Photo of Rong Huang
Evanson-McCoy Professor of Medicinal Chemistry and Molecular Pharmacology
Phone: 765-494-3426
E-mail: huang-r@purdue.edu
Specialization: Drug Discovery, Medicinal Chemistry and Chemical Biology, Epigenetics
Education
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)
Research

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.

Lab Members
Noha A. Ahmed (Post-Doctoral Research Associate)
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)
Service and Engagement

ACS Med Chem Division Long Range Planning Committee (2021-2023)

Editorial Board Member of the Journal of Biological Chemistry (2023-2028)

Teaching

MCMP205 Medicinal Organic Chemistry

MCMP570 Basic Principles of Chemical Action on Biological Systems (Coordinator)

Honors and Credentials

2020-2025 Showalter Faculty Scholar

2020-2025 University Faculty Scholar

 

Grants

DoD Breast Cancer Research Program Breakthrough Award (2023-2026)

NIH R01CA258887 (2021-present)

NIH R01GM117275 (2016-present)

NIH U01CA214649 (2017-2021)

 

Administration and Committee Work

Director of MCM Graduate Program

Chair of MCMP Graduate Advisory Committee

Representative Publications

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 Chemistry66, 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 N‐methyltransferase. 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), 2709-2718Link

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), 3773-3779PMID: 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