vcu bar

Rong Huang, Ph.D.

Assistant Professor
Department of Medicinal Chemistry

Location:  Virginia Biotechnology Research Park, Suite 212
Phone: (804) 828-5619
Web: Research Website

Mailing Address

School of Pharmacy - Dept of Medicinal Chemistry
BioTech One, Suite 205
800 E. Leigh St.
P.O. Box 980540
Richmond, VA 23298-0540
Fax: (804) 827-3664


  • Ph.D., Medicinal Chemistry (Purdue University, 2006)
  • M.S., Pharmaceutical Sciences (Tongji Medical University, 1999)
  • B.Pharm., Pharmacy (Tongji Medical University, 1996)

Post-Graduate Training

  • postdoc - Chemical biology (Johns Hopkins University, 2011)

Academic Appointments/Professional Experience

  • (2011 - Present) Assistant Professor, Dept. of Medicinal Chemistry, VCU School of Pharmacy
  • (2011 - Present) Member, Institute for Structural Biology, Drug Discovery & Development
  • (2011 - Present) Associate Member, VCU Massey Cancer Center

Research Interests

  • Understand the molecular mechanisms of protein post-translational modifications including methylation, acetylation, and phosphorylation; Design and synthesize selective and potent inhibitors to manipulate and probe the epigenetic pathways; Develop novel and targeted cancer therapies through a multidisciplinary approach encompassing the fields of organic and peptide synthesis, chemoproteomics, enzymology, and cell biology.


  • Patents
    • Huang R, Hwang Y, Cole PA. A novel method for site-specific introduction of an acetyl-lysine mimic into peptides and proteins by cysteine conjugation. International Patent Application No. PCT/US2010/053523, Published No. WO 2011/050152.
  • Recent Publications
    • Huang R, Martinez-Ferrando I, Cole PA. (2010) Enhanced interrogation: emerging strategies for cell signaling inhibition. Nature Structural and Molecular Biology, 17(6), 646-649.
    • Huang R, Holbert MA, Tarrant MK, Benitski S, Colquhoun DR, Dancy BM, Dancy BC, Hwang Y, Tang Y, Meeth K, Marmorstein R, Cole RN, Khochbin S, Cole PA. (2010) Site-specific introduction of an acetyl-lysine mimic into peptides and proteins by cysteine alkylation. Journal of American Chemical Society, 132(29), 9986-9987. • The results were highlighted by Chemical & Engineering News in July 19th issue, 2010, 88,32.
    • Blair LP, Avaritt NL, Huang R, Cole PA, Taverna SD, Tackett AJ. (2011) MassSQUIRM: An assay for quantitative measurement of lysine demethylase activity. Epigenetics, 6(4), 490-499.
    • Marian C, Huang R, Borch RF. (2011) Design and synthesis of a potential SH2 domain inhibitor bearing a stereodiversified 1,4-cis-enediol scaffold. Tetrahedron, 67(52), 10216-10221.
    • Huang R, Oh H, Arrendale A, Martin VA, Galan J, Workman EJ, Stout JR, Walczak CE, Tao WA, Borch RF, Geahlen RL. (2013) Intracellular targets for a phosphotyrosine peptidomimetic include the mitotic kinesin, MCAK. Biochemical Pharmacology 86(5):597-611. doi: 10.1016/j.bcp.2013.06.024. Epub 2013 Jul 4.
    • Nahomi RB, Huang R, Panda A, Wang B, Padmanabha S, Santhoshkumar P, Filipek S, Biswas A, Nagaraj RH. (2013) Acetylation of Lysine92 Improves the Chaperone and Anti-apoptotic Activities of Human aB-Crystallin. Biochemistry, 52(45), 8126-8138. doi: 10.1021/bi400638s. Epub 2013 Oct 15.
    • Prusevich P, Kalin JH, Ming SA, Basso M, Givens J, Li X, Hu J, Taylor MS, Cieniewicz AM, Hsiao PY, Huang R, Roberson H, Adejola N, Avery LB, Casero RA Jr, Taverna SD, Qian J, Tackett AJ, Ratan RR, McDonald OG, Feinberg AP, Cole PA. (2014) A selective phenelzine analogue inhibitor of histone demethylase LSD1. ACS Chemical Biology. Epub 2014 April 7.
    • Zhang G, Richardson SL, Mao Y, Huang R. (2015) Design, synthesis, and kinetic analysis of potent protein N-terminal methyltransferase 1 inhibitors. Organic & Biomolecular Chemistry. 13, 4149-4154. PMID: 25712161.
    • Richardson SL, Hanjra P, Zhang G, Mackie BD, Peterson DL, Huang R. (2015) A Direct, ratiometric, and quantitative MALDI-MS assay for protein methyltransferases and acetyltransferases. Analytical Biochemistry: Methods in the Biological Sciences, 478, 59-64. PMID: 25778392.
    • Richardson SL, Mao Y, Zhang G, Hanjra P, Peterson DL, Huang R. (2015) Mechanistic studies of protein N-terminal RCC1 methyltransferase 1. Journal of Biological Chemistry, 290 (18), 11601-11610. PMID: 25771539.
    • Cheng D*, Mao Y*, Tempel W, Qin S, Li L, Loppnau P, Huang R, and Jin M. (2015) Structural basis for the substrate recognition by the human N-terminal methyltransferase 1. Gene & Development, 29 (22), 2343-2348. PMID: 26543161. (* co-first authors)
    • Zhang G, Huang R. (2016) Facile Synthesis of SAM-Peptide Conjugates through Alkyl Linkers Targeting Protein N-terminal Methyltransferase 1. RSC Advance, 6, 6768-6771.
    • Khalil EM, Mackie BD, Mao Y, and Huang R. (2016) Methyltransferases: Key Regulators in Cardiovascular Development and Disease. Annals of Vascular Medicine and Research. 3(2): 1032. Invited Review