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Page 1
Discovery of β2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor.
Aristotelous T, Ahn S, Shukla AK, Gawron S, Sassano MF, Kahsai AW, Wingler LM, Zhu X, Tripathi-Shukla P, Huang XP, Riley J, Besnard J, Read KD, Roth BL, Gilbert IH, Hopkins AL, Lefkowitz RJ, Navratilova I. Aristotelous T, et al. Among authors: kahsai aw. ACS Med Chem Lett. 2013 Oct 10;4(10):1005-1010. doi: 10.1021/ml400312j. Epub 2013 Sep 3. ACS Med Chem Lett. 2013. PMID: 24454993 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: kahsai aw. Nature. 2014 Aug 14;512(7513):218-222. doi: 10.1038/nature13430. Epub 2014 Jun 22. Nature. 2014. PMID: 25043026 Free PMC article.
Conformationally selective RNA aptamers allosterically modulate the β2-adrenoceptor.
Kahsai AW, Wisler JW, Lee J, Ahn S, Cahill Iii TJ, Dennison SM, Staus DP, Thomsen AR, Anasti KM, Pani B, Wingler LM, Desai H, Bompiani KM, Strachan RT, Qin X, Alam SM, Sullenger BA, Lefkowitz RJ. Kahsai AW, et al. Nat Chem Biol. 2016 Sep;12(9):709-16. doi: 10.1038/nchembio.2126. Epub 2016 Jul 11. Nat Chem Biol. 2016. PMID: 27398998 Free PMC article.
Allosteric nanobodies reveal the dynamic range and diverse mechanisms of G-protein-coupled receptor activation.
Staus DP, Strachan RT, Manglik A, Pani B, Kahsai AW, Kim TH, Wingler LM, Ahn S, Chatterjee A, Masoudi A, Kruse AC, Pardon E, Steyaert J, Weis WI, Prosser RS, Kobilka BK, Costa T, Lefkowitz RJ. Staus DP, et al. Among authors: kahsai aw. Nature. 2016 Jul 21;535(7612):448-52. doi: 10.1038/nature18636. Epub 2016 Jul 13. Nature. 2016. PMID: 27409812 Free PMC article.
GPCR-G Protein-β-Arrestin Super-Complex Mediates Sustained G Protein Signaling.
Thomsen ARB, Plouffe B, Cahill TJ 3rd, Shukla AK, Tarrasch JT, Dosey AM, Kahsai AW, Strachan RT, Pani B, Mahoney JP, Huang L, Breton B, Heydenreich FM, Sunahara RK, Skiniotis G, Bouvier M, Lefkowitz RJ. Thomsen ARB, et al. Among authors: kahsai aw. Cell. 2016 Aug 11;166(4):907-919. doi: 10.1016/j.cell.2016.07.004. Epub 2016 Aug 4. Cell. 2016. PMID: 27499021 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: kahsai aw. 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.
Arrestin-biased AT1R agonism induces acute catecholamine secretion through TRPC3 coupling.
Liu CH, Gong Z, Liang ZL, Liu ZX, Yang F, Sun YJ, Ma ML, Wang YJ, Ji CR, Wang YH, Wang MJ, Cui FA, Lin A, Zheng WS, He DF, Qu CX, Xiao P, Liu CY, Thomsen AR, Joseph Cahill T 3rd, Kahsai AW, Yi F, Xiao KH, Xue T, Zhou Z, Yu X, Sun JP. Liu CH, et al. Among authors: kahsai aw. Nat Commun. 2017 Feb 9;8:14335. doi: 10.1038/ncomms14335. Nat Commun. 2017. PMID: 28181498 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: kahsai aw. 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.
29 results