Format
Sort by
Items per page

Send to

Choose Destination

Search results

Items: 19

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. 2020 Feb;25(2):176-185. doi: 10.1177/2472555219884881. Epub 2019 Nov 9.

PMID:
31709883
2.

Determination of Real Time in Vivo Drug Receptor Occupancy for a Covalent Binding Drug as a Clinical Pharmacodynamic Biomarker by Immunocapture-LC-MS/MS.

Zheng N, Catlett IM, Taylor K, Gu H, Pattoli MA, Neely RJ, Li W, Allentoff A, Yuan X, Ciccimaro E, Yao M, Warrack BM, Burke JR, Zhang YJ, Pillutla R, Zeng J.

Anal Chem. 2019 Jul 2;91(13):8443-8452. doi: 10.1021/acs.analchem.9b01462. Epub 2019 Jun 19.

PMID:
31247719
3.

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
4.

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
5.

Bruton's tyrosine kinase inhibitor BMS-986142 in experimental models of rheumatoid arthritis enhances efficacy of agents representing clinical standard-of-care.

Gillooly KM, Pulicicchio C, Pattoli MA, Cheng L, Skala S, Heimrich EM, McIntyre KW, Taylor TL, Kukral DW, Dudhgaonkar S, Nagar J, Banas D, Watterson SH, Tino JA, Fura A, Burke JR.

PLoS One. 2017 Jul 24;12(7):e0181782. doi: 10.1371/journal.pone.0181782. eCollection 2017.

6.

Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers.

Watterson SH, De Lucca GV, Shi Q, Langevine CM, Liu Q, Batt DG, Beaudoin Bertrand M, Gong H, Dai J, Yip S, Li P, Sun D, Wu DR, Wang C, Zhang Y, Traeger SC, Pattoli MA, Skala S, Cheng L, Obermeier MT, Vickery R, Discenza LN, D'Arienzo CJ, Zhang Y, Heimrich E, Gillooly KM, Taylor TL, Pulicicchio C, McIntyre KW, Galella MA, Tebben AJ, Muckelbauer JK, Chang C, Rampulla R, Mathur A, Salter-Cid L, Barrish JC, Carter PH, Fura A, Burke JR, Tino JA.

J Med Chem. 2016 Oct 13;59(19):9173-9200. Epub 2016 Sep 19.

PMID:
27583770
7.

Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177).

De Lucca GV, Shi Q, Liu Q, Batt DG, Beaudoin Bertrand M, Rampulla R, Mathur A, Discenza L, D'Arienzo C, Dai J, Obermeier M, Vickery R, Zhang Y, Yang Z, Marathe P, Tebben AJ, Muckelbauer JK, Chang CJ, Zhang H, Gillooly K, Taylor T, Pattoli MA, Skala S, Kukral DW, McIntyre KW, Salter-Cid L, Fura A, Burke JR, Barrish JC, Carter PH, Tino JA.

J Med Chem. 2016 Sep 8;59(17):7915-35. doi: 10.1021/acs.jmedchem.6b00722. Epub 2016 Aug 26.

PMID:
27531604
8.

Novel tricyclic inhibitors of IKK2: discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066).

Watterson SH, Langevine CM, Van Kirk K, Kempson J, Guo J, Spergel SH, Das J, Moquin RV, Dyckman AJ, Nirschl D, Gregor K, Pattoli MA, Yang X, McIntyre KW, Yang G, Galella MA, Booth-Lute H, Chen L, Yang Z, Wang-Iverson D, McKinnon M, Dodd JH, Barrish JC, Burke JR, Pitts WJ.

Bioorg Med Chem Lett. 2011 Dec 1;21(23):7006-12. doi: 10.1016/j.bmcl.2011.09.111. Epub 2011 Oct 5.

PMID:
22018461
9.

Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis.

Dyckman AJ, Langevine CM, Quesnelle C, Kempson J, Guo J, Gill P, Spergel SH, Watterson SH, Li T, Nirschl DS, Gillooly KM, Pattoli MA, McIntyre KW, Chen L, McKinnon M, Dodd JH, Barrish JC, Burke JR, Pitts WJ.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):383-6. doi: 10.1016/j.bmcl.2010.10.133. Epub 2010 Oct 31.

PMID:
21087862
10.

Periodic, partial inhibition of IkappaB Kinase beta-mediated signaling yields therapeutic benefit in preclinical models of rheumatoid arthritis.

Gillooly KM, Pattoli MA, Taylor TL, Chen L, Cheng L, Gregor KR, Whitney GS, Susulic V, Watterson SH, Kempson J, Pitts WJ, Booth-Lute H, Yang G, Davies P, Kukral DW, Strnad J, McIntyre KW, Darienzo CJ, Salter-Cid L, Yang Z, Wang-Iverson DB, Burke JR.

J Pharmacol Exp Ther. 2009 Nov;331(2):349-60. doi: 10.1124/jpet.109.156018. Epub 2009 Aug 3.

PMID:
19652024
11.

Novel tricyclic inhibitors of IkappaB kinase.

Kempson J, Spergel SH, Guo J, Quesnelle C, Gill P, Belanger D, Dyckman AJ, Li T, Watterson SH, Langevine CM, Das J, Moquin RV, Furch JA, Marinier A, Dodier M, Martel A, Nirschl D, Van Kirk K, Burke JR, Pattoli MA, Gillooly K, McIntyre KW, Chen L, Yang Z, Marathe PH, Wang-Iverson D, Dodd JH, McKinnon M, Barrish JC, Pitts WJ.

J Med Chem. 2009 Apr 9;52(7):1994-2005. doi: 10.1021/jm8015816.

PMID:
19267461
12.

Synthesis and structure-activity relationship of imidazo(1,2-a)thieno(3,2-e)pyrazines as IKK-beta inhibitors.

Belema M, Bunker A, Nguyen VN, Beaulieu F, Ouellet C, Qiu Y, Zhang Y, Martel A, Burke JR, McIntyre KW, Pattoli MA, Daloisio C, Gillooly KM, Clarke WJ, Brassil PJ, Zusi FC, Vyas DM.

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4284-9. Epub 2007 May 16.

PMID:
17540562
13.

Synthesis and biological evaluation of 4-amino derivatives of benzimidazoquinoxaline, benzimidazoquinoline, and benzopyrazoloquinazoline as potent IKK inhibitors.

Beaulieu F, Ouellet C, Ruediger EH, Belema M, Qiu Y, Yang X, Banville J, Burke JR, Gregor KR, MacMaster JF, Martel A, McIntyre KW, Pattoli MA, Zusi FC, Vyas D.

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1233-7. Epub 2006 Dec 9.

PMID:
17197177
14.
15.

A highly selective inhibitor of I kappa B kinase, BMS-345541, blocks both joint inflammation and destruction in collagen-induced arthritis in mice.

McIntyre KW, Shuster DJ, Gillooly KM, Dambach DM, Pattoli MA, Lu P, Zhou XD, Qiu Y, Zusi FC, Burke JR.

Arthritis Rheum. 2003 Sep;48(9):2652-9.

16.

BMS-345541 is a highly selective inhibitor of I kappa B kinase that binds at an allosteric site of the enzyme and blocks NF-kappa B-dependent transcription in mice.

Burke JR, Pattoli MA, Gregor KR, Brassil PJ, MacMaster JF, McIntyre KW, Yang X, Iotzova VS, Clarke W, Strnad J, Qiu Y, Zusi FC.

J Biol Chem. 2003 Jan 17;278(3):1450-6. Epub 2002 Oct 25.

17.

Gangliosides of monocyte-derived macrophages of adults with advanced HIV infection show reduced surface accessibility.

Berenson CS, Gallery MA, Katari MS, Foster EW, Pattoli MA.

J Leukoc Biol. 1998 Sep;64(3):311-21.

PMID:
9738657
18.

Specific binding of Haemophilus influenzae to minor gangliosides of human respiratory epithelial cells.

Fakih MG, Murphy TF, Pattoli MA, Berenson CS.

Infect Immun. 1997 May;65(5):1695-700.

19.

A monoclonal antibody to human macrophage gangliosides inhibits macrophage migration.

Berenson CS, Patterson MA, Pattoli MA, Murphy TF.

J Leukoc Biol. 1996 Mar;59(3):371-9.

PMID:
8604015

Supplemental Content

Loading ...
Support Center