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Journal

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NCATS Publications

Assessing inhibitors of mutant isocitrate dehydrogenase using a suite of pre-clinical discovery assays.


Urban DJ, Martinez N, Davis MI, Brimacombe K, Cheff D, Lee TD, Henderson M, Titus SA, Pragani R, Rohde JM, Liu L, Fang Y, Karavadhi S, Shah P, Lee OW, Wang A, McIver A, Zheng H, Wang X, Xu X, Jadhav A, Simeonov A, Shen M, Boxer MB, Hall M


Sci Rep , (7), 12758, 2017.

Article Pubmed

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Small Molecule Inhibition of the Ubiquitin-specific Protease USP2 Accelerates Cyclin D1 Degradation and Leads to Cell Cycle Arrest in Colorectal Cancer and Mantle Cell Lymphoma Models.


Davis MI, Pragani R, Fox JT, Shen M, Parmar K, Gaudiano EF, Liu L, Tanega C, McGee L, Hall M, McKnight C, Shinn P, Nelson H, Chattopadhyay D, D'Andrea AD, Auld DS, DeLucas LJ, Li Z, Boxer MB, Simeonov A


J. Biol. Chem. , 2016.

Article Pubmed

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Small molecule inhibitor of NRF2 selectively intervenes therapeutic resistance in KEAP1-deficient NSCLC tumors.


Singh A, Venkannagari S, Oh KH, Zhang Y, Liu L, Rohde JM, Nimmagadda S, Sudini K, Brimacombe K, Gajghate S, Ma J, Wang A, Xu X, Shahane SA, Xia M, Woo J, A Mensah G, Wang Z, Ferrer-Alegre M, Gabrielson E, Li Z, Rastinejad F, Shen M, Boxer MB, Biswal S


ACS Chem. Biol. , 2016.

Article Pubmed

A Class of Diacylglycerol Acyltransferase 1 Inhibitors Identified by a Combination of Phenotypic High-throughput Screening, Genomics, and Genetics.


Tschapalda K, Zhang Y, Liu L, Golovnina K, Schlemper T, Eichmann TO, Lal-Nag M, Sreenivasan U, McLenithan J, Ziegler S, Sztalryd C, Lass A, Auld D, Oliver B, Waldmann H, Li Z, Shen M, Boxer MB, Beller M


EBioMedicine , (8), 49-59, 2016.

Article Pubmed

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A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate.


Pacold ME, et al.


Nat. Chem. Biol. , (12), 452-8, 2016.

Article Pubmed

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Structure activity relationships of human galactokinase inhibitors.


Liu L, Tang M, Walsh MJ, Brimacombe K, Pragani R, Tanega C, Rohde JM, Baker H, Fernandez E, Blackman B, Bougie JM, Leister WH, Auld DS, Shen M, Lai K, Boxer MB


Bioorg. Med. Chem. Lett. , (25), 721-7, 2015.

Article Pubmed

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Identification of ML251, a Potent Inhibitor of T. brucei and T. cruzi Phosphofructokinase.


Brimacombe K, Walsh MJ, Liu L, Vásquez-Valdivieso MG, Morgan HP, McNae I, Fothergill-Gilmore LA, Michels PA, Auld DS, Simeonov A, Walkinshaw MD, Shen M, Boxer MB


ACS Med Chem Lett , (5), 12-7, 2014.

Article Pubmed

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Genomic and functional characterizations of phosphodiesterase subtype 4D in human cancers.


Lin DC, Xu L, Ding LW, Sharma A, Liu L, Yang H, Tan P, Vadgama J, Karlan BY, Lester J, Urban N, Schummer M, Doan N, Said JW, Sun H, Walsh M, Thomas C, Patel P, Yin D, Chan D, Koeffler HP


Proc. Natl. Acad. Sci. U.S.A. , (110), 6109-14, 2013.

Article Pubmed

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