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Items: 1 to 20 of 78

1.

Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.

Wan H, Schroeder GM, Hart AC, Inghrim J, Grebinski J, Tokarski JS, Lorenzi MV, You D, Mcdevitt T, Penhallow B, Vuppugalla R, Zhang Y, Gu X, Iyer R, Lombardo LJ, Trainor GL, Ruepp S, Lippy J, Blat Y, Sack JS, Khan JA, Stefanski K, Sleczka B, Mathur A, Sun JH, Wong MK, Wu DR, Li P, Gupta A, Arunachalam PN, Pragalathan B, Narayanan S, K C N, Kuppusamy P, Purandare AV.

ACS Med Chem Lett. 2015 Jul 12;6(8):850-5. doi: 10.1021/acsmedchemlett.5b00226. eCollection 2015 Aug 13.

2.

Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2.

Purandare AV, McDevitt TM, Wan H, You D, Penhallow B, Han X, Vuppugalla R, Zhang Y, Ruepp SU, Trainor GL, Lombardo L, Pedicord D, Gottardis MM, Ross-Macdonald P, de Silva H, Hosbach J, Emanuel SL, Blat Y, Fitzpatrick E, Taylor TL, McIntyre KW, Michaud E, Mulligan C, Lee FY, Woolfson A, Lasho TL, Pardanani A, Tefferi A, Lorenzi MV.

Leukemia. 2012 Feb;26(2):280-8. doi: 10.1038/leu.2011.292. Epub 2011 Oct 21.

PMID:
22015772
3.

Discovery of 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitors of Janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders.

Lim J, Taoka B, Otte RD, Spencer K, Dinsmore CJ, Altman MD, Chan G, Rosenstein C, Sharma S, Su HP, Szewczak AA, Xu L, Yin H, Zugay-Murphy J, Marshall CG, Young JR.

J Med Chem. 2011 Oct 27;54(20):7334-49. doi: 10.1021/jm200909u. Epub 2011 Sep 26.

PMID:
21942426
4.

Therapy with JAK2 inhibitors for myeloproliferative neoplasms.

Santos FP, Verstovsek S.

Hematol Oncol Clin North Am. 2012 Oct;26(5):1083-99. doi: 10.1016/j.hoc.2012.07.008. Epub 2012 Aug 21. Review.

5.

Pyrrole-3-carboxamides as potent and selective JAK2 inhibitors.

Brasca MG, Nesi M, Avanzi N, Ballinari D, Bandiera T, Bertrand J, Bindi S, Canevari G, Carenzi D, Casero D, Ceriani L, Ciomei M, Cirla A, Colombo M, Cribioli S, Cristiani C, Della Vedova F, Fachin G, Fasolini M, Felder ER, Galvani A, Isacchi A, Mirizzi D, Motto I, Panzeri A, Pesenti E, Vianello P, Gnocchi P, Donati D.

Bioorg Med Chem. 2014 Sep 1;22(17):4998-5012. doi: 10.1016/j.bmc.2014.06.025. Epub 2014 Jun 21.

PMID:
25009002
6.

Histone deacetylases inhibitor sodium butyrate inhibits JAK2/STAT signaling through upregulation of SOCS1 and SOCS3 mediated by HDAC8 inhibition in myeloproliferative neoplasms.

Gao SM, Chen CQ, Wang LY, Hong LL, Wu JB, Dong PH, Yu FJ.

Exp Hematol. 2013 Mar;41(3):261-70.e4. doi: 10.1016/j.exphem.2012.10.012. Epub 2012 Oct 27.

PMID:
23111066
7.

Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.

Hanan EJ, van Abbema A, Barrett K, Blair WS, Blaney J, Chang C, Eigenbrot C, Flynn S, Gibbons P, Hurley CA, Kenny JR, Kulagowski J, Lee L, Magnuson SR, Morris C, Murray J, Pastor RM, Rawson T, Siu M, Ultsch M, Zhou A, Sampath D, Lyssikatos JP.

J Med Chem. 2012 Nov 26;55(22):10090-107. doi: 10.1021/jm3012239. Epub 2012 Oct 24.

PMID:
23061660
8.

9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors.

Zimmermann K, Sang X, Mastalerz HA, Johnson WL, Zhang G, Liu Q, Batt D, Lombardo LJ, Vyas D, Trainor GL, Tokarski JS, Lorenzi MV, You D, Gottardis MM, Lippy J, Khan J, Sack JS, Purandare AV.

Bioorg Med Chem Lett. 2015 Jul 15;25(14):2809-12. doi: 10.1016/j.bmcl.2015.04.101. Epub 2015 May 11.

PMID:
25987372
9.

Epigenetic deregulated miR-375 contributes to the constitutive activation of JAK2/STAT signaling in myeloproliferative neoplasm.

Yin LH, Zheng XQ, Li HY, Bi LX, Shi YF, Ye AF, Wu JB, Gao SM.

Leuk Res. 2015 Apr;39(4):471-8. doi: 10.1016/j.leukres.2015.01.009. Epub 2015 Jan 28.

PMID:
25666256
10.

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 Jul 18. doi: 10.1021/acs.jmedchem.9b00444. [Epub ahead of print]

PMID:
31318208
11.

New JAK2 inhibitors for myeloproliferative neoplasms.

Quintás-Cardama A, Verstovsek S.

Expert Opin Investig Drugs. 2011 Jul;20(7):961-72. doi: 10.1517/13543784.2011.579560. Epub 2011 Apr 27. Review.

PMID:
21521147
12.

JAK2 inhibitors in the treatment of myeloproliferative neoplasms.

Tibes R, Bogenberger JM, Geyer HL, Mesa RA.

Expert Opin Investig Drugs. 2012 Dec;21(12):1755-74. doi: 10.1517/13543784.2012.721352. Epub 2012 Sep 19. Review.

PMID:
22991927
13.

Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.

Zak M, Mendonca R, Balazs M, Barrett K, Bergeron P, Blair WS, Chang C, Deshmukh G, Devoss J, Dragovich PS, Eigenbrot C, Ghilardi N, Gibbons P, Gradl S, Hamman C, Hanan EJ, Harstad E, Hewitt PR, Hurley CA, Jin T, Johnson A, Johnson T, Kenny JR, Koehler MF, Bir Kohli P, Kulagowski JJ, Labadie S, Liao J, Liimatta M, Lin Z, Lupardus PJ, Maxey RJ, Murray JM, Pulk R, Rodriguez M, Savage S, Shia S, Steffek M, Ubhayakar S, Ultsch M, van Abbema A, Ward SI, Xiao L, Xiao Y.

J Med Chem. 2012 Jul 12;55(13):6176-93. doi: 10.1021/jm300628c. Epub 2012 Jun 28.

PMID:
22698084
14.

Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805.

Baffert F, Régnier CH, De Pover A, Pissot-Soldermann C, Tavares GA, Blasco F, Brueggen J, Chène P, Drueckes P, Erdmann D, Furet P, Gerspacher M, Lang M, Ledieu D, Nolan L, Ruetz S, Trappe J, Vangrevelinghe E, Wartmann M, Wyder L, Hofmann F, Radimerski T.

Mol Cancer Ther. 2010 Jul;9(7):1945-55. doi: 10.1158/1535-7163.MCT-10-0053. Epub 2010 Jun 29.

15.

Targeting JAK2 in the therapy of myeloproliferative neoplasms.

Reddy MM, Deshpande A, Sattler M.

Expert Opin Ther Targets. 2012 Mar;16(3):313-24. doi: 10.1517/14728222.2012.662956. Epub 2012 Feb 17. Review.

16.

Discovery of potent and highly selective thienopyridine Janus kinase 2 inhibitors.

Schenkel LB, Huang X, Cheng A, Deak HL, Doherty E, Emkey R, Gu Y, Gunaydin H, Kim JL, Lee J, Loberg R, Olivieri P, Pistillo J, Tang J, Wan Q, Wang HL, Wang SW, Wells MC, Wu B, Yu V, Liu L, Geuns-Meyer S.

J Med Chem. 2011 Dec 22;54(24):8440-50. doi: 10.1021/jm200911r. Epub 2011 Nov 16.

PMID:
22087750
17.

Update on JAK2 Inhibitors in Myeloproliferative Neoplasm.

Chan D, Koren-Michowitz M.

Ther Adv Hematol. 2011 Apr;2(2):61-71. doi: 10.1177/2040620711401646.

18.

Myeloproliferative neoplasms: JAK2 signaling pathway as a central target for therapy.

Pasquier F, Cabagnols X, Secardin L, Plo I, Vainchenker W.

Clin Lymphoma Myeloma Leuk. 2014 Sep;14 Suppl:S23-35. doi: 10.1016/j.clml.2014.06.014. Review.

PMID:
25486952
19.

Myeloproliferative neoplasms: from JAK2 mutations discovery to JAK2 inhibitor therapies.

Passamonti F, Maffioli M, Caramazza D, Cazzola M.

Oncotarget. 2011 Jun;2(6):485-90.

20.

Prospect of JAK2 inhibitor therapy in myeloproliferative neoplasms.

Atallah E, Verstovsek S.

Expert Rev Anticancer Ther. 2009 May;9(5):663-70. doi: 10.1586/era.09.14. Review.

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