Institute for Applied Cancer Science

Academic Publications

Selected Peer Reviewed Publications

Novel Therapeutic strategies

Development of novel cellular histone-binding and chromatin-displacement assays for bromodomain drug discovery. Geck Do, M. Epigenetics & Chromatin, 2015, Sep 21; 8:37

The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers: Insights from cDNA Rescue and PFI-3 Inhibitor Studies. Vangamudi, B. Cancer Research, 2015, Sep 15;75(18):3865-78

Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor. Palmer, W. J. Med. Chem., 2015 June 3, Article ASAP

Niraparib: A Poly(ADP-ribose) Polymerase (PARP) Inhibitor for the Treatment of Tumors with Defective Homologous Recombination. Jones, P., Toniatti, C. J. Med. Chem., 2015, March 11; 58 (8), pp 3302–3314

Development of second generation epigenetic agents. Jones, P. Med. Chem. Commun., 3, 135-161 (2012).

Oncogenic NRAS signaling differentially regulates survival and proliferation in melanoma. Kwong LN, …et al, Chin L. Nat Med. 2012 Oct;18(10):1503-10.

Passenger deletions generate therapeutic vulnerabilities in cancer. Muller FL, …et al, Chin L, DePinho RA. Nature. 2012 Aug 16;488(7411):337-42.

Melanoma: from mutations to medicine. Tsao H, Chin L, Garraway LA, Fisher DE. Genes Dev. 2012 Jun 1;26(11):1131-55.

Antitelomerase therapy provokes ALT and mitochondrial adaptive mechanisms in cancer. Hu J, …et al, Chin L, DePinho RA. Cell. 2012 Feb 17;148(4):651-63.

Unique functions of CHK1 and WEE1 underlie synergistic anti-tumor activity upon pharmacologic inhibition. Guertin AD, …et al, Toniatti C, Shumway SD. Cancer Cell Int. 2012 Nov 13;12(1):45.

Forced mitotic entry of S-phase cells as a therapeutic strategy induced by inhibition of WEE1. Aarts M, …et al, Toniatti C, Ashworth A, Turner NC. Cancer Discov. 2012 Jun;2(6):524-39.

MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation. Wang L, …et al, Toniatti C, Milas L. Invest New Drugs. 2012 Dec;30(6):2113-20.

Identification of direct target engagement biomarkers for kinase-targeted therapeutics. Paweletz CP, Andersen JN, …et al.  PLoS One. 2011;6(10):e26459.

Genetic and pharmacological inhibition of PDK1 in cancer cells: characterization of a selective allosteric kinase inhibitor. Nagashima K, …et al, Andersen JN. J Biol Chem. 2011 Feb 25;286(8):6433-48

BET bromodomain inhibition as a therapeutic strategy to target c-Myc. Delmore JE, …et al, Heffernan TP, …et al. Cell. 2011 Sep 16;146(6):904-17

Cancer Genomics and Computational Biology

A landscape of driver mutations in melanoma. Hodis E, …et al, Chin L. Cell. 2012 Jul 20;150(2):251-63.

microRNA regulatory network inference identifies miR-34a as a novel regulator of TGF-β signaling in glioblastoma. Genovese G, …et al, Chin L. Cancer Discov. 2012 Aug;2(8):736-49.

Melanoma genome sequencing reveals frequent PREX2 mutations. Berger MF, …et al, Chin L, Garraway LA. Nature. 2012 May 9;485(7399):502-6.

Proinvasion metastasis drivers in early-stage melanoma are oncogenes. Scott KL, …et al, Chin L. Cancer Cell. 2011 Jul 12;20(1):92-103.

Making sense of cancer genomic data. Chin L, ... et al.  Genes Dev. 2011 Mar 15;25(6):534-55.

Cancer genomics: from discovery science to personalized medicine. Chin L, Andersen JN, Futreal PA. Nat Med. 2011 Mar;17(3):297-303.

Proinvasion metastasis drivers in early-stage melanoma are oncogenes. Scott KL, …et al, Chin L. Cancer Cell. 2011 Jul 12;20(1):92-103.

The BCL11B tumor suppressor is mutated across the major molecular subtypes of T-cell acute lymphoblastic leukemia. Gutierrez A, …et al, Zhang J, Protopopov A, Chin L, …et al, Mullighan CG, Look AT. 2011. Blood. 2011 Oct 13;118(15):4169-73.

Functional Genomics

Integrative functional genomics identifies RINT1 as a novel GBM oncogene. Quayle SN, …et al, Chin L. Neuro Oncol. 2012 Nov;14(11):1325-31.

Cancer Biology and Animal Models

Telomerase reactivation following telomere dysfunction yields murine prostate tumors with bone metastases. Ding Z, Wu CJ, Jaskelioff M, …et al , Zhang J, …et al, Horner JW, Wang YA, Chin L, DePinho RA. Cell. 2012 Mar 2;148(5):896-907

PTEN is a major tumor suppressor in pancreatic ductal adenocarcinoma and regulates an NF-κB-cytokine network. Ying H, …et al, Protopopov A, …et al, Chin L, Thayer SP, DePinho RA. Cancer Discov. 2011 Jul;1(2):158-69.

Telomerase reactivation reverses tissue degeneration in aged telomerase-deficient mice.  Jaskelioff M, al, Protopopov A, Horner JW, …et al, Depinho RA. Nature. 2011 Jan 6;469(7328):102-6.

SMAD4-dependent barrier constrains prostate cancer growth and metastatic progression. Ding Z, …et al, Chin L, DePinho RA. Nature. 2011 Feb 10;470(7333):269-73.


Oncogenic Kras maintains pancreatic tumors through regulation of anabolic glucose metabolism. Ying H, …et al , Chin L, Cantley LC, DePinho RA. Cell. 2012 Apr 27;149(3):656-70.

Telomere dysfunction induces metabolic and mitochondrial compromise. Sahin E, …et al, Heffernan TP, Protopopov A, …et al, Chin L, DePinho RA. Nature. 2011 Feb 17;470(7334):359-65

Assay and Technique Development

A zinc finger nuclease assay to rapidly quantitate homologous recombination proficiency in human cell lines. Yuan J, Strack PR, Toniatti C, Pelletier M. Anal Biochem. 2013 Mar 1;434(1):96-8.

A multiplexed siRNA screening strategy to identify genes in the PARP pathway. Stec E, …et al, Toniatti C, …et al. J Biomol Screen. 2012 Dec;17(10):1316-28.

PDK1 attenuation fails to prevent tumor formation in PTEN-deficient transgenic mouse models. Ellwood-Yen K, …et al, Andersen JN, Kraus M. Cancer Res. 2011 Apr 15;71(8):3052-65.

Conformation-sensing antibodies stabilize the oxidized form of PTP1B and inhibit its phosphatase activity. Haque A, Andersen JN, …et al. Cell. 2011 Sep 30;147(1):185-98