PROTACs in Treatment of Cancer: A Review.
PROTACs
anticancer
cancer
proteins
target.
ubiquitin
Journal
Mini reviews in medicinal chemistry
ISSN: 1875-5607
Titre abrégé: Mini Rev Med Chem
Pays: Netherlands
ID NLM: 101094212
Informations de publication
Date de publication:
2021
2021
Historique:
received:
25
11
2020
revised:
16
01
2021
accepted:
27
01
2021
pubmed:
27
2
2021
medline:
21
12
2021
entrez:
26
2
2021
Statut:
ppublish
Résumé
Cancer treatment has become a major challenge amidst the resistance and relapse caused by the various treatments available. The PROteolysis TAargeting Chimera (PROTAC) technology involves the degradation of target protein against the inhibition by small drug molecules. The PROTACs with high potency and activity have been frequently reported; however, no PROTAC acting against cancer has reached the clinical trials. The concept of PROTACs involves the reduction in the disease-causing protein by its degradation through the ubiquitin-proteasomal enzyme system. This concept has attracted a lot of attention from both industry and academia due to its potential in drug discovery (in the form of PROTACs), which can conquer the resistance associated with current treatments of cancer. Thus, it is the need of the hour to identify and synthesize more PROTACs for a viable treatment of cancer. This article reviews the design, activity and effects produced in cancer by some recently developed PROTACs.
Identifiants
pubmed: 33634757
pii: MRMC-EPUB-114586
doi: 10.2174/1389557521666210226150740
doi:
Substances chimiques
Proteasome Endopeptidase Complex
EC 3.4.25.1
Types de publication
Journal Article
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
2347-2360Informations de copyright
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