Some of the most important targets in cancer, including KRAS and MYC, have thwarted the best efforts of drug developers for decades because their active sites are not amenable to targeting with small ...
Cancer therapies sometimes involve drugs that mediate the breakdown of specific intracellular proteins that participate in cancer formation and proliferation. Proteolysis-targeting chimeras or PROTACs ...
University of Pittsburgh School of Medicine scientists have developed drug candidates that early tests suggest could reverse HIV’s ability to escape detection by the immune system. The team’s research ...
In a recent study, scientists created a chemical that breaks down expanded huntingtin HTT clumps in HD cells and mouse models. This chemical finds HTT clumps and targets them to be broken down or ...
Cancer therapies sometimes involve drugs that mediate the breakdown of specific intracellular proteins that participate in cancer formation and proliferation. Proteolysis-targeting chimeras or PROTACs ...
PROTAC activates the cell's own protein disposal system. Credit: MPI of Molecular Physiology Most diseases are caused by proteins that have spun out of control. Unfortunately, so far, conventional ...
Proteolysis targeting chimeras (PROTACs) are bivalent molecules that simultaneously bind to a chosen protein and E3 ubiquitin ligase, leading to the target protein’s degradation through the proteasome ...
Undruggable targets typically refer to a class of therapeutic targets that are difficult to target through conventional methods or have not yet been targeted, but are of great clinical significance.
Researchers have developed an improved type of PROTAC that has enhanced intracellular accumulation and functions, not only as a degrader, but also as an inhibitor of the target protein. Cancer ...