Remove DNA Remove Regulations Remove Small Molecule
article thumbnail

Chemoproteomics Identifies State-Dependent and Proteoform-Selective Caspase-2 Inhibitors

Covalent Modifiers

3c12240 Caspases are a highly conserved family of cysteine-aspartyl proteases known for their essential roles in regulating apoptosis, inflammation, cell differentiation, and proliferation. Complementary to genetic approaches, small-molecule probes have emerged as useful tools for modulating caspase activity.

article thumbnail

A phenotypic screen with Trypanosoma brucei for discovering small molecules that target the SLiM?binding pocket of proliferating cell nuclear antigen orthologs

Chemical Biology and Drug Design

Abstract Proliferating cell nuclear antigen (PCNA) is a homo-trimeric protein complex that clamps around DNA to tether DNA polymerases to the template during replication and serves as a hub for many other interacting proteins. The assay design is to discover bioactive small molecules that restore proliferation in T. brucei

Insiders

Sign Up for our Newsletter

This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.

article thumbnail

Profiling nuclear cysteine ligandability and effects on nuclear localization using proximity labeling-coupled chemoproteomics

Covalent Modifiers

Covalent ligands are a promising strategy to pharmacologically target nuclear proteins, such as transcription factors, which lack ordered small-molecule binding pockets. To identify nuclear cysteines that are susceptible to covalent liganding, we couple proximity labeling (PL), using a histone H3.3-TurboID

article thumbnail

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. Multifunctional Small Molecules and Peptides Beyond PROTACs, there are other exciting tools in the new drug discovery toolbox.

article thumbnail

A Look Back

Dark Matter Blog

As soon as I learned about DNA and RNA, I wanted to be a molecular biologist. Last stops at RNA My last roles in biotech were where my original passion began: DNA and RNA. My last stop at Arrakis Therapeutics is with a company targeting RNA with small molecules. I wanted to use molecular biology to create drugs.

article thumbnail

ATUZAGINSTAT

New Drug Approvals

link] 01 Aug 2022 Cortexyme is now called Quince Therapeutics You need to be a logged in or subscribed to view this content This small molecule is an orally available protease inhibitor targeting the lysine proteases of the periodontal pathogen Porphyromonas gingivalis. gingivalis DNA fragments in their CSF at baseline.

article thumbnail

What Took So Long: How Tech Has Finally Caught Up With Transcription Factors

LifeSciVC

These hair clip-like molecules clamp onto DNA, thereby turning many genes on and off. That can be a good thing: for example, when determining inherited traits and regulating critical cell functions. Or a bad thing: for example, when increased expression of certain genes contributes to the formation of cancer.