Program

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Journal Year Published

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Author

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73
56
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34

Category

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6
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1

Keyword

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Journal

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NCATS Publications

KDM5B Promotes Drug Resistance by Regulating Melanoma Propagating Cell Subpopulations.


Liu X, Zhang SM, McGeary MK, Krykbaeva I, Lai L, Jansen DJ, Kales S, Simeonov A, Hall M, Kelly DP, Bosenberg MW, Yan Q


Mol. Cancer Ther. , 2018.

Article Pubmed

KDM5 Histone Demethylase Activity Links Cellular Transcriptomic Heterogeneity to Therapeutic Resistance.


Hinohara K, Wu HJ, Vigneau S, McDonald TO, Igarashi KJ, Yamamoto KN, Madsen T, Fassl A, Egri SB, Papanastasiou M, Ding L, Peluffo G, Cohen O, Kales S, Lal-Nag M, Rai Bantukallu G, Maloney DJ, Jadhav A, Simeonov A, Wagle N, Brown M, Meissner A, Sicinski P, Jaffe JD, Jeselsohn R, Gimelbrant AA, Michor F, Polyak K


Cancer Cell , (34), 939-953.e9, 2018.

Article Pubmed

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Structure-Based Engineering of Irreversible Inhibitors against Histone Lysine Demethylase KDM5A.


Horton JR, Woodcock CB, Chen Q, Liu X, Zhang X, Shanks J, Rai Bantukallu G, Mott BT, Jansen DJ, Kales S, Henderson M, Cyr M, Pohida K, Hu X, Shah P, Xu X, Jadhav A, Maloney DJ, Hall M, Simeonov A, Fu H, Vertino PM, Cheng X


J. Med. Chem. , 2018.

Article Pubmed

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KDM5 histone demethylases repress immune response via suppression of STING.


Wu L, Cao J, Cai WL, Lang SM, Horton JR, Jansen DJ, Liu ZZ, Chen JF, Zhang M, Mott BT, Pohida K, Rai Bantukallu G, Kales S, Henderson M, Hu X, Jadhav A, Maloney DJ, Simeonov A, Zhu S, Iwasaki A, Hall M, Cheng X, Shadel GS, Yan Q


PLoS Biol. , (16), e2006134, 2018.

Article Pubmed

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The Assay Guidance Manual: Quantitative Biology and Pharmacology in Preclinical Drug Discovery.




Clin Transl Sci , 2018.

Article Pubmed

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Insights into the Action of Inhibitor Enantiomers against Histone Lysine Demethylase 5A.


Horton JR, Liu X, Wu L, Zhang K, Shanks J, Zhang X, Rai Bantukallu G, Mott BT, Jansen DJ, Kales S, Henderson M, Pohida K, Fang Y, Hu X, Jadhav A, Maloney DJ, Hall M, Simeonov A, Fu H, Vertino PM, Yan Q, Cheng X


J. Med. Chem. , 2018.

Article Pubmed

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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 JS, Kales S, Mott BT, Rai Bantukallu G, Jansen DJ, Henderson M, Urban D, Hall M, Simeonov A, Maloney DJ, Johns MA, Fu H, Jadhav A, Vertino PM, Yan Q, Cheng X


Cell Chem Biol , (23), 769-81, 2016.

Article Pubmed

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Balancing Protein Stability and Activity in Cancer: A New Approach for Identifying Driver Mutations Affecting CBL Ubiquitin Ligase Activation.


Li M, Kales S, Ma K, Shoemaker BA, Crespo-Barreto J, Cangelosi AL, Lipkowitz S, Panchenko AR


Cancer Res. , (76), 561-71, 2016.

Article Pubmed

Enigma prevents Cbl-c-mediated ubiquitination and degradation of RETMEN2A.


Kales S, Nau MM, Merchant AS, Lipkowitz S


PLoS ONE , (9), e87116, 2014.

Article Pubmed