00:38 , Aug 9, 2018 |  BC Innovations  |  Translation in Brief

Identifying the ubiquitinators

A team at University of Dundee and Newcastle University has developed a mass spectrometry-based screening platform to identify ubiquitin ligases and compounds that modulate them. The approach uses the uptake of ubiquitin by enzymes rather...
21:35 , Aug 3, 2018 |  BC Extra  |  Preclinical News

Mechanism identified behind thalidomide-induced birth defects

Researchers at Dana-Farber Cancer Institute uncovered the mechanistic pathway by which thalidomide and two related analogs cause severe fetal harm, answering a long-held question about the three teratogenic drugs now used as cancer therapies. The insight...
22:15 , May 11, 2018 |  BC Extra  |  Preclinical News

Inhibiting the ubiquitin ligase RNF5 to treat CF

In a paper published in Cell Chemical Biology, Italian researchers identified a pharmacological inhibitor of ring finger protein 5 (RNF5) that prevented the premature degradation of mutant F508del cystic fibrosis transmembrane conductance regulator (CFTR) protein,...
11:12 , Apr 24, 2018 |  BioCentury  |  Finance

Protein player

By modulating targets upstream of the ubiquitin proteasome system and inducing both stabilization and destabilization of target proteins, Third Rock Ventures believes newco Cedilla Therapeutics Inc. could have a broader reach than competing protein degradation...
18:24 , Apr 19, 2018 |  BC Extra  |  Preclinical News

Increased ubiquitination of EZH2 or ALK for cancer therapies

Papers published in Cell Reports and Journal of Medicinal Chemistry suggest that targeted degradation by increasing ubiquitination of proteins that promote cancer could be a more complete strategy to treat cancer than catalytic inhibition. As increased...
03:45 , Apr 13, 2018 |  BC Innovations  |  Targets & Mechanisms

Meeting the burden

A major theme at this year’s AACR is the abundance of preclinical discovery driven by molecular signatures in patient samples, suggesting the research community is heeding the call for studies better grounded in human data,...
16:04 , Mar 26, 2018 |  BC Extra  |  Preclinical News

Bradner, Gray explore targeted degradation-based model systems

C4 Therapeutics Inc. co-founders James Bradner and Nathanael Gray published a paper in Nature Chemical Biology demonstrating a generalizable target-specific protein degradation system that can be used to create preclinical models that offer better control...
16:01 , Mar 26, 2018 |  BC Innovations  |  Translation in Brief

Tagging out

C4 Therapeutics Inc. co-founders James Bradner and Nathanael Gray have demonstrated in a paper published in Nature Chemical Biology that targeted protein degradation can be used to create preclinical models that offer better control over...
01:44 , Feb 2, 2018 |  BC Innovations  |  Translation in Brief

Ubiquitin choke point

Takeda has shown its first-in-class UBA1 inhibitor could safely treat cancer by blocking a protein on which virtually all cells depend for ubiquitin-mediated protein degradation, upending conventional wisdom about how to disrupt the pathway that...
19:03 , Nov 27, 2017 |  BC Innovations  |  Distillery Therapeutics

Autoimmune disease; musculoskeletal; neurology; renal

INDICATION: Multiple sclerosis (MS); tissue damage; ataxia; renal In vitro and cell culture studies identified a UBE2M-derived peptide inhibitor of the DCUND1-UBE2M interaction that could help treat NFE2L2-deficient diseases such MS, tissue damage, Friedreich’s ataxia and...