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Discovery of small molecule c?Maf inhibitors using molecular docking?based virtual screening, molecular dynamics simulation, and biological evaluation

Chemical Biology and Drug Design

Sorafenib and glimepiride simultaneously downregulated c-Maf protein expression to induce G1 phase arrest and apoptosis in myeloma cells. Moreover, both compounds simultaneously downregulated c-Maf protein expression to induce G1 phase arrest and apoptosis in myeloma cells.

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Multifaceted approach toward mapping out the anticancer properties of small molecules via in vitro evaluation on melanoma and nonmelanoma skin cancer cells, and in silico target fishing

Chemical Biology and Drug Design

μM), significantly and dose-dependently induced apoptosis of SCC-12 and SK-MEL-28 cells, as evidenced by the suppression of Bcl-2 and upregulation of Bax, cleaved caspase-3, caspase-9, and PARP protein expression levels. The most active compounds 11 (A431: IC 50  = 5.0 μM, μM, SCC-12: IC 50  = 2.9 μM, μM, SKMEL-28: IC 50  = 4.9 μM,

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The Future of Drug Discovery: Tackling the Undruggable with New Biotechnologies

DrugBank

These multifunctional small molecules are like tiny spies, hijacking the body’s natural protein degradation system to remove unwanted proteins. Similarly, PROTACs can target and degrade overexpressed proteins, offering a way to overcome drug resistance, a common issue in cancer treatment.

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SRC-3: CoRegen’s revolutionary approach to cancer

Drug Target Review

Focusing on SRC-3 within the nucleus activates a series of changes in protein expression that have a profound impact of enhancing the immune system’s ability to engage and attack cancer cells. By working directly at this level in the Treg, CoRegen can precisely manipulate its cellular activity at its source, the TME.

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Marina Saffold

Broad Institute

Recently published literature has identified three proteins (Lap2β, H3K9me3, and HP1γ) that exhibit decreased expression in aged fibroblasts and a “senescence cocktail” of small molecules that have been observed to reduce the expression of these chromatin proteins in a way that models aged cells.

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CRISPR and single-cell sequencing highlight genetic variants for traits and diseases

Drug Target Review

The researchers then use CRISPR to target each of the regions of the genomes implicated by GWAS and conduct single-cell sequencing to evaluate gene and protein expression. STING-seq works by taking biobank-scale GWAS and looking for likely causal variants using a combination of biochemical hallmarks and regulatory elements.

Disease 52
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Five Promising Treatment Areas in Early-Phase Drug Development in 2024

Alta Sciences

They work by binding to specific sequences of nucleotides present within the mRNA structure and can induce mechanisms that either decrease, restore, or modify protein expression. And since proteins are often linked to disease, there's huge potential to treat a broad range of diseases with this technology.