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A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate.
Pacold ME, Brimacombe KR, Chan SH, Rohde JM, Lewis CA, Swier LJ, Possemato R, Chen WW, Sullivan LB, Fiske BP, Cho S, Freinkman E, Birsoy K, Abu-Remaileh M, Shaul YD, Liu CM, Zhou M, Koh MJ, Chung H, Davidson SM, Luengo A, Wang AQ, Xu X, Yasgar A, Liu L, Rai G, Westover KD, Vander Heiden MG, Shen M, Gray NS, Boxer MB, Sabatini DM. Pacold ME, et al. Among authors: boxer mb. Nat Chem Biol. 2016 Jun;12(6):452-8. doi: 10.1038/nchembio.2070. Epub 2016 Apr 25. Nat Chem Biol. 2016. PMID: 27110680 Free PMC article.
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: boxer mb. 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.
Synthesis and structure-activity evaluation of isatin-β-thiosemicarbazones with improved selective activity toward multidrug-resistant cells expressing P-glycoprotein.
Hall MD, Brimacombe KR, Varonka MS, Pluchino KM, Monda JK, Li J, Walsh MJ, Boxer MB, Warren TH, Fales HM, Gottesman MM. Hall MD, et al. Among authors: boxer mb. J Med Chem. 2011 Aug 25;54(16):5878-89. doi: 10.1021/jm2006047. Epub 2011 Aug 1. J Med Chem. 2011. PMID: 21721528 Free PMC article.
2-Oxo-N-aryl-1,2,3,4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.
Walsh MJ, Brimacombe KR, Veith H, Bougie JM, Daniel T, Leister W, Cantley LC, Israelsen WJ, Vander Heiden MG, Shen M, Auld DS, Thomas CJ, Boxer MB. Walsh MJ, et al. Among authors: boxer mb. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6322-7. doi: 10.1016/j.bmcl.2011.08.114. Epub 2011 Sep 14. Bioorg Med Chem Lett. 2011. PMID: 21958545 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: boxer mb. Nat Chem Biol. 2012 Oct;8(10):839-47. doi: 10.1038/nchembio.1060. Nat Chem Biol. 2012. PMID: 22922757 Free PMC article.
High-throughput combinatorial screening identifies drugs that cooperate with ibrutinib to kill activated B-cell-like diffuse large B-cell lymphoma cells.
Mathews Griner LA, Guha R, Shinn P, Young RM, Keller JM, Liu D, Goldlust IS, Yasgar A, McKnight C, Boxer MB, Duveau DY, Jiang JK, Michael S, Mierzwa T, Huang W, Walsh MJ, Mott BT, Patel P, Leister W, Maloney DJ, Leclair CA, Rai G, Jadhav A, Peyser BD, Austin CP, Martin SE, Simeonov A, Ferrer M, Staudt LM, Thomas CJ. Mathews Griner LA, et al. Among authors: boxer mb. Proc Natl Acad Sci U S A. 2014 Feb 11;111(6):2349-54. doi: 10.1073/pnas.1311846111. Epub 2014 Jan 27. Proc Natl Acad Sci U S A. 2014. PMID: 24469833 Free PMC article.
75 results