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Items: 29


Combination Treatment of the Oral CHK1 Inhibitor, SRA737, and Low-Dose Gemcitabine Enhances the Effect of Programmed Death Ligand 1 Blockade by Modulating the Immune Microenvironment in SCLC.

Sen T, Della Corte CM, Milutinovic S, Cardnell RJ, Diao L, Ramkumar K, Gay CM, Stewart CA, Fan Y, Shen L, Hansen RJ, Strouse B, Hedrick MP, Hassig CA, Heymach JV, Wang J, Byers LA.

J Thorac Oncol. 2019 Dec;14(12):2152-2163. doi: 10.1016/j.jtho.2019.08.009. Epub 2019 Aug 27.


Cardiac Glycosides Activate the Tumor Suppressor and Viral Restriction Factor Promyelocytic Leukemia Protein (PML).

Milutinovic S, Heynen-Genel S, Chao E, Dewing A, Solano R, Milan L, Barron N, He M, Diaz PW, Matsuzawa S, Reed JC, Hassig CA.

PLoS One. 2016 Mar 31;11(3):e0152692. doi: 10.1371/journal.pone.0152692. eCollection 2016.


SBI-0640756 Attenuates the Growth of Clinically Unresponsive Melanomas by Disrupting the eIF4F Translation Initiation Complex.

Feng Y, Pinkerton AB, Hulea L, Zhang T, Davies MA, Grotegut S, Cheli Y, Yin H, Lau E, Kim H, De SK, Barile E, Pellecchia M, Bosenberg M, Li JL, James B, Hassig CA, Brown KM, Topisirovic I, Ronai ZA.

Cancer Res. 2015 Dec 15;75(24):5211-8. doi: 10.1158/0008-5472.CAN-15-0885. Epub 2015 Nov 24.


Cell-Based High-Throughput Luciferase Reporter Gene Assays for Identifying and Profiling Chemical Modulators of Endoplasmic Reticulum Signaling Protein, IRE1.

Rong J, Pass I, Diaz PW, Ngo TA, Sauer M, Magnuson G, Zeng FY, Hassig CA, Jackson MR, Cosford ND, Matsuzawa S, Reed JC.

J Biomol Screen. 2015 Dec;20(10):1232-45. doi: 10.1177/1087057115600414. Epub 2015 Aug 11.


Ultra-High-Throughput Screening of Natural Product Extracts to Identify Proapoptotic Inhibitors of Bcl-2 Family Proteins.

Hassig CA, Zeng FY, Kung P, Kiankarimi M, Kim S, Diaz PW, Zhai D, Welsh K, Morshedian S, Su Y, O'Keefe B, Newman DJ, Rusman Y, Kaur H, Salomon CE, Brown SG, Baire B, Michel AR, Hoye TR, Francis S, Georg GI, Walters MA, Divlianska DB, Roth GP, Wright AE, Reed JC.

J Biomol Screen. 2014 Sep;19(8):1201-11. doi: 10.1177/1087057114536227. Epub 2014 May 27.


Evidence that the DNA endonuclease ARTEMIS also has intrinsic 5'-exonuclease activity.

Li S, Chang HH, Niewolik D, Hedrick MP, Pinkerton AB, Hassig CA, Schwarz K, Lieber MR.

J Biol Chem. 2014 Mar 14;289(11):7825-34. doi: 10.1074/jbc.M113.544874. Epub 2014 Feb 5.


Inhibition of melanoma growth by small molecules that promote the mitochondrial localization of ATF2.

Varsano T, Lau E, Feng Y, Garrido M, Milan L, Heynen-Genel S, Hassig CA, Ronai ZA.

Clin Cancer Res. 2013 May 15;19(10):2710-22. doi: 10.1158/1078-0432.CCR-12-2689. Epub 2013 Apr 15.


Heteroaromatic-aminomethyl quinolones: potent and selective iNOS inhibitors.

DurĂ³n SG, Lindstrom A, Bonnefous C, Zhang H, Chen X, Symons KT, Sablad M, Rozenkrants N, Zhang Y, Wang L, Yazdani N, Shiau AK, Noble SA, Rix P, Rao TS, Hassig CA, Smith ND.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1237-41. doi: 10.1016/j.bmcl.2011.11.073. Epub 2011 Nov 25.


Identification and SAR of selective inducible nitric oxide synthase (iNOS) dimerization inhibitors.

Gahman TC, Herbert MR, Lang H, Thayer A, Symons KT, Nguyen PM, Massari ME, Dozier S, Zhang Y, Sablad M, Rao TS, Noble SA, Shiau AK, Hassig CA.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6888-94. doi: 10.1016/j.bmcl.2011.08.112. Epub 2011 Sep 8.


Pharmacological characterization of KLYP961, a dual inhibitor of inducible and neuronal nitric-oxide synthases.

Symons KT, Nguyen PM, Massari ME, Anzola JV, Staszewski LM, Wang L, Yazdani N, Dorow S, Muhammad J, Sablad M, Rozenkrants N, Bonefous C, Payne JE, Rix PJ, Shiau AK, Noble SA, Smith ND, Hassig CA, Zhang Y, Rao TS.

J Pharmacol Exp Ther. 2011 Feb;336(2):468-78. doi: 10.1124/jpet.110.172817. Epub 2010 Oct 29.


Discovery of inducible nitric oxide synthase (iNOS) inhibitor development candidate KD7332, part 1: Identification of a novel, potent, and selective series of quinolinone iNOS dimerization inhibitors that are orally active in rodent pain models.

Bonnefous C, Payne JE, Roppe J, Zhuang H, Chen X, Symons KT, Nguyen PM, Sablad M, Rozenkrants N, Zhang Y, Wang L, Severance D, Walsh JP, Yazdani N, Shiau AK, Noble SA, Rix P, Rao TS, Hassig CA, Smith ND.

J Med Chem. 2009 May 14;52(9):3047-62. doi: 10.1021/jm900173b.


KLYP956 is a non-imidazole-based orally active inhibitor of nitric-oxide synthase dimerization.

Symons KT, Massari ME, Nguyen PM, Lee TT, Roppe J, Bonnefous C, Payne JE, Smith ND, Noble SA, Sablad M, Rozenkrants N, Zhang Y, Rao TS, Shiau AK, Hassig CA.

Mol Pharmacol. 2009 Jul;76(1):153-62. doi: 10.1124/mol.109.055434. Epub 2009 Apr 13.


Alpha-mercaptoketone based histone deacetylase inhibitors.

Wash PL, Hoffman TZ, Wiley BM, Bonnefous C, Smith ND, Sertic MS, Lawrence CM, Symons KT, Nguyen PM, Lustig KD, Guo X, Annable T, Noble SA, Hager JH, Hassig CA, Malecha JW.

Bioorg Med Chem Lett. 2008 Dec 15;18(24):6482-5. doi: 10.1016/j.bmcl.2008.10.058. Epub 2008 Oct 17.


Identification of KD5170: a novel mercaptoketone-based histone deacetylase inhibitor.

Payne JE, Bonnefous C, Hassig CA, Symons KT, Guo X, Nguyen PM, Annable T, Wash PL, Hoffman TZ, Rao TS, Shiau AK, Malecha JW, Noble SA, Hager JH, Smith ND.

Bioorg Med Chem Lett. 2008 Dec 1;18(23):6093-6. doi: 10.1016/j.bmcl.2008.10.029. Epub 2008 Oct 11.


KD5170, a novel mercaptoketone-based histone deacetylase inhibitor, exerts antimyeloma effects by DNA damage and mitochondrial signaling.

Feng R, Ma H, Hassig CA, Payne JE, Smith ND, Mapara MY, Hager JH, Lentzsch S.

Mol Cancer Ther. 2008 Jun;7(6):1494-505. doi: 10.1158/1535-7163.MCT-08-0183.


KD5170, a novel mercaptoketone-based histone deacetylase inhibitor that exhibits broad spectrum antitumor activity in vitro and in vivo.

Hassig CA, Symons KT, Guo X, Nguyen PM, Annable T, Wash PL, Payne JE, Jenkins DA, Bonnefous C, Trotter C, Wang Y, Anzola JV, Milkova EL, Hoffman TZ, Dozier SJ, Wiley BM, Saven A, Malecha JW, Davis RL, Muhammad J, Shiau AK, Noble SA, Rao TS, Smith ND, Hager JH.

Mol Cancer Ther. 2008 May;7(5):1054-65. doi: 10.1158/1535-7163.MCT-07-2347.


Inhibition of inducible nitric oxide synthase expression by a novel small molecule activator of the unfolded protein response.

Symons KT, Massari ME, Dozier SJ, Nguyen PM, Jenkins D, Herbert M, Gahman TC, Noble SA, Rozenkrants N, Zhang Y, Rao TS, Shiau AK, Hassig CA.

Curr Chem Genomics. 2008 Sep 27;2:1-9. doi: 10.2174/1875397300802010001.


XOL-1, primary determinant of sexual fate in C. elegans, is a GHMP kinase family member and a structural prototype for a class of developmental regulators.

Luz JG, Hassig CA, Pickle C, Godzik A, Meyer BJ, Wilson IA.

Genes Dev. 2003 Apr 15;17(8):977-90. Epub 2003 Apr 2.


Three proteins define a class of human histone deacetylases related to yeast Hda1p.

Grozinger CM, Hassig CA, Schreiber SL.

Proc Natl Acad Sci U S A. 1999 Apr 27;96(9):4868-73.


Chromatin deacetylation by an ATP-dependent nucleosome remodelling complex.

Tong JK, Hassig CA, Schnitzler GR, Kingston RE, Schreiber SL.

Nature. 1998 Oct 29;395(6705):917-21.


Nuclear histone acetylases and deacetylases and transcriptional regulation: HATs off to HDACs.

Hassig CA, Schreiber SL.

Curr Opin Chem Biol. 1997 Oct;1(3):300-8. Review.


A role for histone deacetylase activity in HDAC1-mediated transcriptional repression.

Hassig CA, Tong JK, Fleischer TC, Owa T, Grable PG, Ayer DE, Schreiber SL.

Proc Natl Acad Sci U S A. 1998 Mar 31;95(7):3519-24.


Depudecin induces morphological reversion of transformed fibroblasts via the inhibition of histone deacetylase.

Kwon HJ, Owa T, Hassig CA, Shimada J, Schreiber SL.

Proc Natl Acad Sci U S A. 1998 Mar 31;95(7):3356-61.


Fiber-derived butyrate and the prevention of colon cancer.

Hassig CA, Tong JK, Schreiber SL.

Chem Biol. 1997 Nov;4(11):783-9. Review.


Nuclear receptor repression mediated by a complex containing SMRT, mSin3A, and histone deacetylase.

Nagy L, Kao HY, Chakravarti D, Lin RJ, Hassig CA, Ayer DE, Schreiber SL, Evans RM.

Cell. 1997 May 2;89(3):373-80.


Histone deacetylase activity is required for full transcriptional repression by mSin3A.

Hassig CA, Fleischer TC, Billin AN, Schreiber SL, Ayer DE.

Cell. 1997 May 2;89(3):341-7.


A mammalian histone deacetylase related to the yeast transcriptional regulator Rpd3p.

Taunton J, Hassig CA, Schreiber SL.

Science. 1996 Apr 19;272(5260):408-11.


Structural analysis of antibody specificity. Detailed comparison of five Fab'-steroid complexes.

Arevalo JH, Hassig CA, Stura EA, Sims MJ, Taussig MJ, Wilson IA.

J Mol Biol. 1994 Sep 2;241(5):663-90.


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