Literature DB >> 27588169

Facile synthesis of SAM-peptide conjugates through alkyl linkers targeting protein N-terminal methyltransferase 1.

Gang Zhang1, Rong Huang1.   

Abstract

We report the first chemical synthesis of SAM-peptide conjugates through alkyl linkers to prepare bisubstrate analogs for protein methyltransferases. We demonstrate its application by developing a series of bisubstrate inhibitors for protein N-terminal methyltransferase 1 and the most potent one exhibits a Ki value of 310 ± 55 nM.

Entities:  

Year:  2016        PMID： 27588169      PMCID： PMC5004777          DOI： 10.1039/C5RA20625A

Source DB:  PubMed          Journal:  RSC Adv        ISSN： 2046-2069            Impact factor:   3.361


  36 in total

1.  Crystal structure of the conserved core of protein arginine methyltransferase PRMT3.

Authors:  X Zhang; L Zhou; X Cheng
Journal:  EMBO J       Date:  2000-07-17       Impact factor: 11.598

2.  A general synthesis of 5'-azido-5'-deoxy-2',3'-O-isopropylidene nucleosides.

Authors:  F Liu; D J Austin
Journal:  J Org Chem       Date:  2001-12-14       Impact factor: 4.354

3.  Design, synthesis, and characterization of an ATP-peptide conjugate inhibitor of protein kinase A.

Authors:  Aliya C Hines; Philip A Cole
Journal:  Bioorg Med Chem Lett       Date:  2004-06-07       Impact factor: 2.823

4.  Letter: SN2-like transition state for methyl transfer catalyzed by catechol-O-methyl-transferase.

Authors:  M F Hegazi; R T Borchard; R L Schowen
Journal:  J Am Chem Soc       Date:  1976-05-12       Impact factor: 15.419

5.  In situ generation of a bisubstrate analogue for protein arginine methyltransferase 1.

Authors:  Tanesha Osborne; Rachel L Weller Roska; Scott R Rajski; Paul R Thompson
Journal:  J Am Chem Soc       Date:  2008-03-14       Impact factor: 15.419

Review 6.  Targeting epigenetic enzymes for drug discovery.

Authors:  Robert A Copeland; Edward J Olhava; Margaret Porter Scott
Journal:  Curr Opin Chem Biol       Date:  2010-08       Impact factor: 8.822

Review 7.  Bisphenol A as epigenetic modulator: setting the stage for carcinogenesis?

Authors:  Luciana L Ferreira; Renata Couto; Paulo J Oliveira
Journal:  Eur J Clin Invest       Date:  2015-01       Impact factor: 4.686

8.  Kinetic mechanism of protein N-terminal methyltransferase 1.

Authors:  Stacie L Richardson; Yunfei Mao; Gang Zhang; Pahul Hanjra; Darrell L Peterson; Rong Huang
Journal:  J Biol Chem       Date:  2015-03-14       Impact factor: 5.157

9.  Kinetic and catalytic mechanism of HhaI methyltransferase.

Authors:  J C Wu; D V Santi
Journal:  J Biol Chem       Date:  1987-04-05       Impact factor: 5.157

10.  Identification of novel α-n-methylation of CENP-B that regulates its binding to the centromeric DNA.

Authors:  Xiaoxia Dai; Koichiro Otake; Changjun You; Qian Cai; Zi Wang; Hiroshi Masumoto; Yinsheng Wang
Journal:  J Proteome Res       Date:  2013-08-26       Impact factor: 4.466
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  9 in total

1.  Optimization of High-Throughput Methyltransferase Assays for the Discovery of Small Molecule Inhibitors.

Authors:  Guangping Dong; Adam Yasgar; Darrell L Peterson; Alexey Zakharov; Daniel Talley; Ken Chih-Chien Cheng; Ajit Jadhav; Anton Simeonov; Rong Huang
Journal:  ACS Comb Sci       Date:  2020-06-27       Impact factor: 3.784

2.  Probing the Plasticity in the Active Site of Protein N-terminal Methyltransferase 1 Using Bisubstrate Analogues.

Authors:  Dongxing Chen; Cheng Dong; Guangping Dong; Karthik Srinivasan; Jinrong Min; Nicholas Noinaj; Rong Huang
Journal:  J Med Chem       Date:  2020-07-16       Impact factor: 7.446

3.  Discovery of Bisubstrate Inhibitors for Protein N-Terminal Methyltransferase 1.

Authors:  Dongxing Chen; Guangping Dong; Nicholas Noinaj; Rong Huang
Journal:  J Med Chem       Date:  2019-03-27       Impact factor: 7.446

4.  Selective Peptidomimetic Inhibitors of NTMT1/2: Rational Design, Synthesis, Characterization, and Crystallographic Studies.

Authors:  Brianna D Mackie; Dongxing Chen; Guangping Dong; Cheng Dong; Haley Parker; Christine E Schaner Tooley; Nicholas Noinaj; Jinrong Min; Rong Huang
Journal:  J Med Chem       Date:  2020-08-05       Impact factor: 7.446

5.  Select human cancer mutants of NRMT1 alter its catalytic activity and decrease N-terminal trimethylation.

Authors:  Kaitlyn M Shields; John G Tooley; Janusz J Petkowski; Daniel W Wilkey; Nichola C Garbett; Michael L Merchant; Alan Cheng; Christine E Schaner Tooley
Journal:  Protein Sci       Date:  2017-06-11       Impact factor: 6.725

6.  Discovery of a potent and dual-selective bisubstrate inhibitor for protein arginine methyltransferase 4/5.

Authors:  Ayad A Al-Hamashi; Dongxing Chen; Youchao Deng; Guangping Dong; Rong Huang
Journal:  Acta Pharm Sin B       Date:  2020-10-16       Impact factor: 14.903

7.  Structure-based Discovery of Cell-Potent Peptidomimetic Inhibitors for Protein N-Terminal Methyltransferase 1.

Authors:  Dongxing Chen; Guangping Dong; Youchao Deng; Nicholas Noinaj; Rong Huang
Journal:  ACS Med Chem Lett       Date:  2021-03-01       Impact factor: 4.632

Review 8.  Chemical Biology of Protein N-Terminal Methyltransferases.

Authors:  Rong Huang
Journal:  Chembiochem       Date:  2019-02-13       Impact factor: 3.164

9.  Chemoproteomic Study Uncovers HemK2/KMT9 As a New Target for NTMT1 Bisubstrate Inhibitors.

Authors:  Dongxing Chen; Ying Meng; Dan Yu; Nicholas Noinaj; Xiaodong Cheng; Rong Huang
Journal:  ACS Chem Biol       Date:  2021-06-30       Impact factor: 4.634
  9 in total

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