Format
Sort by
Items per page

Send to

Choose Destination

Search results

Items: 24

1.

A High-Throughput BRET Cellular Target Engagement Assay Links Biochemical to Cellular Activity for Bruton's Tyrosine Kinase.

Ong LL, Vasta JD, Monereau L, Locke G, Ribeiro H, Pattoli MA, Skala S, Burke JR, Watterson SH, Tino JA, Meisenheimer PL, Arey B, Lippy J, Zhang L, Robers MB, Tebben A, Chaudhry C.

SLAS Discov. 2019 Nov 9:2472555219884881. doi: 10.1177/2472555219884881. [Epub ahead of print]

PMID:
31709883
2.

Autoimmune pathways in mice and humans are blocked by pharmacological stabilization of the TYK2 pseudokinase domain.

Burke JR, Cheng L, Gillooly KM, Strnad J, Zupa-Fernandez A, Catlett IM, Zhang Y, Heimrich EM, McIntyre KW, Cunningham MD, Carman JA, Zhou X, Banas D, Chaudhry C, Li S, D'Arienzo C, Chimalakonda A, Yang X, Xie JH, Pang J, Zhao Q, Rose SM, Huang J, Moslin RM, Wrobleski ST, Weinstein DS, Salter-Cid LM.

Sci Transl Med. 2019 Jul 24;11(502). pii: eaaw1736. doi: 10.1126/scitranslmed.aaw1736.

PMID:
31341059
3.

Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.

Wrobleski ST, Moslin R, Lin S, Zhang Y, Spergel S, Kempson J, Tokarski JS, Strnad J, Zupa-Fernandez A, Cheng L, Shuster D, Gillooly K, Yang X, Heimrich E, McIntyre KW, Chaudhry C, Khan J, Ruzanov M, Tredup J, Mulligan D, Xie D, Sun H, Huang C, D'Arienzo C, Aranibar N, Chiney M, Chimalakonda A, Pitts WJ, Lombardo L, Carter PH, Burke JR, Weinstein DS.

J Med Chem. 2019 Oct 24;62(20):8973-8995. doi: 10.1021/acs.jmedchem.9b00444. Epub 2019 Jul 18.

PMID:
31318208
4.

Identification of N-Methyl Nicotinamide and N-Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2).

Moslin R, Zhang Y, Wrobleski ST, Lin S, Mertzman M, Spergel S, Tokarski JS, Strnad J, Gillooly K, McIntyre KW, Zupa-Fernandez A, Cheng L, Sun H, Chaudhry C, Huang C, D'Arienzo C, Heimrich E, Yang X, Muckelbauer JK, Chang C, Tredup J, Mulligan D, Xie D, Aranibar N, Chiney M, Burke JR, Lombardo L, Carter PH, Weinstein DS.

J Med Chem. 2019 Oct 24;62(20):8953-8972. doi: 10.1021/acs.jmedchem.9b00443. Epub 2019 Jul 17.

PMID:
31314518
5.

Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK).

Watterson SH, Liu Q, Beaudoin Bertrand M, Batt DG, Li L, Pattoli MA, Skala S, Cheng L, Obermeier MT, Moore R, Yang Z, Vickery R, Elzinga PA, Discenza L, D'Arienzo C, Gillooly KM, Taylor TL, Pulicicchio C, Zhang Y, Heimrich E, McIntyre KW, Ruan Q, Westhouse RA, Catlett IM, Zheng N, Chaudhry C, Dai J, Galella MA, Tebben AJ, Pokross M, Li J, Zhao R, Smith D, Rampulla R, Allentoff A, Wallace MA, Mathur A, Salter-Cid L, Macor JE, Carter PH, Fura A, Burke JR, Tino JA.

J Med Chem. 2019 Apr 11;62(7):3228-3250. doi: 10.1021/acs.jmedchem.9b00167. Epub 2019 Mar 29.

PMID:
30893553
6.

Identification of Imidazo[1,2-b]pyridazine Derivatives as Potent, Selective, and Orally Active Tyk2 JH2 Inhibitors.

Liu C, Lin J, Moslin R, Tokarski JS, Muckelbauer J, Chang C, Tredup J, Xie D, Park H, Li P, Wu DR, Strnad J, Zupa-Fernandez A, Cheng L, Chaudhry C, Chen J, Chen C, Sun H, Elzinga P, D'arienzo C, Gillooly K, Taylor TL, McIntyre KW, Salter-Cid L, Lombardo LJ, Carter PH, Aranibar N, Burke JR, Weinstein DS.

ACS Med Chem Lett. 2019 Feb 21;10(3):383-388. doi: 10.1021/acsmedchemlett.9b00035. eCollection 2019 Mar 14.

PMID:
30891145
7.

Conversion of carbazole carboxamide based reversible inhibitors of Bruton's tyrosine kinase (BTK) into potent, selective irreversible inhibitors in the carbazole, tetrahydrocarbazole, and a new 2,3-dimethylindole series.

Liu Q, Batt DG, Chaudhry C, Lippy JS, Pattoli MA, Surti N, Xu S, Carter PH, Burke JR, Tino JA.

Bioorg Med Chem Lett. 2018 Oct 1;28(18):3080-3084. doi: 10.1016/j.bmcl.2018.07.041. Epub 2018 Jul 30.

PMID:
30097367
8.

Discovery of highly potent, selective, covalent inhibitors of JAK3.

Kempson J, Ovalle D, Guo J, Wrobleski ST, Lin S, Spergel SH, Duan JJ, Jiang B, Lu Z, Das J, Yang BV, Hynes J Jr, Wu H, Tokarski J, Sack JS, Khan J, Schieven G, Blatt Y, Chaudhry C, Salter-Cid LM, Fura A, Barrish JC, Carter PH, Pitts WJ.

Bioorg Med Chem Lett. 2017 Oct 15;27(20):4622-4625. doi: 10.1016/j.bmcl.2017.09.023. Epub 2017 Sep 11.

PMID:
28927786
9.

Identification of imidazo[1,2-b]pyridazine TYK2 pseudokinase ligands as potent and selective allosteric inhibitors of TYK2 signalling.

Moslin R, Gardner D, Santella J, Zhang Y, Duncia JV, Liu C, Lin J, Tokarski JS, Strnad J, Pedicord D, Chen J, Blat Y, Zupa-Fernandez A, Cheng L, Sun H, Chaudhry C, Huang C, D'Arienzo C, Sack JS, Muckelbauer JK, Chang C, Tredup J, Xie D, Aranibar N, Burke JR, Carter PH, Weinstein DS.

Medchemcomm. 2016 Dec 15;8(4):700-712. doi: 10.1039/c6md00560h. eCollection 2017 Apr 1.

10.

Ultrasensitive quantitative LC-MS/MS of an inhibitor of apoptosis protein's antagonist in plasma using protein target affinity extraction.

Discenza LN, Cornelius G, Gan J, Szapiel N, Talbott RL, Chaudhry C, Roy A, Borzilleri RM, Vuppugalla R, Stefanski K, Moore R, D'Arienzo CJ, Olah TV, Mehl JT.

Bioanalysis. 2016 Feb;8(4):265-74. doi: 10.4155/bio.15.246. Epub 2016 Jan 25.

PMID:
26807991
11.

Building homogeneous time-resolved fluorescence resonance energy transfer assays for characterization of bivalent inhibitors of an inhibitor of apoptosis protein target.

Chaudhry C, Davis J, Zhang Y, Posy S, Lei M, Shen H, Yan C, Devaux B, Zhang L, Blat Y, Metzler W, Borzilleri RM, Talbott RL.

Anal Biochem. 2016 Mar 15;497:8-17. doi: 10.1016/j.ab.2015.11.026. Epub 2015 Dec 30.

PMID:
26743718
12.

Pharmacology of smac mimetics; chemotype differentiation based on physical association with caspase regulators and cellular transport.

Talbott RL, Borzilleri RM, Chaudhry C, Fargnoli J, Shen H, Fairchild C, Barnhart B, Ortega M, McDonagh TE, Vuppugalla R, Vite GD, Hunt JT, Gottardis M, Naglich JG.

Exp Cell Res. 2015 Nov 1;338(2):251-60. doi: 10.1016/j.yexcr.2015.08.011. Epub 2015 Aug 21.

PMID:
26302264
13.

Dimeric Macrocyclic Antagonists of Inhibitor of Apoptosis Proteins for the Treatment of Cancer.

Zhang Y, Seigal BA, Terrett NK, Talbott RL, Fargnoli J, Naglich JG, Chaudhry C, Posy SL, Vuppugalla R, Cornelius G, Lei M, Wang C, Zhang Y, Schmidt RJ, Wei DD, Miller MM, Allen MP, Li L, Carter PH, Vite GD, Borzilleri RM.

ACS Med Chem Lett. 2015 May 27;6(7):770-5. doi: 10.1021/acsmedchemlett.5b00091. eCollection 2015 Jul 9.

14.

Discovery of potent heterodimeric antagonists of inhibitor of apoptosis proteins (IAPs) with sustained antitumor activity.

Perez HL, Chaudhry C, Emanuel SL, Fanslau C, Fargnoli J, Gan J, Kim KS, Lei M, Naglich JG, Traeger SC, Vuppugalla R, Wei DD, Vite GD, Talbott RL, Borzilleri RM.

J Med Chem. 2015 Feb 12;58(3):1556-62. doi: 10.1021/jm501482t. Epub 2015 Jan 23.

PMID:
25584393
15.

Discovery of tetrahydroisoquinoline-based bivalent heterodimeric IAP antagonists.

Kim KS, Zhang L, Williams D, Perez HL, Stang E, Borzilleri RM, Posy S, Lei M, Chaudhry C, Emanuel S, Talbott R.

Bioorg Med Chem Lett. 2014 Nov 1;24(21):5022-9. doi: 10.1016/j.bmcl.2014.09.022. Epub 2014 Sep 16.

PMID:
25278234
16.

Building and breaking interfaces: how a receptor takes shape.

Chaudhry C, Scimemi A, Kumar J.

J Neurosci. 2011 Jul 27;31(30):10749-51. doi: 10.1523/JNEUROSCI.2312-11.2011. No abstract available.

17.

Accounting for solvent signal offsets in the analysis of interferometric sedimentation velocity data.

Zhao H, Brown PH, Balbo A, Fernández-Alonso Mdel C, Polishchuck N, Chaudhry C, Mayer ML, Ghirlando R, Schuck P.

Macromol Biosci. 2010 Jul 7;10(7):736-45. doi: 10.1002/mabi.200900456.

PMID:
20480511
18.

Energetics of glutamate receptor ligand binding domain dimer assembly are modulated by allosteric ions.

Chaudhry C, Plested AJ, Schuck P, Mayer ML.

Proc Natl Acad Sci U S A. 2009 Jul 28;106(30):12329-34. doi: 10.1073/pnas.0904175106. Epub 2009 Jul 15.

19.

Comparative evaluation of corpus callosum DTI metrics in acute mild and moderate traumatic brain injury: its correlation with neuropsychometric tests.

Kumar R, Gupta RK, Husain M, Chaudhry C, Srivastava A, Saksena S, Rathore RK.

Brain Inj. 2009 Jul;23(7):675-85. doi: 10.1080/02699050903014915.

PMID:
19557571
20.

Stability of ligand-binding domain dimer assembly controls kainate receptor desensitization.

Chaudhry C, Weston MC, Schuck P, Rosenmund C, Mayer ML.

EMBO J. 2009 May 20;28(10):1518-30. doi: 10.1038/emboj.2009.86. Epub 2009 Apr 2.

21.

Substrate polypeptide presents a load on the apical domains of the chaperonin GroEL.

Motojima F, Chaudhry C, Fenton WA, Farr GW, Horwich AL.

Proc Natl Acad Sci U S A. 2004 Oct 19;101(42):15005-12. Epub 2004 Oct 12.

22.
23.

Role of the gamma-phosphate of ATP in triggering protein folding by GroEL-GroES: function, structure and energetics.

Chaudhry C, Farr GW, Todd MJ, Rye HS, Brunger AT, Adams PD, Horwich AL, Sigler PB.

EMBO J. 2003 Oct 1;22(19):4877-87.

24.

Influenza hemagglutinin is spring-loaded by a metastable native conformation.

Carr CM, Chaudhry C, Kim PS.

Proc Natl Acad Sci U S A. 1997 Dec 23;94(26):14306-13.

Supplemental Content

Loading ...
Support Center