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Structure based discovery of clomifene as a potent inhibitor of cancer-associated mutant IDH1
Clomifene may have clinical potential in tumor therapies as a safe and effective inhibitor of mutant IDH1 by virtual screening method and in vivo studies indicated that clomifenes significantly suppressed the tumor growth of HT1080-bearing CB-17/Icr-scid mice.
Triterpenoids from Ganoderma lucidum and Their Potential Anti-inflammatory Effects.
- Yanli Wu, Fei Han, +4 authors Lixia Chen
- Medicine, BiologyJournal of agricultural and food chemistry
- 17 April 2019
Compound 4 exhibited the most potent inhibition on nitric oxide production induced by lipopolysaccharide (LPS) in RAW264, and could be used as a potential anti-inflammatory candidate and the total triterpenoids might be developed as value-added functional food for the prevention of inflammation.
Proton pump inhibitor ilaprazole suppresses cancer growth by targeting T-cell-originated protein kinase
The results suggested that ilaprazole inhibited the cancer growth by targeting TOPK both in vitro and in vivo.
A natural inhibitor of kidney-type glutaminase: a withanolide from Physalis pubescens with potent anti-tumor activity
Interestingly, physapubescin K could reverse the resistance of HCC827-ER cells to erlotinib and synergize with the hexokinase 2 inhibitor to markedly enhance the inhibition of SW1990 cell proliferation.
Aspulvinone O, a natural inhibitor of GOT1 suppresses pancreatic ductal adenocarcinoma cells growth by interfering glutamine metabolism
- Weiguang Sun, Shanshan Luan, +4 authors Yonghui Zhang
- Medicine, ChemistryCell Communication and Signaling
- 30 August 2019
Screening of an in-house natural compound library identified the AO as a novel inhibitor of GOT1 and repressed glutamine metabolism, which sensitizes PDAC cells to oxidative stress and suppresses cell proliferation in vitro and in vivo.
Adapalene inhibits ovarian cancer ES-2 cells growth by targeting glutamic-oxaloacetic transaminase 1.
The data strongly suggest Adapalene, as a GOT1 inhibitor, could be regarded as a potential drug candidate for ovarian cancer therapy.