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

Crystallography, X-Ray Methylation Methyltransferases / antagonists & inhibitors Protein Conformation Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization Substrate Specificity

Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
11 04 2019
Historique:
pubmed: 19 3 2019
medline: 15 9 2020
entrez: 19 3 2019
Statut: ppublish

Résumé

Protein N-terminal methyltransferase 1 (NTMT1) plays an important role in regulating mitosis and DNA repair. Here, we describe the discovery of a potent NTMT1 bisubstrate inhibitor 4 (IC

Identifiants

DOI: 10.1021/acs.jmedchem.9b00206 PMID: 30883119 PMC: PMC6760264
pubmed: 30883119
doi: 10.1021/acs.jmedchem.9b00206
pmc: PMC6760264
mid: NIHMS1050998
doi:

Substances chimiques

Methyltransferases EC 2.1.1.-
NTMT1 protein, human EC 2.1.1.-

Types de publication

Journal Article Research Support, N.I.H., Extramural Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

3773-3779

Subventions

Organisme : NCI NIH HHS
ID : P30 CA023168
Pays : United States
Organisme : NIAID NIH HHS
ID : K22 AI113078
Pays : United States
Organisme : NIAID NIH HHS
ID : R01 AI127793
Pays : United States
Organisme : NIGMS NIH HHS
ID : R01 GM117275
Pays : United States
Organisme : NIGMS NIH HHS
ID : R01 GM127896
Pays : United States

Références

Chembiochem. 2019 Apr 15;20(8):976-984
pubmed: 30479015
J Med Chem. 2018 Feb 22;61(4):1541-1551
pubmed: 29320176
J Mol Biol. 1977 Apr;111(2):173-81
pubmed: 323502
Proc Natl Acad Sci U S A. 2013 May 28;110(22):8870-5
pubmed: 23671120
Nat Commun. 2017 Mar 07;8:14678
pubmed: 28266506
J Biol Chem. 2014 Jun 6;289(23):16046-56
pubmed: 24753253
Nat Cell Biol. 2007 May;9(5):596-603
pubmed: 17435751
J Proteome Res. 2015 Jun 5;14(6):2575-82
pubmed: 25886813
Nat Commun. 2015 Jul 22;6:7821
pubmed: 26199140
J Proteome Res. 2013 Sep 6;12(9):4167-75
pubmed: 23978223
Neuron. 2015 Jan 7;85(1):88-100
pubmed: 25569348
Oncotarget. 2015 May 20;6(14):12248-63
pubmed: 25909287
RSC Adv. 2016;6(8):6768-6771
pubmed: 27588169
Biochemistry. 2010 Jun 29;49(25):5225-35
pubmed: 20481588
FEBS Lett. 1982 Jul 19;144(1):11-5
pubmed: 7106295
Genes Dev. 2015 Nov 15;29(22):2343-8
pubmed: 26543161
Mech Ageing Dev. 2015 Mar;146-148:42-52
pubmed: 25843235
J Biochem. 1982 Nov;92(5):1675-8
pubmed: 6818230
Bioorg Med Chem. 2010 Dec 1;18(23):8158-66
pubmed: 21036620
Genes Dev. 2015 Nov 15;29(22):2337-42
pubmed: 26543159
J Biol Chem. 2015 May 1;290(18):11601-10
pubmed: 25771539
Org Biomol Chem. 2017 Aug 9;15(31):6656-6667
pubmed: 28758655
BMC Cell Biol. 2010 Jun 21;11:43
pubmed: 20565941
J Cell Biol. 2008 Sep 8;182(5):827-36
pubmed: 18762580
Org Biomol Chem. 2015 Apr 14;13(14):4149-54
pubmed: 25712161
Nature. 2010 Aug 26;466(7310):1125-8
pubmed: 20668449
Anal Biochem. 2005 Jul 1;342(1):86-92
pubmed: 15958184
Anal Biochem. 2015 Jun 1;478:59-64
pubmed: 25778392

Auteurs

Dongxing Chen (D)

Department of Medicinal Chemistry and Molecular Pharmacology, Center for Cancer Research, Institute for Drug Discovery , Purdue University , West Lafayette , Indiana 47907 , United States.

Guangping Dong (G)

Department of Medicinal Chemistry and Molecular Pharmacology, Center for Cancer Research, Institute for Drug Discovery , Purdue University , West Lafayette , Indiana 47907 , United States.

Nicholas Noinaj (N)

Markey Center for Structural Biology, Department of Biological Sciences and the Purdue Institute of Inflammation, Immunology and Infectious Disease , Purdue University , West Lafayette , Indiana 47907 , United States.

Rong Huang (R)

Department of Medicinal Chemistry and Molecular Pharmacology, Center for Cancer Research, Institute for Drug Discovery , Purdue University , West Lafayette , Indiana 47907 , United States.
ORCID: 0000-0002-1477-3165

Articles similaires

Polyphasic identification of Vibrio species from aquatic sources using mass spectrometry, housekeeping gene sequencing and whole genome analysis.

Anna Luiza Bauer Canellas, Adriana Rocha Faria, Gabriel Rodrigues Dias et al.
1.00
Vibrio Whole Genome Sequencing Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization Genome, Bacterial Water Microbiology

Mutational analysis of Phanerochaete chrysosporium´s purine transporter.

Mariana Barraco-Vega, Manuel Sanguinetti, Gabriela da Rosa et al.
1.00
Phanerochaete Fungal Proteins Purines Aspergillus nidulans DNA Mutational Analysis

Structural basis for molecular assembly of fucoxanthin chlorophyll

Koji Kato, Yoshiki Nakajima, Jian Xing et al.
1.00
Diatoms Photosystem I Protein Complex Chlorophyll Binding Proteins Cryoelectron Microscopy Light-Harvesting Protein Complexes

RNA methylation patterns of tumor microenvironment cells regulate prognosis and immunotherapeutic responsiveness in patients with triple-negative breast cancer.

Tingjun Li, Yiqin Huang, Shien Cui et al.
1.00
Triple Negative Breast Neoplasms Tumor Microenvironment Humans Prognosis Female

Classifications MeSH

questionsmedicales.fr › Techniques d'investigation › Techniques de chimie analytique › Cristallographie aux rayons X › Discovery of Bisubstrate Inhibitors for...
questionsmedicales.fr › Métabolisme › Alkylation › Méthylation › Discovery of Bisubstrate Inhibitors for...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Transferases › One-carbon group transferases › Methyltransferases › Discovery of Bisubstrate Inhibitors for...
questionsmedicales.fr › Phénomènes chimiques › Phénomènes biochimiques › Conformation moléculaire › Conformation des protéines › Discovery of Bisubstrate Inhibitors for...
questionsmedicales.fr › Techniques d'investigation › Techniques de chimie analytique › Spectrométrie de masse › Spectrométrie de masse MALDI › Discovery of Bisubstrate Inhibitors for...
questionsmedicales.fr › Phénomènes chimiques › Phénomènes biochimiques › Spécificité du substrat › Discovery of Bisubstrate Inhibitors for...