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Items: 28


Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors.

Grimster NP, Anderson E, Alimzhanov M, Bebernitz G, Bell K, Chuaqui C, Deegan T, Ferguson AD, Gero T, Harsch A, Huszar D, Kawatkar A, Kettle JG, Lyne P, Read JA, Rivard Costa C, Ruston L, Schroeder P, Shi J, Su Q, Throner S, Toader D, Vasbinder M, Woessner R, Wang H, Wu A, Ye M, Zheng W, Zinda M.

J Med Chem. 2018 Jun 28;61(12):5235-5244. doi: 10.1021/acs.jmedchem.8b00076. Epub 2018 Jun 13.


Inhibition of ALK1 signaling with dalantercept combined with VEGFR TKI leads to tumor stasis in renal cell carcinoma.

Wang X, Solban N, Khanna P, Callea M, Song J, Alsop DC, Pearsall RS, Atkins MB, Mier JW, Signoretti S, Alimzhanov M, Kumar R, Bhasin MK, Bhatt RS.

Oncotarget. 2016 Jul 5;7(27):41857-41869. doi: 10.18632/oncotarget.9621.


Potent and Selective CK2 Kinase Inhibitors with Effects on Wnt Pathway Signaling in Vivo.

Dowling JE, Alimzhanov M, Bao L, Chuaqui C, Denz CR, Jenkins E, Larsen NA, Lyne PD, Pontz T, Ye Q, Holdgate GA, Snow L, O'Connell N, Ferguson AD.

ACS Med Chem Lett. 2016 Jan 20;7(3):300-5. doi: 10.1021/acsmedchemlett.5b00452. eCollection 2016 Mar 10.


Identification of azabenzimidazoles as potent JAK1 selective inhibitors.

Vasbinder MM, Alimzhanov M, Augustin M, Bebernitz G, Bell K, Chuaqui C, Deegan T, Ferguson AD, Goodwin K, Huszar D, Kawatkar A, Kawatkar S, Read J, Shi J, Steinbacher S, Steuber H, Su Q, Toader D, Wang H, Woessner R, Wu A, Ye M, Zinda M.

Bioorg Med Chem Lett. 2016 Jan 1;26(1):60-7. doi: 10.1016/j.bmcl.2015.11.031. Epub 2015 Nov 12.


Identification and Characterization of MEDI4736, an Antagonistic Anti-PD-L1 Monoclonal Antibody.

Stewart R, Morrow M, Hammond SA, Mulgrew K, Marcus D, Poon E, Watkins A, Mullins S, Chodorge M, Andrews J, Bannister D, Dick E, Crawford N, Parmentier J, Alimzhanov M, Babcook JS, Foltz IN, Buchanan A, Bedian V, Wilkinson RW, McCourt M.

Cancer Immunol Res. 2015 Sep;3(9):1052-62. doi: 10.1158/2326-6066.CIR-14-0191. Epub 2015 May 5.


Structure and Property Based Design of Pyrazolo[1,5-a]pyrimidine Inhibitors of CK2 Kinase with Activity in Vivo.

Dowling JE, Alimzhanov M, Bao L, Block MH, Chuaqui C, Cooke EL, Denz CR, Hird A, Huang S, Larsen NA, Peng B, Pontz TW, Rivard-Costa C, Saeh JC, Thakur K, Ye Q, Zhang T, Lyne PD.

ACS Med Chem Lett. 2013 Jul 3;4(8):800-5. doi: 10.1021/ml400197u. eCollection 2013 Aug 8.


Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors.

Su Q, Ioannidis S, Chuaqui C, Almeida L, Alimzhanov M, Bebernitz G, Bell K, Block M, Howard T, Huang S, Huszar D, Read JA, Rivard Costa C, Shi J, Su M, Ye M, Zinda M.

J Med Chem. 2014 Jan 9;57(1):144-58. doi: 10.1021/jm401546n. Epub 2013 Dec 20.


Complement C4 maintains peripheral B-cell tolerance in a myeloid cell dependent manner.

Chatterjee P, Agyemang AF, Alimzhanov MB, Degn S, Tsiftsoglou SA, Alicot E, Jones SA, Ma M, Carroll MC.

Eur J Immunol. 2013 Sep;43(9):2441-2450. doi: 10.1002/eji.201343412. Epub 2013 Jul 3.


Discovery of novel Jak2-Stat pathway inhibitors with extended residence time on target.

Guan H, Lamb ML, Peng B, Huang S, Degrace N, Read J, Hussain S, Wu J, Rivard C, Alimzhanov M, Bebernitz G, Bell K, Ye M, Zinda M, Ioannidis S.

Bioorg Med Chem Lett. 2013 May 15;23(10):3105-10. doi: 10.1016/j.bmcl.2013.02.111. Epub 2013 Mar 7.


In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors.

Wang T, Ioannidis S, Almeida L, Block MH, Davies AM, Lamb ML, Scott DA, Su M, Zhang HJ, Alimzhanov M, Bebernitz G, Bell K, Zinda M.

Bioorg Med Chem Lett. 2011 May 15;21(10):2958-61. doi: 10.1016/j.bmcl.2011.03.053. Epub 2011 Mar 21.


Discovery of 5-chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the Jak/Stat pathway.

Ioannidis S, Lamb ML, Wang T, Almeida L, Block MH, Davies AM, Peng B, Su M, Zhang HJ, Hoffmann E, Rivard C, Green I, Howard T, Pollard H, Read J, Alimzhanov M, Bebernitz G, Bell K, Ye M, Huszar D, Zinda M.

J Med Chem. 2011 Jan 13;54(1):262-76. doi: 10.1021/jm1011319. Epub 2010 Dec 7.


Replacement of pyrazol-3-yl amine hinge binder with thiazol-2-yl amine: Discovery of potent and selective JAK2 inhibitors.

Ioannidis S, Lamb ML, Almeida L, Guan H, Peng B, Bebernitz G, Bell K, Alimzhanov M, Zinda M.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1669-73. doi: 10.1016/j.bmcl.2010.01.091. Epub 2010 Jan 25.


The JAK2 inhibitor AZD1480 potently blocks Stat3 signaling and oncogenesis in solid tumors.

Hedvat M, Huszar D, Herrmann A, Gozgit JM, Schroeder A, Sheehy A, Buettner R, Proia D, Kowolik CM, Xin H, Armstrong B, Bebernitz G, Weng S, Wang L, Ye M, McEachern K, Chen H, Morosini D, Bell K, Alimzhanov M, Ioannidis S, McCoon P, Cao ZA, Yu H, Jove R, Zinda M.

Cancer Cell. 2009 Dec 8;16(6):487-97. doi: 10.1016/j.ccr.2009.10.015.


Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors.

Ioannidis S, Lamb ML, Davies AM, Almeida L, Su M, Bebernitz G, Ye M, Bell K, Alimzhanov M, Zinda M.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6524-8. doi: 10.1016/j.bmcl.2009.10.054. Epub 2009 Oct 24.


Oncogenic transformation in the absence of Xrcc4 targets peripheral B cells that have undergone editing and switching.

Wang JH, Alt FW, Gostissa M, Datta A, Murphy M, Alimzhanov MB, Coakley KM, Rajewsky K, Manis JP, Yan CT.

J Exp Med. 2008 Dec 22;205(13):3079-90. doi: 10.1084/jem.20082271. Epub 2008 Dec 8.


B cell-specific deletion of protein-tyrosine phosphatase Shp1 promotes B-1a cell development and causes systemic autoimmunity.

Pao LI, Lam KP, Henderson JM, Kutok JL, Alimzhanov M, Nitschke L, Thomas ML, Neel BG, Rajewsky K.

Immunity. 2007 Jul;27(1):35-48. Epub 2007 Jun 28.


FDC-specific functions of p55TNFR and IKK2 in the development of FDC networks and of antibody responses.

Victoratos P, Lagnel J, Tzima S, Alimzhanov MB, Rajewsky K, Pasparakis M, Kollias G.

Immunity. 2006 Jan;24(1):65-77.


Survival of resting mature B lymphocytes depends on BCR signaling via the Igalpha/beta heterodimer.

Kraus M, Alimzhanov MB, Rajewsky N, Rajewsky K.

Cell. 2004 Jun 11;117(6):787-800.


B cell receptor signal strength determines B cell fate.

Casola S, Otipoby KL, Alimzhanov M, Humme S, Uyttersprot N, Kutok JL, Carroll MC, Rajewsky K.

Nat Immunol. 2004 Mar;5(3):317-27. Epub 2004 Feb 1.


Redundancy in tumor necrosis factor (TNF) and lymphotoxin (LT) signaling in vivo: mice with inactivation of the entire TNF/LT locus versus single-knockout mice.

Kuprash DV, Alimzhanov MB, Tumanov AV, Grivennikov SI, Shakhov AN, Drutskaya LN, Marino MW, Turetskaya RL, Anderson AO, Rajewsky K, Pfeffer K, Nedospasov SA.

Mol Cell Biol. 2002 Dec;22(24):8626-34.


[Comparative characteristics of transcription of genes for alpha and beta-lymphotoxin subunits in B- and T-lymphocyte lines, in peripheral lymphocytes, and in normal human tissue].

Boĭchenko VE, Alimzhanov MB, Turetskaia RL, Rulman A, Nordhaim A, Kuprash DV, Nedospasov SA.

Mol Biol (Mosk). 2001 Jan-Feb;35(1):128-35. Russian.


TNF and lymphotoxin beta cooperate in the maintenance of secondary lymphoid tissue microarchitecture but not in the development of lymph nodes.

Kuprash DV, Alimzhanov MB, Tumanov AV, Anderson AO, Pfeffer K, Nedospasov SA.

J Immunol. 1999 Dec 15;163(12):6575-80.


Mature follicular dendritic cell networks depend on expression of lymphotoxin beta receptor by radioresistant stromal cells and of lymphotoxin beta and tumor necrosis factor by B cells.

Endres R, Alimzhanov MB, Plitz T, Fütterer A, Kosco-Vilbois MH, Nedospasov SA, Rajewsky K, Pfeffer K.

J Exp Med. 1999 Jan 4;189(1):159-68.


Abnormal development of secondary lymphoid tissues in lymphotoxin beta-deficient mice.

Alimzhanov MB, Kuprash DV, Kosco-Vilbois MH, Luz A, Turetskaya RL, Tarakhovsky A, Rajewsky K, Nedospasov SA, Pfeffer K.

Proc Natl Acad Sci U S A. 1997 Aug 19;94(17):9302-7.


Functional analysis of the lymphotoxin-beta promoter. Sequence requirements for PMA activation.

Kuprash DV, Osipovich OA, Pokholok DK, Alimzhanov MB, Biragyn A, Turetskaya RL, Nedospasov SA.

J Immunol. 1996 Apr 1;156(7):2465-72.


Cloning and expression analysis of the murine lymphotoxin beta gene.

Pokholok DK, Maroulakou IG, Kuprash DV, Alimzhanov MB, Kozlov SV, Novobrantseva TI, Turetskaya RL, Green JE, Nedospasov SA.

Proc Natl Acad Sci U S A. 1995 Jan 31;92(3):674-8.


[Characteristics of murine chromosome 17 containing three tumor necrosis factor family genes, including the gene of the transmembrane subunit of lymphotoxin].

Kuprash DV, Alimzhanov MB, Pokholok DK, Kozlov SV, Novobrantseva TI, Turetskaia RL, Nedospasov SA.

Dokl Akad Nauk. 1994 Aug;337(5):683-6. Russian. No abstract available.


[Cloning and characteristics of murine genes coding for the human GADD45 analog--a protein induced in response to DNA damage].

Alimzhanov MB, Kuprash DV, Turetskaia RL, Osipovich OA, Borodulina OR, Osovskaia VS, Chumakov PM, Nedospasov SA.

Dokl Akad Nauk. 1993 Dec;333(6):788-91. Russian. No abstract available.


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