Chemical evolution for taming the 'pathogenic kinase' PAK1.
Drug Discov Today
; 25(6): 959-964, 2020 06.
Article
in English
| MEDLINE | ID: covidwho-828446
ABSTRACT
To celebrate the 25th anniversary of the cloning of the first mammalian p21-activated kinases (PAKs) (RAC/CDC42-activated kinases) by Ed Manser, the first international PAK symposium was held in NYC in October 2019. Among six distinct PAKs in mammals, PAK1 is the major 'pathogenic kinase', the abnormal activation of which is responsible for a wide variety of diseases and disorders including cancers, ageing processes and infectious and inflammatory diseases such as pandemic coronaviral infection. Recently, for a clinical application, a few potent (highly cell-permeable and water-soluble) PAK1 blockers have been developed from natural or synthetic PAK1 blockers (triptolide, vitamin D3 and ketorolac) via a series of 'chemical evolutions' that boost pharmacological activities >500 times.
Full text:
Available
Collection:
International databases
Database:
MEDLINE
Main subject:
P21-Activated Kinases
Type of study:
Prognostic study
Limits:
Animals
/
Humans
Language:
English
Journal:
Drug Discov Today
Journal subject:
Pharmacology
/
Drug Therapy
Year:
2020
Document Type:
Article
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