New Type of Drug Can Target All Disease-causing Proteins
News Jun 15, 2015
The new type of drug, called Proteolysis Targeting Chimeras (PROTACs), also can continue to destroy mutant proteins in mouse tumors.
“This new drug modality culminates a decade of work in the field by my lab,” said Craig Crews, the Lewis B. Cullman Professor of Molecular, Cellular, and Developmental Biology and senior author of the paper, which was done in collaboration with scientists from GlaxoSmithKline and Arvinas, LLC.
Almost all current drugs are small molecules designed to fit into the folds of disease-causing proteins and inhibit their function. High doses are often needed to ensure that protein function is blocked sufficiently to produce therapeutic results, which in turn can produce harmful side effects.
In contrast, PROTACs engage the cells’ own protein degradation machinery to destroy targeted proteins by tagging them for removal and can do so multiple times, meaning it can work at lower doses, the authors say. This suggests this new type of drug has not only the potential to target proteins that are not currently “pharmaceutically vulnerable” but could do so safely, Crews said.
“This is a game-changer for drug development,” Crews said.
The PROTAC technology is being commercialized by New Haven biotechnology company Arvinas, LLC, which recently signed a $434 million partnership from pharmaceutical giant Merck to further explore the potential of the PROTAC technology.
Crews is scientific founder of Arvinas, LLC and Proteolix, Inc., which developed the next generation multiple myeloma drug Kyprolis® based on work from his lab. The study was funded by the National Institutes of Health and GlaxoSmithKline.
Antimicrobial Found in Toiletries Could be Used Against MalariaNews
Triclosan, an antimicrobial compound used in soap, toothpaste, deodorant and many other products, can inhibit target genes in the malaria parasite during two crucial stages of its lifecycle in humans - the hepatic stage.READ MORE
Pre-Treatment with Targeted Drugs Could Mean Less Breast Cancer Patients Require Radical SurgeryNews
Extensive surgery involving mastectomy and removal of several lymph nodes can be safely avoided for more women with some types of breast cancer, if they receive targeted drugs before surgery, according to research presented at the 11th European Breast Cancer Conference.READ MORE