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个人简介

B.S. -1996 Tongji Medical University (Pharmacy) M.S. - 1999 Tongji Medical University (Pharmaceutical Science) Ph.D. -2006 Purdue University (Medicinal Chemistry) Postdoc. -2007-2011 Johns Hopkins University (Chemical Biology)

研究领域

Project 1: Targeting Methyltransferases to discover new drugs Project 2: Targeting Protein α-N-terminal Acetylation Our lab applies a multidisciplinary approach to: Elucidate the mechanisms and functions of epigenetic modifications including methylation and acetylation Rational design and synthesize selective and potent inhibitors for methyltransferases and acetyltransferases Develop novel therapeutic agents for cancer and other diseases through targeting epigenetic pathways

近期论文

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Deng Y, Dong G, Meng Y, Noinaj N, Huang R. (2022) Structure-activity relationship studies of Venglustat on NTMT1 inhibition. Journal of Medicinal Chemistry. Dong G, Deng Y, Yasgar A, Yadav R, Talley D, Zakharov A, Jain S, Ganesha R, Noinaj N, Simeonov A, Huang R. (2022) Venglustat inhibits protein N-terminal methyltransferase 1 in a substrate-competitive manner. Journal of Medicinal Chemistry. In press. Iyamu ID, Vilseck J, Yadav R, Noinaj N, Huang R. (2022) Exploring unconventional SAM analogs to build cell-potent bisubstrate inhibitors for Nicotinamide N‐methyltransferase. Angewandte Chemie International Edition. Feb 8. https://onlinelibrary.wiley.com/doi/10.1002/anie.202114813​ Ho Y and Huang R. (2022) Effects of oncohistone mutations and PTM crosstalk on the N-terminal acetylation activities of NatD. ACS Chemical Biology. Jan 19. PMID: 35044762. https://pubs.acs.org/doi/full/10.1021/acschembio.1c00840 Griffiths A, Wang J, Song Q, Iyamu ID, Liu L, Park J, Jiang Y, Huang R, Song Z. (2021) Nicotinamide N-methyltransferase (NNMT) upregulation via the mTORC1-ATF4 pathway activation contributes to palmitate-induced lipotoxicity in hepatocytes. American Journal of Physiology-Cell Physiology. 321(3), C585-C595. PMID: 34378991. pubmed.ncbi.nlm.nih.gov/34378991/ Chen D, Meng Y, Yu D, Noinaj N, Chen X, Huang R. (2021) Chemoproteomic study uncovers HemK2/KMT9 as a new target for NTMT1 bisubstrate inhibitors. ACS Chemical Biology. https://pubs.acs.org/doi/pdf/10.1021/acschembio.1c00279 Deng Y, Deng S, Ho Y, Gardner SM, Huang Z, Marmorstein R, Huang R. (2021) Novel bisubstrate inhibitors for protein N-terminal acetyltransferase D. Journal of Medicinal Chemistry. 64, 8263-8271. PMID: 34110812. pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.1c00141 Iyamu ID, Al-Hamashi AA and Huang R. (2021) A pan-inhibitor for protein arginine methyltransferase family enzymes. Biomolecules. 11(6), 854. www.mdpi.com/2218-273X/11/6/854. Iyamu ID, and Huang R. (2021) Mechanisms and inhibitors of nicotinamide N-methyltransferase. RSC Medicinal Chemistry. doi.org/10.1039/D1MD00016K Diaz K, Meng Y, Huang R. (2021) Past, present, and perspectives of protein N-terminal methylation. Current Opinion in Chemical Biology. 63, 115-122. https://pubmed.ncbi.nlm.nih.gov/33839647/ Chen D, Dong G, Deng Y, Noinaj N, Huang R. (2021) Structure-based Discovery of Cell-potent Peptidomimetic Inhibitors for Protein N-terminal Methyltransferase 1. ACS Medicinal Chemistry Letters. 12, 485-493. https://pubs.acs.org/doi/full/10.1021/acsmedchemlett.1c00012 Ho Y, Chen L, Huang R. (2021) Development of a continuous fluorescence-based assay for N-terminal acetyltransferase D. International Journal of Molecular Sciences. 22, 594. PMID: 33435607; PMCID:PMC7827481. www.mdpi.com/1422-0067/22/2/594 Al-Hamashi AA, Chen D, Deng Y, Dong G, Huang R. (2020) Discovery of a Potent and Dual-Selective Bisubstrate Inhibitor for Protein Arginine Methyltransferase 4/5. Acta Pharmaceutica Sinica B. in press. https://doi.org/10.1016/j.apsb.2020.10.013 Mackie BD, Chen D, Dong G, Dong C, Parker H, Schaner Tooley C, Noinaj N, Min J, Huang R. (2020) Selective Peptidomimetic Inhibitors of NTMT1/2: Rational design, synthesis, characterization, and crystallographic studies. Journal of Medicinal Chemistry. 63, 9512-9522. PMID: 32689795. PMCID: PMC74286280. https://pubs.acs.org/doi/10.1021/acs.jmedchem.0c00689 Chen D, Dong C, Dong G, Srinivasan K, Min J. Noinaj N, Huang R. (2020) Probing the plasticity in the active site of protein N-terminal methyltransferase 1 using bisubstrate analogs. Journal of Medicinal Chemistry. 63, 8419-8431. PMID: 32605369. https://pubs.acs.org/doi/10.1021/acs.jmedchem.0c00770 Iyamu, I. D., and Huang, R. (2020) Development of fluorescence polarization-based competition assay for nicotinamide N-methyltransferase. Analytical Biochemistry: Methods in the Biological Sciences. 604, 113833. PMID: 32622979. https://pubmed.ncbi.nlm.nih.gov/32622979/ Dong G., Yasgar A., Darrell Dl, Zakharov A., Talley D., Cheng K., Jadhav A., Simeonov A., Huang R. (2020) Optimization of high-throughput methyltransferase assays for the discovery of small molecule inhibitors. ACS Combinatorial Science. 22, 422-432. PMID: 32525297. PMCID: PMC7429283. https://pubs.acs.org/doi/10.1021/acscombsci.0c00077.

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