M.S. - 1999 Tongji Medical University (Pharmaceutical Science)
Ph.D. -2006 Purdue University (Medicinal Chemistry)
Postdoc. -2007-2011 Johns Hopkins University (Chemical Biology)
Currently Accepting Students
Project 1: Targeting Methyltransferases to discover new drugs
Project 2: Targeting Protein α-N-terminal Acetylation
Project 3: Targeting N-/C-degron
Our lab applies a multidisciplinary approach to:
- Elucidate the mechanisms and functions of epigenetic modifications including methylation and acetylation to develop novel therapeutic agents for cancer, metabolic, infectious, and neurodegenerative diseases
- Rational design and synthesize selective and potent inhibitors for methyltransferases and acetyltransferases
- Develop HTS assay and efficiently create compound libraries to screen lead compounds.
Please see: http://www.rhuanglab.com for detailed information.
Shihao Cheng (Post-Doctoral Research Associate)
Julian Andres Gonzalez Cortes (Graduate Student)
Ming He (Research Associate)
Yi-Hsun Ho (Graduate Student)
Baharul Islam (Post-Doctoral Research Associate)
Akshay Suhas Kulkarni (Post-Doctoral Research Associate)
Ying Meng (Graduate Student)
Hye S. (Regina) Nam (Graduate Student)
Emma K. Seipp (Graduate Student)
Tianqi Zhao (Graduate Student)
ACS Med Chem Division Long Range Planning Committee (2021-2023)
Editorial Board Member of the Journal of Biological Chemistry (2023-2028)
MCMP205 Medicinal Organic Chemistry
MCMP570 Basic Principles of Chemical Action on Biological Systems (Coordinator)
2020-2025 Showalter Faculty Scholar
2020-2025 University Faculty Scholar
DoD Breast Cancer Research Program Breakthrough Award (2023-2026)
NIH R01CA258887 (2021-present)
NIH R01GM117275 (2016-present)
NIH U01CA214649 (2017-2021)
Director of MCM Graduate Program
Chair of MCMP Graduate Advisory Committee
2018-present
# co-first author; * co-corresponding author
Iyamu ID, Zhao T, and Huang R. (2023) Structure-activity relationship studies on cell-potent bisubstrate inhibitors of nicotinamide N-methyltransferase. Journal of Medicinal Chemistry. 66, 10510-10527 Link
Deng Y#, Song X#, Iyamu ID, Dong A, Min J*, and Huang R*. (2023) A unique binding pocket induced by a noncanonical SAH mimic to develop potent and selective PRMT inhibitors. Acta Pharmaceutica Sinica B. Available online July 29 Link
Meng Y. and Huang R. (2023) Site-specific methylation on α-N-terminus of peptides through chemical and enzymatic methods. Methods in Enzymology. Protein Termini – modifications and targeting. Link
Zhou J#, Deng Y#, Iyamu ID, Horton J, Yu D, Hajian T, Vedadi M, Rotili D, Mai A, Blumenthal R, Zhang X, Huang R*, Cheng X*. (2023) Comparative study of adenosine analogs as inhibitors of protein arginine methyltransferases and a Clostridioides difficile-specific DNA adenine methyltransferase. ACS Chemical Biology. 18, 734-745. Link
Deng Y, Dong G, Meng Y, Noinaj N, Huang R. (2023) Structure-activity relationship studies of Venglustat on NTMT1 inhibition. Journal of Medicinal Chemistry. 66 (2), 1601-1605. Link
Ho Y and Huang R. (2023) Effects of oncohistone mutations and PTM crosstalk on the N-terminal acetylation activities of NatD. ACS Chemical Biology. 18, 693-700. PMID: 35044762. Link
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. 65 (18), 12334-12345. Link
Iyamu ID, Vilseck J, Yadav R, Noinaj N, Huang R. (2022) Exploring unconventional SAM analogs to build cell-potent bisubstrate inhibitors for Nicotinamide Nâmethyltransferase. Angewandte Chemie International Edition. Feb 8. Link
Dong G, Iyamu ID, Vilseck J, Chen D, Huang R. (2022) Improved Cell-potent and Selective Peptidomimetic Inhibitors of Protein N-terminal Methyltransferase 1. Molecules. 27, 1381. Link
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. Link
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. 16, 1234-1242. Link
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. Link
Iyamu ID, Al-Hamashi AA and Huang R. (2021) A pan-inhibitor for protein arginine methyltransferase family enzymes. Biomolecules. 11(6), 854. Link
Iyamu ID, and Huang R. (2021) Mechanisms and inhibitors of nicotinamide N-methyltransferase. RSC Medicinal Chemistry. 12, 1254 - 1261. Link
Diaz K, Meng Y, Huang R. (2021) Past, present, and perspectives of protein N-terminal methylation. Current Opinion in Chemical Biology. 63, 115-122. Link
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. Link
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. Link
Al-Hamashi AA, Chen D, Deng Y, Dong G, Huang R. (2021) Discovery of a Potent and Dual-Selective Bisubstrate Inhibitor for Protein Arginine Methyltransferase 4/5. Acta Pharmaceutica Sinica B. 11(9), 2709-2718. Link
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. Link
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. Link
Iyamu ID 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. Link
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. Link
Al-Hamashi A, Diaz K, Huang R (2020) Non-histone arginine methylation by protein arginine methyltransferases. Current Protein & Peptide Science 21(7), 699-712. PMID: 32379587. DOI: Link
Chen D, Li L, Diaz K, Iyamu I, Yadav R, Noinaj N, Huang R. (2019) Novel propargyl-linked bisubstrate analogs as tight-binding Inhibitors for nicotinamide N-methyltransferase. Journal of Medicinal Chemistry 62 (23), 10783-10797. PMID: 31724854. Link
Chen D, Dong G, Noinaj N, Huang R. (2019) Discovery of bisubstrate inhibitors for protein N-terminal methyltransferase 1. Journal of Medicinal Chemistry 62(7), 3773-3779. PMID: 30883119. Link
Huang R. (2019) Chemical biology of protein N-terminal methyltransferases. ChemBioChem. Young Researcher Issue: ChemBioTalents. 20 (8), 976-984. PMID: 30479015. PMCID: PMC6465133. Link
Cheng D#, Dong G#, Li L, Zhu L., Tempel W, Liu Y, Huang R*, and Jin M*. (2018) An asparagine/glycine switch governs product specificity of human N-terminal methyltransferase NTMT2. Communications Biology 1, 183. PMID: 30417120. PMCID: PMC6214909 Link