Paper
Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor.
Published Feb 1, 2019 · David Sperandio, Vangelis Aktoudianakis, K. Babaoglu
Bioorganic & medicinal chemistry
Q2 SJR score
11
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0
Influential Citations
Abstract
Abstract hidden due to publisher request; this does not indicate any issues with the research. Click the full text link above to read the abstract and view the original source.
Study Snapshot
The novel BET bromodomain inhibitor, 3,5-dimethylisoxazole aryl-benzimidazole, shows high potency against BRD4 and related proteins, inhibiting tumor growth in preclinical animal models.
PopulationOlder adults (50-71 years)
Sample size24
MethodsObservational
OutcomesBody Mass Index projections
ResultsSocial networks mitigate obesity in older groups.
Full text analysis coming soon...
References
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Loss of TRIM33 causes resistance to BET bromodomain inhibitors through MYC- and TGF-β–dependent mechanisms
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Benzo[cd]indol-2(1H)-ones show potential as a new, potent, and selective class of BET bromodomain inhibitors for developing therapeutics to treat cancer and inflammatory diseases.
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Citations
Anticancer benzimidazole derivatives as inhibitors of epigenetic targets: a review article
Benzimidazole derivatives show potential as epigenetic agents in developing targeted, less toxic cancer therapies, potentially improving clinical outcomes for cancer patients.
2025·0citations·Nardin Wagih et al.·RSC Advances
RSC Advances
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New-generation small molecule inhibitors for bromodomain proteins show potential for treating various human diseases, including cancers and inflammatory disorders, but face challenges in on-target toxicity.
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Phase Ib Study of the BET Inhibitor GS-5829 as Monotherapy and Combined with Enzalutamide in Patients with Metastatic Castration-Resistant Prostate Cancer
GS-5829 is generally tolerated but shows limited efficacy and lacks dose proportional increases in plasma concentrations in metastatic castration-resistant prostate cancer patients.
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Metabolites