Publications
33. 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. in press. www.biorxiv.org/content/10.1101/2021.04.13.439666v1
32. 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. In press. pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.1c00141
31. Iyamu ID, Al-Hamashi AA and Huang R. (2021) A pan-inhibitor for protein arginine methyltransferase family enzymes. Biomolecules. 11(6), 854. www.mdpi.com/2218-273X/11/6/854
Invited submission to the Collection Feature Papers in Enzymology
30. Iyamu ID, and Huang R. (2021) Mechanisms and inhibitors of nicotinamide N-methyltransferase. RSC Medicinal Chemistry. doi.org/10.1039/D1MD00016K. (Invited review)
29. Diaz K, Meng Y, Huang R. (2021) Past, present, and perspectives of protein N-terminal methylation. Current Opinion in Chemical Biology. 63, 115-122. PMID: 33839647. https://www.sciencedirect.com/science/article/abs/pii/S1367593121000399
Invited review to a themed issue on Chemical genetics and epigenetics
28. 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. PMID: 33738076; PMCID:PMC7958150. pubs.acs.org/doi/full/10.1021/acsmedchemlett.1c00012
27. 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. www.mdpi.com/1422-0067/22/2/594. Invited submission to a special issue "Modifications of Protein Termini"
26. 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. www.sciencedirect.com/science/article/pii/S2211383520307656 Invited submission
25. 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
24. 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. PMCID: PMC7429357. https://pubs.acs.org/doi/10.1021/acs.jmedchem.0c00770
23. 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. PMCID: PMC7416818. https://pubmed.ncbi.nlm.nih.gov/32622979/
22. 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.
21. 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. PMCID: PMC7529871. DOI: 10.2174/1389203721666200507091952.
20. 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; PMCID: PMC7296983. www.ncbi.nlm.nih.gov/pubmed/31724854
19. 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; PMCID:PMC6760264 pubs.acs.org/doi/10.1021/acs.jmedchem.9b00206
18. 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.
17. Dong C, 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
16. 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. PMID: 29276780. PMCID: PMC5737812. https://doi.org/10.1080/23808993.2017.1284557
15. 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): 1032-1039. Invited Review Link
14. 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. PMID: 27588169. PMCID: PMC5004777. Link
13. Dong C, 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
12.Richardson SL, Mao Y, Zhang G, Hanjra P, Peterson DL, Huang R. (2015) Mechanistic studies of protein N-terminal methyltransferase 1. Journal of Biological Chemistry, 290 (18), 11601-11610. PMID: 25771539. PMCID:PMC4416863 Link
11. 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
10. 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
This work was highlighted in its front cover image.
9. 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.9(6), 1284-93. PMID:24707965. PMCID: PMC4076021. Link
8. 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. PMID:24128140; PMCID: PMC3889837. Link
7. 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 Pharmacology86(5):597-611. PMID:23830822; PMCID: PMC3755495. Link
6. 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. PMID:22199405; PMCID: PMC3244727. Link
5.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. PMID:21273814; PMCID: PMC3230537. Link
4. 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. PMID:20608637. PMCID: PMC2912447. Link
• The results were highlighted by Chemical & Engineering News in July 19th issue, 2010, 88,32.
3. 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. PMID:20520657; PMCID: PMC3160762. Link
2. Zhu J, Huang R, Li C, Xiong Y. (2000) Studies on the synthetic technique of Dequalinium Chloride. Chinese Pharmacist, 3(2), 73-74.
1. Huang R, Zhu J, Li S. (2000) Progress of study on the structure-activity relationships of Dequalinium analogues. Herald of Medicine, 19(3), 267-268.
32. 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. In press. pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.1c00141
31. Iyamu ID, Al-Hamashi AA and Huang R. (2021) A pan-inhibitor for protein arginine methyltransferase family enzymes. Biomolecules. 11(6), 854. www.mdpi.com/2218-273X/11/6/854
Invited submission to the Collection Feature Papers in Enzymology
30. Iyamu ID, and Huang R. (2021) Mechanisms and inhibitors of nicotinamide N-methyltransferase. RSC Medicinal Chemistry. doi.org/10.1039/D1MD00016K. (Invited review)
29. Diaz K, Meng Y, Huang R. (2021) Past, present, and perspectives of protein N-terminal methylation. Current Opinion in Chemical Biology. 63, 115-122. PMID: 33839647. https://www.sciencedirect.com/science/article/abs/pii/S1367593121000399
Invited review to a themed issue on Chemical genetics and epigenetics
28. 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. PMID: 33738076; PMCID:PMC7958150. pubs.acs.org/doi/full/10.1021/acsmedchemlett.1c00012
27. 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. www.mdpi.com/1422-0067/22/2/594. Invited submission to a special issue "Modifications of Protein Termini"
26. 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. www.sciencedirect.com/science/article/pii/S2211383520307656 Invited submission
25. 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
24. 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. PMCID: PMC7429357. https://pubs.acs.org/doi/10.1021/acs.jmedchem.0c00770
23. 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. PMCID: PMC7416818. https://pubmed.ncbi.nlm.nih.gov/32622979/
22. 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.
21. 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. PMCID: PMC7529871. DOI: 10.2174/1389203721666200507091952.
20. 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; PMCID: PMC7296983. www.ncbi.nlm.nih.gov/pubmed/31724854
19. 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; PMCID:PMC6760264 pubs.acs.org/doi/10.1021/acs.jmedchem.9b00206
18. 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.
17. Dong C, 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
16. 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. PMID: 29276780. PMCID: PMC5737812. https://doi.org/10.1080/23808993.2017.1284557
15. 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): 1032-1039. Invited Review Link
14. 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. PMID: 27588169. PMCID: PMC5004777. Link
13. Dong C, 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
12.Richardson SL, Mao Y, Zhang G, Hanjra P, Peterson DL, Huang R. (2015) Mechanistic studies of protein N-terminal methyltransferase 1. Journal of Biological Chemistry, 290 (18), 11601-11610. PMID: 25771539. PMCID:PMC4416863 Link
11. 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
10. 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
This work was highlighted in its front cover image.
9. 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.9(6), 1284-93. PMID:24707965. PMCID: PMC4076021. Link
8. 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. PMID:24128140; PMCID: PMC3889837. Link
7. 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 Pharmacology86(5):597-611. PMID:23830822; PMCID: PMC3755495. Link
6. 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. PMID:22199405; PMCID: PMC3244727. Link
5.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. PMID:21273814; PMCID: PMC3230537. Link
4. 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. PMID:20608637. PMCID: PMC2912447. Link
• The results were highlighted by Chemical & Engineering News in July 19th issue, 2010, 88,32.
3. 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. PMID:20520657; PMCID: PMC3160762. Link
2. Zhu J, Huang R, Li C, Xiong Y. (2000) Studies on the synthetic technique of Dequalinium Chloride. Chinese Pharmacist, 3(2), 73-74.
1. Huang R, Zhu J, Li S. (2000) Progress of study on the structure-activity relationships of Dequalinium analogues. Herald of Medicine, 19(3), 267-268.