Rong Huang

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 protein methyltransferases and alpha N-terminal acetyltransferases
• Develop novel therapeutic agents for cancer and other diseased through targeting epigenetic pathways 

Please see: http://www.rhuanglab.com for detailed information.

MCMP205 Medicinal Organic Chemistry

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

2020 Showalter Faculty Scholar

NIH R01GM117275

NIH U01CA214649

Purdue University College of Pharmacy Startup Funds

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. 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.

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: 10.2174/1389203721666200507091952.

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.  https://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.9b01255.

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. pubs.acs.org/doi/10.1021/acs.jmedchem.9b00206

Huang R. (2019) Chemical biology of protein N-terminal methyltransferases. ChemBioChem. Young Researcher Issue: ChemBioTalents.  20 (8), 976-984. PMID: 30479015. PMCID: PMC6465133. http://onlinelibrary.wiley.com/doi/10.1002/cbic.201800615.

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 (* co-corresponding  authors) www.nature.com/articles/s42003-018-0196-2

Kronfol MM, Dozmorov MG, Huang R, Slattum PW and McClay JL (2017) The role of epigenomics in personalized medicine. Expert Review of Precision Medicine and Drug Development 2(1), 33-45. 

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 Link

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. Link

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. PMCID:PMC4691889 (* co-corresponding  authors) Link

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. PMCID:PMC4416863 Link

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. PMCID: PMC4855292. Link

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. PMCID: PMC4857722. Link
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