Discovery of a New-Generation S-Adenosylmethionine-Noncompetitive Covalent Inhibitor Targeting the Lysine Methyltransferase Enhancer of Zeste Homologue 2.

S-Adenosylmethionine / pharmacology Lysine Enhancer of Zeste Homolog 2 Protein Polycomb Repressive Complex 2 Cell Proliferation Cell Line, Tumor

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:
08 06 2023
Historique:
medline: 9 6 2023
pubmed: 19 5 2023
entrez: 19 5 2023
Statut: ppublish

Résumé

The first-generation enhancer of zeste homologue 2 (EZH2) inhibitors suffer from several limitations, such as high dosage, cofactor S-adenosylmethionine (SAM) competition, and acquired drug resistance. Development of covalent EZH2 inhibitors that are noncompetitive with cofactor SAM offers an opportunity to overcome these disadvantages. The structure-based design of compound

Identifiants

DOI: 10.1021/acs.jmedchem.3c00504 PMID: 37203326
pubmed: 37203326
doi: 10.1021/acs.jmedchem.3c00504
doi:

Substances chimiques

S-Adenosylmethionine 7LP2MPO46S
Lysine K3Z4F929H6
Enhancer of Zeste Homolog 2 Protein EC 2.1.1.43
Polycomb Repressive Complex 2 EC 2.1.1.43

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

7629-7644

Auteurs

Yi Zhang (Y)

Balance-Based Drug Discovery Laboratory, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510006, China.

Hong Yang (H)

Lingang Laboratory, Shanghai 200031, China.
Division of Antitumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai 201203, China.

Bingbing Li (B)

Balance-Based Drug Discovery Laboratory, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510006, China.

Jiayi Li (J)

University of Chinese Academy of Sciences, Beijing 100049, China.
School of Pharmaceutical Science and Technology, Hangzhou Institute for Advanced Study, University of Chinese Academy of Sciences, Hangzhou 310024, China.

Huaxuan Li (H)

Balance-Based Drug Discovery Laboratory, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510006, China.

Qiongyu Shi (Q)

Lingang Laboratory, Shanghai 200031, China.

Bang Li (B)

Balance-Based Drug Discovery Laboratory, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510006, China.

Zekun Wang (Z)

Division of Antitumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai 201203, China.
University of Chinese Academy of Sciences, Beijing 100049, China.

Jiahong Zheng (J)

Balance-Based Drug Discovery Laboratory, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510006, China.

Ying Zhang (Y)

Lingang Laboratory, Shanghai 200031, China.
University of Chinese Academy of Sciences, Beijing 100049, China.
School of Life Science and Technology, ShanghaiTech University, Shanghai 201210, China.

Hui Dong (H)

Balance-Based Drug Discovery Laboratory, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510006, China.

Xun Huang (X)

Lingang Laboratory, Shanghai 200031, China.
University of Chinese Academy of Sciences, Beijing 100049, China.
School of Pharmaceutical Science and Technology, Hangzhou Institute for Advanced Study, University of Chinese Academy of Sciences, Hangzhou 310024, China.

Yuanxiang Wang (Y)

Balance-Based Drug Discovery Laboratory, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510006, China.
ORCID: 0000-0001-5650-4396

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Classifications MeSH

questionsmedicales.fr › Acides nucléiques, nucléotides et nucléosides › Nucléosides › Ribonucléosides › Adénosine › Adémétionine › Discovery of a New-Generation...
questionsmedicales.fr › Acides aminés, peptides et protéines › Acides aminés › Acides aminés essentiels › Lysine › Discovery of a New-Generation...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Facteurs de transcription › Protéines de répression › Protéines du groupe Polycomb › Complexe répresseur Polycomb-2 › Protéine-2 homologue de l'activateur de Zeste › Discovery of a New-Generation...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Facteurs de transcription › Protéines de répression › Protéines du groupe Polycomb › Complexe répresseur Polycomb-2 › Discovery of a New-Generation...
questionsmedicales.fr › Phénomènes physiologiques › Croissance et développement › Croissance › Processus de croissance cellulaire › Prolifération cellulaire › Discovery of a New-Generation...
questionsmedicales.fr › Cellules › Cellules cultivées › Cellules cancéreuses en culture › Lignée cellulaire tumorale › Discovery of a New-Generation...