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|Graduate Students||Postdoctoral Fellows||Researchers / Staff||Principal Investigator|
Deepak Gurbani, Ph.D. – Biophysics/Biochemistry
Education: B.S – Biology, 1999, Kanpur University, India. M.S – Botany, 2001, Kanpur University, India. Ph.D – Biotechnology, 2012, CSIR-Indian Institute of Toxicology Research & Jamia Hamdard University, New Delhi, India.
Research interests: Mechanisms that transform normal cells to cancer cells are complex. I study how small molecules perturb the function of key cellular enzymes. Kinases play a vital role in cellular physiology and normal and abnormal growth. My research includes performing X-ray crystallography, enzymatic and cellular assays to study structure and function of different kinases. I also work in collaboration with medicinal chemists to develop reversible and irreversible inhibitors of kinases involved in different cancers.
J. Totzke, D. Gurbani*, R. Raphemot, P.F. Hughes, K. Bodoor, D.A. Carlson, D. R. Loiselle, A. K. Bera, L.S. Eibschutz, M.M. Perkins, A.L. Eubanks, P. Campbell, D.A. Fox, K.D. Westover, T.A. Haystead, E.R. Derbyshire. Takinib, an exquisitely selective inhibitor of TAK1, targets pro survival TNFα-dependent signaling, inducing apoptosis in rheumatoid arthritis and breast cancer models. Cell Chemical Biology 24 (2017), 1029–1039.
L. Tan, D. Gurbani*, E.L. Weisberg, D.S. Jones, S. Rao, W.D. Singer, F.M. Bernard, S. Mowafy, A. Jenney, G. Du, A. Nonami, J.D. Griffin, D.A. Lauffenburger, K.D. Westover, P.K. Sorger, N.S. Gray, Studies of TAK1-centered polypharmacology with novel covalent TAK1 inhibitors, Bioorg Med Chem, 25 (2017) 1320-1328.
L. Tan, D. Gurbani*, E.L. Weisberg, J.C. Hunter, L. Li, D.S. Jones, S.B. Ficarro, S. Mowafy, C.P. Tam, S. Rao, G. Du, J.D. Griffin, P.K. Sorger, J.A. Marto, K.D. Westover, N.S. Gray, Structure-guided development of covalent TAK1 inhibitors, Bioorg Med Chem, 25 (2017) 838-846.
L. Tan, T. Nomanbhoy, D. Gurbani, M. Patricelli, J. Hunter, J. Geng, L. Herhaus, J. Zhang, E. Pauls, Y. Ham, H.G. Choi, T. Xie, X. Deng, S.J. Buhrlage, T. Sim, P. Cohen, G. Sapkota, K.D. Westover, N.S. Gray, Discovery of type II inhibitors of TGFbeta-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2), J Med Chem, 58 (2015) 183-196.
J.C. Hunter, D. Gurbani, S.B. Ficarro, M.A. Carrasco, S.M. Lim, H.G. Choi, T. Xie, J.A. Marto, Z. Chen, N.S. Gray, K.D. Westover, In situ selectivity profiling and crystal structure of SML-8-73-1, an active site inhibitor of oncogenic K-Ras G12C, Proc Natl Acad Sci U S A, 111 (2014) 8895-8900.
D. Gurbani, V. Kukshal, J. Laubenthal, A. Kumar, A. Pandey, S. Tripathi, A. Arora, S.K. Jain, R. Ramachandran, D. Anderson, A. Dhawan, Mechanism of inhibition of the ATPase domain of human topoisomerase IIalpha by 1,4-benzoquinone, 1,2-naphthoquinone, 1,4-naphthoquinone, and 9,10-phenanthroquinone, Toxicol Sci, 126 (2012) 372-390. Article on Cover Page, April issue.
Yan Liu, Ph.D. – Cancer Biology
Education: B.S. - Biochemistry, 1999, Nankai University, China; Ph.D. – Biochemistry, 2009, Ohio University
Research interests: Cancer Biology, Kinase Inhibitor Development, Molecular Cancer Epidemiology
Yan Liu, Csaba Laszlo, Yi Liu, Wei Liu, Xiaozhuo Chen, Susan C Evans, Shiyong Wu. (2010) Regulation of G1 Arrest and Apoptosis in Hypoxia by PERK and GCN2-mediated eIF2 Phosphorylation. Neoplasia 12(1): 61–68.
Yan Liu, Pui-Kai Li, Chenglong Li, Jiayuh Lin. (2010) Inhibition of STAT3 Signaling Blocks the Anti-Apoptotic Activity of IL-6 in Human Liver Cancer Cells. Journal of Biological Chemistry 285(35):27429-39.
Yan Liu, James Fuchs, Chenglong Li, Jiayuh Lin. (2010) IL-6, a Risk Factor for Hepatocellular Carcinoma: FLLL32 Inhibits IL-6-Induced STAT3 Phosphorylation in Human Hepatocellular Cancer Cells. Cell Cycle 9(17):3423-7.
Yan Liu, Aiguo Liu, Zhenghu Xu, Wenying Yu, Hong Wang, Chenglong Li, Jiayuh Lin. (2011) XZH-5 Inhibits Constitutive and Interleukin-6-Induced STAT3 Phosphorylation in Human Hepatocellular Carcinoma Cells. Apoptosis 16(5):502-10.
Yan Liu, Aiguo Liu, Huameng Li, Chenglong Li, Jiayuh Lin. (2011) Celecoxib Inhibits Constitutive and Interleukin-6-Induced STAT3 Phosphorylation in Human Hepatocellular Carcinoma Cells. Cancer Prevention Research 4(8):1296-305.
Yan Liu, Oriana E. Hawkins, Yingjun Su, Anna Vilgelm, Tammy Sobolik-Delmaire, Yee-Mon Thu, Sara Kantrow, Ryan C. Splittgerber, Sara Short, Katayoun I. Amiri, Jeffery A. Ecsedy, Jeffery A. Sosman, Mark C. Kelley, Ann Richmond. (2013) Targeting Aurora Kinases Limits Tumor Growth through DNA Damage Mediated Senescence and Blockade of NF-κB Impairs this Drug Induced Senescence. EMBO Molecular Medicine 5(1): 1946-66.
Yan Liu, Qiuyin Cai, Ping-Ping Bao, Yinghao Su, Hui Cai, Jie Wu, Fei Ye, Xingyi Guo, Wei Zheng, Ying Zheng, and Xiao-Ou Shu. (2015) Tumor tissue microRNA expression in association with triple-negative breast cancer outcomes. Breast Cancer Research and Treatment 152 (1): 183-191
Yan Liu, Oriana E Hawkins, Anna E Vilgelm, Jeff S Pawlikowski, Jeffrey A Ecsedy, Jeffrey Alan Sosman, Mark C Kelley, Ann Richmond. (2015) Combining an Aurora Kinase Inhibitor and a Death Receptor Ligand/Agonist Antibody Triggers Apoptosis in Melanoma Cells and Prevents Tumor Growth in Preclinical Mouse Models. Clinical Cancer Research Online First July 7, 2015; doi: 10.1158/1078-0432
Yan Liu , Michelle Baglia , Ying Zheng , William Blot , Ping-Ping Bao , Hui Cai , Sarah Nechuta , Wei Zheng , Qiuyin Cai, and Xiao-Ou Shu. (2015) ALDH1A1 mRNA expression in Association with Prognosis of Triple-Negative Breast Cancer. Oncotarget Online First October 8, 2015; doi: 10.18632/oncotarget.6023
Harshbarger, W., Gondi, S., Ficarro, S.B., Hunter, J., Udayakumar, D., Gurbani, D., Singer, W.D., Liu, Y., Li, L., Marto, J.A., and Westover, K.D.; Structural and Biochemical Analyses Reveal the Mechanism of Glutathione-S-Transferase Pi 1 Inhibition by the Anti-cancer Compound Piperlongumine; J. Biol. Chem. 292: 112-120 (2017).
Lianbo Li, Ph.D. – Biophysics/Biochemistry
Education: B.S. – Biotechnology, 2007, Shandong Normal University, China; PhD – Cell Biology, 2014, Peking University, China.
Research interests: Protein structure guided drug discovery with emphasis on the oncogenic protein KRAS.
Zeng, M., Lu, J., Li, L., Feru, F., Quan, C., Gero, T. W., Ficarro, S. B., Xiong, Y., Ambrogio, C., Paranal, R. M., Catalano, M., Shao, J., Wong, K. K., Marto, J. A., Fischer, E. S., Janne, P. A., Scott, D. A., Westover, K. D., and Gray, N. S. (2017) Potent and Selective Covalent Quinazoline Inhibitors of KRAS G12C. Cell Chem Biol.
Lu, J., Harrison, R. A., Li, L., Zeng, M., Gondi, S., Scott, D., Gray, N. S., Engen, J. R., and Westover, K. D. (2017) KRAS G12C Drug Development: Discrimination between Switch II Pocket Configurations Using Hydrogen/Deuterium-Exchange Mass Spectrometry. Structure.
Xiong, Y., Lu, J., Hunter, J., Li, L., Scott, D., Choi, H. G., Lim, S. M., Manandhar, A., Gondi, S., Sim, T., Westover, K. D., and Gray, N. S. (2017) Covalent Guanosine Mimetic Inhibitors of G12C KRAS. ACS medicinal chemistry letters 8, 61-66.
Montalvo, S. K., Li, L., and Westover, K. D. (2017) Rationale for RAS mutation-tailored therapies. Future Oncol 13, 263-271.
Li, L., Zhang, W., Liu, Q., Gao, Y., Gao, Y., Wang, Y., Wang, D. Z., Li, Z., and Wang, T. (2013) Structural Insights on the bacteriolytic and self-protection mechanism of muramidase effector Tse3 in Pseudomonas aeruginosa. J Biol Chem 288, 30607-30613.
Zhi-Wei (George) Zhou, Ph.D. – Cancer Biology/Biophysics
Education: B.S.- Biotechnology and Pharmacology, 2007, Nanchang University, China; Ph.D.- Health Sciences, 2013, RMIT University, Melbourne, Australia
Research interests: Cancer pharmacology and anticancer drug (synthesized and natural compounds) discovery and development, with a specific focus on KRAS.
He SJ, Shu LP, Zhou ZW, Yang TX, Duan W, Zhang X, He ZX, Zhou SF. Inhibition of Aurora kinases induces apoptosis and autophagy via AURKB/p70S6K/RPL15 axis in human leukemia cells. 2016; Cancer Letters 2016 Sep 6;382(2):215-230.
Li YC, He SM, He ZX, Li M, Yang Y, Pang JX, Zhang X, Chow K, Zhou Q, Duan W, Zhou ZW, Yang T, Huang GH, Liu A, Qiu JX, Liu JP & Zhou SF. Plumbagin induces apoptotic and autophagic cell death through inhibition of the PI3K/Akt/mTOR pathway in human non-small cell lung cancer cells. Cancer Lett 2014 Mar 28;344(2):239-259. 24280585.
Li M, Yang Y, He ZX, Zhou ZW, Yang T, Guo P, Zhang X & Zhou SF. MicroRNA-561 promotes acetaminophen-induced hepatotoxicity in HepG2 cells and primary human hepatocytes through down-regulation of the nuclear receptor co-repressor dosage-sensitive sex reversal adrenal hypoplasia congenital critical region on X chromosome, gene 1 (DAX-1). Drug Metab Dispos 2014 Jan;42(1):44-61. 24104199.
Zhou ZW, Xie XL, Zhou SF & Li CG. Mechanism of reversal of high glucose-induced endothelial nitric oxide synthase uncoupling by tanshinone IIA in human endothelial cell line EA.hy926. Eur J Pharmacol 2012 Dec 15;697(1-3):97-105.
Xingxiao (Shelly) Li, M.S.– Cancer Biology
Education: B.S. – Biotechnology, 2007, Nanchung University, China ; M.S. – Cancer Biology, 2010, Guangdong Cardiovascular Institute, China
Research interests: Development of cellular and biological techniques, including, but not limited to culturing noncancerous and cancerous cell lines and molecular biology.