Remove Engineering Remove Regulations Remove Small Molecule
article thumbnail

Chimeric deubiquitinase engineering reveals structural basis for specific inhibition of the mitophagy regulator USP30

Covalent Modifiers

Nafizul Haque Kazi, Nikolas Klink, Kai Gallant, Gian-Marvin Kipka & Malte Gersch Nat Struct Mol Biol , 2025 [link] The mitochondrial deubiquitinase ubiquitin-specific protease (USP) 30 negatively regulates PINK1parkin-driven mitophagy. However, the molecular basis for specific inhibition of USP30 by small molecules has remained elusive.

article thumbnail

Site-Specific Molecular Glues for the 14-3-3/Tau pS214 ProteinProtein Interaction via Reversible Covalent Imine Tethering

Covalent Modifiers

DOI Ansgar Oberheide, Maxime van den Oetelaar, Jakob Scheele, Jan Borggrfe, Semmy Engelen, Michael Sattler, Christian Ottmann, Peter Cossar and Luc Brunsveld RSC Med Chem 2025 [link] Protein-protein interactions (PPIs) are key regulators of various cellular processes.

Insiders

Sign Up for our Newsletter

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

article thumbnail

How GPCR agonists, including antibodies, are shaping the future of metabolic care

Drug Target Review

G protein-coupled receptors (GPCRs) represent a cornerstone of modern drug discovery due to their crucial role in regulating human physiology and their involvement in numerous diseases. Cedric has a PhD in bioscience engineering from KU Leuven (Belgium).

article thumbnail

SRC-3: CoRegen’s revolutionary approach to cancer

Drug Target Review

This master regulator of the regulatory T cell (Treg) genome has opened new horizons in the fight against cancer, offering a precise and tailored solution to modulate the immune system’s response. Our team has created proprietary techniques to engineer Tregs that specifically remove SRC-3 that is expressed in the nucleus.

article thumbnail

Scientists generate new targeted protein degradation system that tunes a cell’s own proteins

Broad Institute

In one approach, they mark targeted proteins with “destroy me” tags that work with small molecules known as molecular glues to prompt the cell’s own protein-clearing machinery to gobble up the proteins. Continuous evolution of compact protein degradation tags regulated by selective cereblon molecular glues. March 14, 2024.

article thumbnail

Leveraging agonist antibodies to address immunological diseases

Drug Target Review

Agonist antibodies of immune checkpoint regulators These represent a groundbreaking class of immunotherapeutic agents that mimic the natural function of endogenous ligands by binding to specific cell-surface receptors. This approach augments the strength of achieving immune homeostasis.

Disease 52
article thumbnail

Condensate biology: advancing drug discovery for complex diseases

Drug Target Review

They found that although the targets themselves may not be easily druggable due to their disordered nature, their ability to condense can be modulated using small molecules. By focusing on molecules that modulate the condensate formation, they identified tractable chemical matter that specifically impacted the target of interest.

Disease 98