70 hasil untuk "Basappa Basappa"
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Artikel Jurnal Teks lengkap
Reply to: “The non-cytotoxic small molecule NPB does not inhibit BAD phosphorylation and forms colloidal aggregates”
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Synthesis, Computational Studies, and Anti-Tuberculosis Activity of Benzoxazines That Act as RAGE Inhibitors
Novel benzoxazines were synthesized by microwave irradiation and tested for their potential binding affinity towards receptors of advanced glycation end products (RAGE). We found that the compound (2-(2-bromophenyl)-6-methyl-2,4-dihydro-1H-benzo[d][1,3]oxazine) (3i) is a lead inhibitor of RAGE…
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A review on antifungal activities of benzoxazoles against Candida Albicans and SAR studies
Abstract Millions of people are dying due to fungal infections annually across the globe. About 70% of the fungal infections are due to Candida Albicans in the world with mortality rate around 40%. This fungus has the ability to develop resistance upon prolonged exposure to antifungal drugs. To…
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TFF3 facilitates dormancy of anti-estrogen treated ER+ mammary carcinoma
BACKGROUND: Tumor dormancy is a substantial clinical obstacle in treatment of estrogen receptor positive mammary carcinoma (ER+MC), contributing to drug resistance, metastatic outgrowth, relapse, and consequent mortality. METHODS: Preclinical models mimicking clinical anti-estrogen-induced ER+MC…
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Cyclization of Activated Methylene Isocyanides with Methyl N(N),N′-Di(tri)substituted Carbamimidothioate: A Novel Entry for the Synthesis of N,1-Aryl-4-tosyl/ethoxycarbonyl-1H-imidazol-5-amines
Abstract Base-induced cyclization of active methylene isocyanides with carbamimidothioates for the synthesis of N,1-aryl-4-tosyl/ethylcarboxy-1H-imidazol-5-amines is reported. The diversity of the reactions is exemplified by using various carbamimidothioates obtained from symmetrical…
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Novel Biphenyl Amines Inhibit Oestrogen Receptor (ER)-α in ER-Positive Mammary Carcinoma Cells
Herein, the activity of adamantanyl-tethered-biphenyl amines (ATBAs) as oestrogen receptor alpha (ERα) modulating ligands is reported. Using an ERα competitor assay it was demonstrated that ATBA compound 3-(adamantan-1-yl)-4-methoxy-N-(4-(trifluoromethyl) phenyl) aniline (AMTA) exhibited an…
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Inhibition of TFF3 synergizes with c-MET inhibitors to decrease the CSC-like phenotype and metastatic burden in ER+HER2+ mammary carcinoma
The interaction between HER2 and ERα signaling pathways contributes to resistance to anti-estrogen and HER2-targeted therapies, presenting substantial treatment challenges in ER-positive (ER+) HER2-positive (HER2+) mammary carcinoma (MC). Trefoil Factor-3 (TFF3) has been reported to mediate…
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Inhibition of BAD-Ser99 phosphorylation synergizes with PARP inhibition to ablate PTEN-deficient endometrial carcinoma
Loss of phosphatase and tensin homolog (PTEN) impairs DNA double-strand repair and confers sensitivity to poly (ADP-ribose) polymerase inhibitors (PARPis). However, PARPis also hyperactivate the MAPK and PI3K/AKT/mTOR pathways in PTEN-deficient endometrial carcinoma (EC), which allows the emergence…
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Combining Mitomycin C with inhibition of BAD phosphorylation enhances apoptotic cell death in advanced cervical cancer
OBJECTIVE: Mitomycin C (MMC), a DNA-damaging chemotherapeutic, is commonly used clinically for recurrent cervical carcinoma (CC), either alone or in combination. MMC generates DNA damage resulting in CC cell death yet also induces increased AKT-BAD phosphorylation associated with drug resistance…
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Thiouracil and triazole conjugate induces autophagy through the downregulation of Wnt/β‐catenin signaling pathway in human breast cancer cells
Autophagy is vital for maintaining cellular homeostasis by breaking down unnecessary organelles and proteins within cells. Its activity varies abnormally in several diseases, including cancer, making it a potential target for therapeutic strategies. The Wnt/β‐catenin signaling pathway significantly…
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New Heparanase-Inhibiting Triazolo-Thiadiazoles Attenuate Primary Tumor Growth and Metastasis
SIMPLE SUMMARY: Heparanase is an endoglycosidase that plays a critical role in tumor progression and metastasis. The expression of heparanase in the tumor microenvironment is positively correlated with the aggressiveness of the tumor and is associated with poor prognosis. In this study, we have…
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Design and Activity of Novel Oxadiazole Based Compounds That Target Poly(ADP-ribose) Polymerase
Novel PARP inhibitors with selective mode-of-action have been approved for clinical use. Herein, oxadiazole based ligands that are predicted to target PARP-1 have been synthesized and screened for the loss of cell viability in mammary carcinoma cells, wherein seven compounds were observed to…
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Targeting the epigenome and tumor heterogeneity: advances in immunotherapy for chemoresistant metastatic colorectal cancer
Mitochondria are pivotal organelles that regulate oxidative phosphorylation (OXPHOS). Although microsatellite-stable colorectal cancer represents the majority of CRC cases, the functional aspects of mitochondrial DNA copy number alterations in its progression remains poorly explored. The aim of…
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Artikel Jurnal Teks lengkap
Combined inhibition of BADSer99 phosphorylation and PARP ablates models of recurrent ovarian carcinoma
BACKGROUND: Poly (ADP-ribose) polymerase inhibitors (PARPis) have been approved for the treatment of recurrent epithelial ovarian cancer (EOC), regardless of BRCA status or homologous recombination repair deficiency. However, the low response of platinum-resistant EOC, the emergence of resistance…