Rong Huang

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 neurodenegerative 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.

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

MCMP205 Medicinal Organic Chemistry

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

2020-2025 Showalter Faculty Scholar

2020-2025 University Faculty Scholar

NIH R01CA258887 (2021-present)

NIH R01GM117275 (2016-present)

NIH U01CA214649 (2017-2021)

Purdue University College of Pharmacy Startup Funds

Chair of MCMP Graduate Advisory Committee

2018-present

^# co-first author; * co-corresponding  author

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. 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

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 

Ho Y and Huang R. (2022) Effects of oncohistone mutations and PTM crosstalk on the N-terminal acetylation activities of NatD. ACS Chemical Biology. Jan 19. PMID: 35044762. 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