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Items: 19

1.

Small Molecule Positive Allosteric Modulators of the β2-Adrenoceptor Isolated from DNA Encoded Libraries.

Ahn S, Pani B, Kahsai AW, Olsen EK, Husemoen G, Vestrgaard 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.

Mol Pharmacol. 2018 May 16. pii: mol.118.111948. doi: 10.1124/mol.118.111948. [Epub ahead of print]

2.

Design, synthesis, and functional assessment of Cmpd-15 derivatives as negative allosteric modulators for the β2-adrenergic receptor.

Meng K, Shim P, Wang Q, Zhao S, Gu T, Kahsai AW, Ahn S, Chen X.

Bioorg Med Chem. 2018 May 15;26(9):2320-2330. doi: 10.1016/j.bmc.2018.03.023. Epub 2018 Mar 15.

PMID:
29588128
3.

Gq activity- and β-arrestin-1 scaffolding-mediated ADGRG2/CFTR coupling are required for male fertility.

Zhang DL, Sun YJ, Ma ML, Wang YJ, Lin H, Li RR, Liang ZL, Gao Y, Yang Z, He DF, Lin A, Mo H, Lu YJ, Li MJ, Kong W, Chung KY, Yi F, Li JY, Qin YY, Li J, Thomsen ARB, Kahsai AW, Chen ZJ, Xu ZG, Liu M, Li D, Yu X, Sun JP.

Elife. 2018 Feb 2;7. pii: e33432. doi: 10.7554/eLife.33432.

4.

Mechanism of intracellular allosteric β2AR antagonist revealed by X-ray crystal structure.

Liu X, Ahn S, Kahsai AW, Meng KC, Latorraca NR, Pani B, Venkatakrishnan AJ, Masoudi A, Weis WI, Dror RO, Chen X, Lefkowitz RJ, Kobilka BK.

Nature. 2017 Aug 24;548(7668):480-484. doi: 10.1038/nature23652. Epub 2017 Aug 16.

PMID:
28813418
5.

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.

Proc Natl Acad Sci U S A. 2017 Mar 7;114(10):2562-2567. doi: 10.1073/pnas.1701529114. Epub 2017 Feb 21.

6.

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.

Nat Commun. 2017 Feb 9;8:14335. doi: 10.1038/ncomms14335.

7.

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.

Proc Natl Acad Sci U S A. 2017 Feb 14;114(7):1708-1713. doi: 10.1073/pnas.1620645114. Epub 2017 Jan 27.

8.

Adaptive Activation of a Stress Response Pathway Improves Learning and Memory Through Gs and β-Arrestin-1-Regulated Lactate Metabolism.

Dong JH, Wang YJ, Cui M, Wang XJ, Zheng WS, Ma ML, Yang F, He DF, Hu QX, Zhang DL, Ning SL, Liu CH, Wang C, Wang Y, Li XY, Yi F, Lin A, Kahsai AW, Cahill TJ 3rd, Chen ZY, Yu X, Sun JP.

Biol Psychiatry. 2017 Apr 15;81(8):654-670. doi: 10.1016/j.biopsych.2016.09.025. Epub 2016 Oct 13.

PMID:
27916196
9.

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.

Cell. 2016 Aug 11;166(4):907-919. doi: 10.1016/j.cell.2016.07.004. Epub 2016 Aug 4.

10.

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.

Nature. 2016 Jul 21;535(7612):448-52. Epub 2016 Jul 13.

11.

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.

Nat Chem Biol. 2016 Sep;12(9):709-16. doi: 10.1038/nchembio.2126. Epub 2016 Jul 11.

12.

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.

Nature. 2014 Aug 14;512(7513):218-222. doi: 10.1038/nature13430. Epub 2014 Jun 22.

13.

Monitoring protein conformational changes and dynamics using stable-isotope labeling and mass spectrometry.

Kahsai AW, Rajagopal S, Sun J, Xiao K.

Nat Protoc. 2014;9(6):1301-19. doi: 10.1038/nprot.2014.075. Epub 2014 May 8.

14.

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.

ACS Med Chem Lett. 2013 Oct 10;4(10):1005-1010. Epub 2013 Sep 3.

15.

Multiple ligand-specific conformations of the β2-adrenergic receptor.

Kahsai AW, Xiao K, Rajagopal S, Ahn S, Shukla AK, Sun J, Oas TG, Lefkowitz RJ.

Nat Chem Biol. 2011 Aug 21;7(10):692-700. doi: 10.1038/nchembio.634.

16.

Cucurbitacin I inhibits cell motility by indirectly interfering with actin dynamics.

Knecht DA, LaFleur RA, Kahsai AW, Argueta CE, Beshir AB, Fenteany G.

PLoS One. 2010 Nov 24;5(11):e14039. doi: 10.1371/journal.pone.0014039.

17.

G protein-coupled receptor kinase 2 activates radixin, regulating membrane protrusion and motility in epithelial cells.

Kahsai AW, Zhu S, Fenteany G.

Biochim Biophys Acta. 2010 Feb;1803(2):300-10. doi: 10.1016/j.bbamcr.2009.11.002. Epub 2009 Nov 11.

18.

Analogs of tetrahydroisoquinoline natural products that inhibit cell migration and target galectin-3 outside of its carbohydrate-binding site.

Kahsai AW, Cui J, Kaniskan HU, Garner PP, Fenteany G.

J Biol Chem. 2008 Sep 5;283(36):24534-45. doi: 10.1074/jbc.M800006200. Epub 2008 Jun 13.

19.

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