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Items: 1 to 20 of 94

1.

Specificity and mechanism-of-action of the JAK2 tyrosine kinase inhibitors ruxolitinib and SAR302503 (TG101348).

Zhou T, Georgeon S, Moser R, Moore DJ, Caflisch A, Hantschel O.

Leukemia. 2014 Feb;28(2):404-7. doi: 10.1038/leu.2013.205. Epub 2013 Jul 4. No abstract available. Erratum in: Leukemia. 2014 Feb;28(2):471-2.

PMID:
23823659
2.

Targeting substrate-site in Jak2 kinase prevents emergence of genetic resistance.

Kesarwani M, Huber E, Kincaid Z, Evelyn CR, Biesiada J, Rance M, Thapa MB, Shah NP, Meller J, Zheng Y, Azam M.

Sci Rep. 2015 Sep 30;5:14538. doi: 10.1038/srep14538.

3.

Dual PI3K/AKT/mTOR inhibitor BEZ235 synergistically enhances the activity of JAK2 inhibitor against cultured and primary human myeloproliferative neoplasm cells.

Fiskus W, Verstovsek S, Manshouri T, Smith JE, Peth K, Abhyankar S, McGuirk J, Bhalla KN.

Mol Cancer Ther. 2013 May;12(5):577-88. doi: 10.1158/1535-7163.MCT-12-0862. Epub 2013 Feb 27.

4.

A randomized, placebo-controlled study of the pharmacokinetics, pharmacodynamics, and tolerability of the oral JAK2 inhibitor fedratinib (SAR302503) in healthy volunteers.

Zhang M, Xu CR, Shamiyeh E, Liu F, Yin JY, von Moltke LL, Smith WB.

J Clin Pharmacol. 2014 Apr;54(4):415-21. doi: 10.1002/jcph.218. Epub 2013 Nov 16.

PMID:
24165976
5.

Inhibition of JAK-STAT signaling by TG101348: a novel mechanism for inhibition of KITD816V-dependent growth in mast cell leukemia cells.

Lasho T, Tefferi A, Pardanani A.

Leukemia. 2010 Jul;24(7):1378-80. doi: 10.1038/leu.2010.109. Epub 2010 May 20. No abstract available.

PMID:
20485374
6.

Fragment-based discovery of JAK-2 inhibitors.

Antonysamy S, Hirst G, Park F, Sprengeler P, Stappenbeck F, Steensma R, Wilson M, Wong M.

Bioorg Med Chem Lett. 2009 Jan 1;19(1):279-82. doi: 10.1016/j.bmcl.2008.08.064. Epub 2008 Aug 22.

PMID:
19019674
7.

Decrease of Store-Operated Ca2+ Entry and Increase of Na+/Ca2+ Exchange by Pharmacological JAK2 Inhibition.

Yan J, Hosseinzadeh Z, Zhang B, Froeschl M, Schulze-Osthoff K, Stournaras C, Lang F.

Cell Physiol Biochem. 2016;38(2):683-95. doi: 10.1159/000443126. Epub 2016 Feb 8.

8.

New generation small-molecule inhibitors in myeloproliferative neoplasms.

Passamonti F, Maffioli M, Caramazza D.

Curr Opin Hematol. 2012 Mar;19(2):117-23. doi: 10.1097/MOH.0b013e32834ff575. Review.

PMID:
22227528
9.

Analogs of cinnamic acid benzyl amide as nonclassical inhibitors of activated JAK2 kinase.

Mielecki M, Milner-Krawczyk M, Grzelak K, Mielecki D, Krzysko KA, Lesyng B, Priebe W.

Curr Cancer Drug Targets. 2014;14(7):638-51.

PMID:
25146330
10.

JAK inhibitors: pharmacology and clinical activity in chronic myeloprolipherative neoplasms.

TreliƄski J, Robak T.

Curr Med Chem. 2013;20(9):1147-61.

PMID:
23317159
11.

TG101348, a JAK2-selective antagonist, inhibits primary hematopoietic cells derived from myeloproliferative disorder patients with JAK2V617F, MPLW515K or JAK2 exon 12 mutations as well as mutation negative patients.

Lasho TL, Tefferi A, Hood JD, Verstovsek S, Gilliland DG, Pardanani A.

Leukemia. 2008 Sep;22(9):1790-2. doi: 10.1038/leu.2008.56. Epub 2008 Mar 20. No abstract available.

PMID:
18354492
12.

Insights into the Structural Features Essential for JAK2 Inhibition and Selectivity.

Zhao C, Khadka DB, Cho WJ.

Curr Med Chem. 2016;23(13):1331-55. Review.

PMID:
27048338
13.

Pyrrolo[1,2-f]triazines as JAK2 inhibitors: achieving potency and selectivity for JAK2 over JAK3.

Harikrishnan LS, Kamau MG, Wan H, Inghrim JA, Zimmermann K, Sang X, Mastalerz HA, Johnson WL, Zhang G, Lombardo LJ, Poss MA, Trainor GL, Tokarski JS, Lorenzi MV, You D, Gottardis MM, Baldwin KF, Lippy J, Nirschl DS, Qiu R, Miller AV, Khan J, Sack JS, Purandare AV.

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1425-8. doi: 10.1016/j.bmcl.2011.01.022. Epub 2011 Jan 11.

PMID:
21282055
14.

Inhibition of Janus kinases by tyrosine phosphorylation inhibitor, Tyrphostin AG-490.

Rashid S, Bibi N, Parveen Z, Shafique S.

J Biomol Struct Dyn. 2015;33(11):2368-79. doi: 10.1080/07391102.2015.1050696. Epub 2015 Jun 23.

PMID:
26017266
15.

JAK2 inhibitors and their impact in myeloproliferative neoplasms.

Geyer HL, Tibes R, Mesa RA.

Hematology. 2012 Apr;17 Suppl 1:S129-32. doi: 10.1179/102453312X13336169156375.

PMID:
22507800
16.

Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2).

Liu Q, Batt DG, Lippy JS, Surti N, Tebben AJ, Muckelbauer JK, Chen L, An Y, Chang C, Pokross M, Yang Z, Wang H, Burke JR, Carter PH, Tino JA.

Bioorg Med Chem Lett. 2015 Oct 1;25(19):4265-9. doi: 10.1016/j.bmcl.2015.07.102. Epub 2015 Aug 6.

PMID:
26320619
17.

In silico identification of natural product inhibitors of JAK2.

Zhong HJ, Lin S, Tam IL, Lu L, Chan DS, Ma DL, Leung CH.

Methods. 2015 Jan;71:21-5. doi: 10.1016/j.ymeth.2014.07.003. Epub 2014 Jul 16.

PMID:
25038528
18.

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
19.

Dual inhibitors of Janus kinase 2 and 3 (JAK2/3): designing by pharmacophore- and docking-based virtual screening approach.

Jasuja H, Chadha N, Kaur M, Silakari O.

Mol Divers. 2014 May;18(2):253-67. doi: 10.1007/s11030-013-9497-z. Epub 2014 Jan 11.

PMID:
24415188
20.

Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors.

Labadie S, Barrett K, Blair WS, Chang C, Deshmukh G, Eigenbrot C, Gibbons P, Johnson A, Kenny JR, Kohli PB, Liimatta M, Lupardus PJ, Shia S, Steffek M, Ubhayakar S, van Abbema A, Zak M.

Bioorg Med Chem Lett. 2013 Nov 1;23(21):5923-30. doi: 10.1016/j.bmcl.2013.08.082. Epub 2013 Aug 27.

PMID:
24042009

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