Franch T, Chen X, Lefkowitz RJ. Ahn S, et al. Among authors: chen x. Mol Pharmacol. 2018 Aug;94(2):850-861. doi: 10.1124/mol.118.111948. Epub 2018 May 16. Mol Pharmacol. 2018. PMID: 29769246 Free PMC article.
Visualization of arrestin recruitment by a G-protein-coupled receptor.
Shukla AK, Westfield GH, Xiao K, Reis RI, Huang LY, Tripathi-Shukla P, Qian J, Li S, Blanc A, Oleskie AN, Dosey AM, Su M, Liang CR, Gu LL, Shan JM, Chen X, Hanna R, Choi M, Yao XJ, Klink BU, Kahsai AW, Sidhu SS, Koide S, Penczek PA, Kossiakoff AA, Woods VL Jr, Kobilka BK, Skiniotis G, Lefkowitz RJ. Shukla AK, et al. Among authors: chen x. Nature. 2014 Aug 14;512(7513):218-222. doi: 10.1038/nature13430. Epub 2014 Jun 22. Nature. 2014. PMID: 25043026 Free PMC article.
Structure of an endosomal signaling GPCR-G protein-β-arrestin megacomplex.
Nguyen AH, Thomsen ARB, Cahill TJ 3rd, Huang R, Huang LY, Marcink T, Clarke OB, Heissel S, Masoudi A, Ben-Hail D, Samaan F, Dandey VP, Tan YZ, Hong C, Mahoney JP, Triest S, Little J 4th, Chen X, Sunahara R, Steyaert J, Molina H, Yu Z, des Georges A, Lefkowitz RJ. Nguyen AH, et al. Among authors: chen x. Nat Struct Mol Biol. 2019 Dec;26(12):1123-1131. doi: 10.1038/s41594-019-0330-y. Epub 2019 Nov 18. Nat Struct Mol Biol. 2019. PMID: 31740855 Free PMC article.
Allosteric "beta-blocker" isolated from a DNA-encoded small molecule library.
Ahn S, Kahsai AW, Pani B, Wang QT, Zhao S, Wall AL, Strachan RT, Staus DP, Wingler LM, Sun LD, Sinnaeve J, Choi M, Cho T, Xu TT, Hansen GM, Burnett MB, Lamerdin JE, Bassoni DL, Gavino BJ, Husemoen G, Olsen EK, Franch T, Costanzi S, Chen X, Lefkowitz RJ. Ahn S, et al. Among authors: chen x. Proc Natl Acad Sci U S A. 2017 Feb 14;114(7):1708-1713. doi: 10.1073/pnas.1620645114. Epub 2017 Jan 27. Proc Natl Acad Sci U S A. 2017. PMID: 28130548 Free PMC article.
Distinct conformations of GPCR-β-arrestin complexes mediate desensitization, signaling, and endocytosis.
Cahill TJ 3rd, Thomsen AR, Tarrasch JT, Plouffe B, Nguyen AH, Yang F, Huang LY, Kahsai AW, Bassoni DL, Gavino BJ, Lamerdin JE, Triest S, Shukla AK, Berger B, Little J 4th, Antar A, Blanc A, Qu CX, Chen X, Kawakami K, Inoue A, Aoki J, Steyaert J, Sun JP, Bouvier M, Skiniotis G, Lefkowitz RJ. Cahill TJ 3rd, et al. Among authors: chen x. Proc Natl Acad Sci U S A. 2017 Mar 7;114(10):2562-2567. doi: 10.1073/pnas.1701529114. Epub 2017 Feb 21. Proc Natl Acad Sci U S A. 2017. PMID: 28223524 Free PMC article.
Allosteric ligands for the pharmacologically dark receptors GPR68 and GPR65.
Huang XP, Karpiak J, Kroeze WK, Zhu H, Chen X, Moy SS, Saddoris KA, Nikolova VD, Farrell MS, Wang S, Mangano TJ, Deshpande DA, Jiang A, Penn RB, Jin J, Koller BH, Kenakin T, Shoichet BK, Roth BL. Huang XP, et al. Among authors: chen x. Nature. 2015 Nov 26;527(7579):477-83. doi: 10.1038/nature15699. Epub 2015 Nov 9. Nature. 2015. PMID: 26550826 Free PMC article.
Functional competence of a partially engaged GPCR-β-arrestin complex.
Kumari P, Srivastava A, Banerjee R, Ghosh E, Gupta P, Ranjan R, Chen X, Gupta B, Gupta C, Jaiman D, Shukla AK. Kumari P, et al. Among authors: chen x. Nat Commun. 2016 Nov 9;7:13416. doi: 10.1038/ncomms13416. Nat Commun. 2016. PMID: 27827372 Free PMC article.
Topoisomerase inhibitors unsilence the dormant allele of Ube3a in neurons.
Huang HS, Allen JA, Mabb AM, King IF, Miriyala J, Taylor-Blake B, Sciaky N, Dutton JW Jr, Lee HM, Chen X, Jin J, Bridges AS, Zylka MJ, Roth BL, Philpot BD. Huang HS, et al. Among authors: chen x. Nature. 2011 Dec 21;481(7380):185-9. doi: 10.1038/nature10726. Nature. 2011. PMID: 22190039 Free PMC article.
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