Wiley Online Library : Chemical Biology & Drug Design
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Novel carbamodithioate regulates cellular hypoxia through chemical activation of prolyl hydroxylase‐2 for breast cancer chemoprevention

BBAP-6 was identified as an inducer of PHD-2 and was found to reinstate apoptosis in MCF-7 cells in-vitro as well as in DMBA-induced mammary gland carcinoma in vivo. All in all, according to the current study's findings, BBAP-6 upregulated PHD-2 and, when combined with TPZ, exhibited greater chemopreventive potential. Abstract Inhibition of prolylhydroxylase-2...

Sat May 11, 2024 12:07
Comparison of feline and human immunodeficiency virus reverse transcriptase enzymes through chemical screening and computational analysis

Feline immunodeficiency virus (FIV), is a common infection found in domesticated and wild cats worldwide. We employ a chemo-centric approach to assess the similarity between FIV-RT and HIV1-RT using experimental screening and computational chemistry methods. Through this, we identify more potent inhibitors and gain a better appreciation of FIV-RT...

Fri May 10, 2024 12:18
4,4‐Diallyl curcumin bis(2,2‐hydroxymethyl)propanoate ameliorates nonalcoholic steatohepatitis in methionine‐choline‐deficient diet and Western diet mouse models

4,4-Diallyl curcumin bis(2,2-hydroxymethyl)propanoate, also known as 35e, displayed significant antilipid accumulation and antifibrotic effects in two complementary mice models. Abstract Nonalcoholic steatohepatitis (NASH) is a progressive form of nonalcoholic fatty liver disease (NAFLD) that causes severe liver damage, fibrosis, and scarring....

Fri May 10, 2024 12:18
Glycyrrhizic acid inhibits DNA damage repair and enhances cisplatin‐induced apoptosis of melanoma cells

Our results showed that, compared with GA or CP alone, CP and GA combined treatment significantly inhibited the viability of melanoma cells and promoted cell apoptosis at the cytological level. At the protein level, the expression levels of Caspase3 and Bcl-2 were significantly decreased, and the expression levels of cleaved Caspase3 and γH2AX were...

Fri May 10, 2024 12:18
Structural and molecular insights from dual inhibitors of EGFR and VEGFR2 as a strategy to improve the efficacy of cancer therapy

Simultaneous inhibition of EGFR and VEGFR2 may improve the efficacy of cancer treatment. Understanding the macromolecular structures, activation mechanism, and pharmacophore features of both kinase inhibitors and their selectivity is essential in designing dual inhibitors of EGFR and VEGFR2. Abstract Epidermal growth factor receptor (EGFR) and...

Fri May 3, 2024 12:02
Recombinant hirudin suppresses angiogenesis of diffuse large B‐cell lymphoma through regulation of the PAR‐1‐VEGF

PAR-1 with VEGF interaction, PAR-1 promoted proliferation, migration, and angiogenesis of EA.hy926 or Diffuse large B-cell lymphoma (DLBCL) cells through up-regulation VEGF. While Recombinant hirudin (RH) inhibited that effect. In vivo, RH inhibited tumor growth and angiogenesis of DLBCL mice by down-regulation PAR-1-VEGF. Abstract Hirudin is...

Tue Apr 30, 2024 11:54

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