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Evaluation of thieno[3,2-b]pyrrole[3,2-d]pyridazinones as activators of the tumor cell specific M2 isoform of pyruvate kinase.
Jiang JK, Boxer MB, Vander Heiden MG, Shen M, Skoumbourdis AP, Southall N, Veith H, Leister W, Austin CP, Park HW, Inglese J, Cantley LC, Auld DS, Thomas CJ. Jiang JK, et al. Among authors: skoumbourdis ap. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3387-93. doi: 10.1016/j.bmcl.2010.04.015. Epub 2010 Apr 11. Bioorg Med Chem Lett. 2010. PMID: 20451379 Free PMC article.
Identification of a potent new chemotype for the selective inhibition of PDE4.
Skoumbourdis AP, Huang R, Southall N, Leister W, Guo V, Cho MH, Inglese J, Nirenberg M, Austin CP, Xia M, Thomas CJ. Skoumbourdis AP, et al. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1297-303. doi: 10.1016/j.bmcl.2008.01.028. Epub 2008 Jan 11. Bioorg Med Chem Lett. 2008. PMID: 18243697 Free PMC article.
Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis.
Anastasiou D, Yu Y, Israelsen WJ, Jiang JK, Boxer MB, Hong BS, Tempel W, Dimov S, Shen M, Jha A, Yang H, Mattaini KR, Metallo CM, Fiske BP, Courtney KD, Malstrom S, Khan TM, Kung C, Skoumbourdis AP, Veith H, Southall N, Walsh MJ, Brimacombe KR, Leister W, Lunt SY, Johnson ZR, Yen KE, Kunii K, Davidson SM, Christofk HR, Austin CP, Inglese J, Harris MH, Asara JM, Stephanopoulos G, Salituro FG, Jin S, Dang L, Auld DS, Park HW, Cantley LC, Thomas CJ, Vander Heiden MG. Anastasiou D, et al. Among authors: skoumbourdis ap. Nat Chem Biol. 2012 Oct;8(10):839-47. doi: 10.1038/nchembio.1060. Nat Chem Biol. 2012. PMID: 22922757 Free PMC article.
Elucidation of the structural basis of interaction of the BCR-ABL kinase inhibitor, nilotinib (Tasigna) with the human ABC drug transporter P-glycoprotein.
Shukla S, Chufan EE, Singh S, Skoumbourdis AP, Kapoor K, Boxer MB, Duveau DY, Thomas CJ, Talele TT, Ambudkar SV. Shukla S, et al. Among authors: skoumbourdis ap. Leukemia. 2014 Apr;28(4):961-4. doi: 10.1038/leu.2014.21. Epub 2014 Jan 14. Leukemia. 2014. PMID: 24418991 Free PMC article. No abstract available.
Phosphodiesterase 4 inhibitors enhance sexual pleasure-seeking activity in rodents.
Yuan P, Tragon T, Xia M, Leclair CA, Skoumbourdis AP, Zheng W, Thomas CJ, Huang R, Austin CP, Chen G, Guitart X. Yuan P, et al. Among authors: skoumbourdis ap. Pharmacol Biochem Behav. 2011 May;98(3):349-55. doi: 10.1016/j.pbb.2011.02.001. Epub 2011 Feb 4. Pharmacol Biochem Behav. 2011. PMID: 21296104 Free PMC article.
16 results