Second-Generation JK-206 Targets the Oncogenic Signal Mediator RHOA in Gastric Cancer.
JK-206
RHOA
Rhosin
gastric cancer
pharmacogenomics
transcriptomics
Journal
Cancers
ISSN: 2072-6694
Titre abrégé: Cancers (Basel)
Pays: Switzerland
ID NLM: 101526829
Informations de publication
Date de publication:
22 Mar 2022
22 Mar 2022
Historique:
received:
28
02
2022
revised:
14
03
2022
accepted:
20
03
2022
entrez:
12
4
2022
pubmed:
13
4
2022
medline:
13
4
2022
Statut:
epublish
Résumé
Ras homologous A (RHOA), a signal mediator and a GTPase, is known to be associated with the progression of gastric cancer (GC), which is the fourth most common cause of death in the world. Previously, we designed pharmacologically optimized inhibitors against RHOA, including JK-136 and JK-139. Based on this previous work, we performed lead optimization and designed novel RHOA inhibitors for greater anti-GC potency. Two of these compounds, JK-206 and JK-312, could successfully inhibit the viability and migration of GC cell lines. Furthermore, using transcriptomic analysis of GC cells treated with JK-206, we revealed that the inhibition of RHOA might be associated with the inhibition of the mitogenic pathway. Therefore, JK-206 treatment for RHOA inhibition may be a new therapeutic strategy for regulating GC proliferation and migration.
Identifiants
pubmed: 35406376
pii: cancers14071604
doi: 10.3390/cancers14071604
pmc: PMC8997135
pii:
doi:
Types de publication
Journal Article
Langues
eng
Subventions
Organisme : Gachon University Gil Medical Center
ID : FRD2019-11-02 (2)
Organisme : National Research Foundation of Korea
ID : NRF-2020R1F1A1069206
Organisme : National Research Foundation of Korea
ID : NRF-2020R1I1A1A0106589212
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