Polyisoprenylated Cysteinyl Amide Inhibitors: A Novel Approach to Controlling Cancers with Hyperactive Growth Signaling.
G-proteins
K-Ras
Polyisoprenylated Cysteinyl Amide Inhibitors (PCAIs)
Polyisoprenylated methylated protein
methyl esterase (PMPMEase)
RhoA
fascin
isoprenylation
polyisoprenylation
vinculin
Journal
Current medicinal chemistry
ISSN: 1875-533X
Titre abrégé: Curr Med Chem
Pays: United Arab Emirates
ID NLM: 9440157
Informations de publication
Date de publication:
2021
2021
Historique:
received:
23
05
2020
revised:
18
09
2020
accepted:
25
09
2020
pubmed:
13
11
2020
medline:
23
6
2021
entrez:
12
11
2020
Statut:
ppublish
Résumé
Aberrant activation of monomeric G-protein signaling pathways drives some of the most aggressive cancers. Suppressing these hyperactivities has been the focus of efforts to obtain targeted therapies. Polyisoprenylated methylated protein methyl esterase (PMPMEase) is overexpressed in various cancers. Its inhibition induces the death of cancer cells that harbor the constitutively active K-Ras proteins. Furthermore, the viability of cancer cells driven by factors upstream of K-Ras, such as overexpressed growth factors and their receptors or the mutationally-activated receptors, is also susceptible to PMPMEase inhibition. Polyisoprenylated cysteinyl amide inhibitors (PCAIs) were thus designed to target cancers with hyperactive signaling pathways involving the G-proteins. The PCAIs were, however, poor inhibitors of PMPMEase, with K
Identifiants
pubmed: 33176634
pii: CMC-EPUB-111393
doi: 10.2174/0929867327666201111140825
pmc: PMC9175089
doi:
Substances chimiques
Amides
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
3476-3489Subventions
Organisme : NIMHD NIH HHS
ID : G12 MD007582
Pays : United States
Organisme : NCI NIH HHS
ID : SC1 CA190505
Pays : United States
Organisme : NIMHD NIH HHS
ID : U54 MD007582
Pays : United States
Organisme : National Institute of General Medical Sciences (NIGMS)
ID : SC1CA190505
Informations de copyright
Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.
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