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Page 1
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: rai g. 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.
4-(3-Chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-methoxypyridin-2-yl)piperazine-1-carbothioamide (ML267), a potent inhibitor of bacterial phosphopantetheinyl transferase that attenuates secondary metabolism and thwarts bacterial growth.
Foley TL, Rai G, Yasgar A, Daniel T, Baker HL, Attene-Ramos M, Kosa NM, Leister W, Burkart MD, Jadhav A, Simeonov A, Maloney DJ. Foley TL, et al. Among authors: rai g. J Med Chem. 2014 Feb 13;57(3):1063-78. doi: 10.1021/jm401752p. Epub 2014 Jan 22. J Med Chem. 2014. PMID: 24450337 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: rai g. 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.
KDM4/JMJD2 Histone Demethylase Inhibitors Block Prostate Tumor Growth by Suppressing the Expression of AR and BMYB-Regulated Genes.
Duan L, Rai G, Roggero C, Zhang QJ, Wei Q, Ma SH, Zhou Y, Santoyo J, Martinez ED, Xiao G, Raj GV, Jadhav A, Simeonov A, Maloney DJ, Rizo J, Hsieh JT, Liu ZP. Duan L, et al. Among authors: rai g. Chem Biol. 2015 Sep 17;22(9):1185-96. doi: 10.1016/j.chembiol.2015.08.007. Epub 2015 Sep 10. Chem Biol. 2015. PMID: 26364928 Free PMC article.
Structural Basis for KDM5A Histone Lysine Demethylase Inhibition by Diverse Compounds.
Horton JR, Liu X, Gale M, Wu L, Shanks JR, Zhang X, Webber PJ, Bell JSK, Kales SC, Mott BT, Rai G, Jansen DJ, Henderson MJ, Urban DJ, Hall MD, Simeonov A, Maloney DJ, Johns MA, Fu H, Jadhav A, Vertino PM, Yan Q, Cheng X. Horton JR, et al. Among authors: rai g. Cell Chem Biol. 2016 Jul 21;23(7):769-781. doi: 10.1016/j.chembiol.2016.06.006. Epub 2016 Jul 14. Cell Chem Biol. 2016. PMID: 27427228 Free PMC article.
Corrigendum: 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 MR, 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, Heiden MG, Shen M, Gray NS, Boxer MB, Sabatini DM. Pacold ME, et al. Among authors: rai g. Nat Chem Biol. 2016 Jul 19;12(8):656. doi: 10.1038/nchembio0816-656. Nat Chem Biol. 2016. PMID: 27434767 No abstract available.
A High-Throughput Screen Identifies 2,9-Diazaspiro[5.5]Undecanes as Inducers of the Endoplasmic Reticulum Stress Response with Cytotoxic Activity in 3D Glioma Cell Models.
Martinez NJ, Rai G, Yasgar A, Lea WA, Sun H, Wang Y, Luci DK, Yang SM, Nishihara K, Takeda S, Sagor M, Earnshaw I, Okada T, Mori K, Wilson K, Riggins GJ, Xia M, Grimaldi M, Jadhav A, Maloney DJ, Simeonov A. Martinez NJ, et al. Among authors: rai g. PLoS One. 2016 Aug 29;11(8):e0161486. doi: 10.1371/journal.pone.0161486. eCollection 2016. PLoS One. 2016. PMID: 27570969 Free PMC article.
Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH).
Rai G, Brimacombe KR, Mott BT, Urban DJ, Hu X, Yang SM, Lee TD, Cheff DM, Kouznetsova J, Benavides GA, Pohida K, Kuenstner EJ, Luci DK, Lukacs CM, Davies DR, Dranow DM, Zhu H, Sulikowski G, Moore WJ, Stott GM, Flint AJ, Hall MD, Darley-Usmar VM, Neckers LM, Dang CV, Waterson AG, Simeonov A, Jadhav A, Maloney DJ. Rai G, et al. J Med Chem. 2017 Nov 22;60(22):9184-9204. doi: 10.1021/acs.jmedchem.7b00941. Epub 2017 Nov 9. J Med Chem. 2017. PMID: 29120638 Free PMC article.
507 results