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)

2020-2025 Showalter Faculty Scholar

NIH R01GM117275

NIH U01CA214649

Purdue University College of Pharmacy Startup Funds

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://authors.elsevier.com/a/1ct4q4sz6MBAlF

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. 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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