Sub-Journal of "Nature": Protein degradation therapy attracts attention. At least 15 models are expected to enter the clinic by the end of the year

Although scientists have found that many specific proteins are closely related to human diseases, it is difficult to find small molecules or antibody drugs that can bind to many of these proteins.

Because protein degradation therapy has expanded the range of drug targets, it has become one of the hot technologies that people pay attention to in recent years.

PROTAC, the full name Proteolysis Targeting Chimera, is called a protein targeted degradation chimera.

1.

Arvinas, founded by Professor Craig Crews in 2013, was one of the first companies to enter the field of protein degradation therapy.

Nurix Therapeutics' research product NX-2127 targets B-cell developmental kinase BTK, which is also a proven target.

2.

3.

Through the differential selection of E3 ligase, protein degradation therapy is expected to improve this situation.

4.

The protein degradation therapy CC-92480 developed by Bristol-Myers Squibb is derived from lenalidomide, an approved therapy for the treatment of multiple myeloma (MM).

In addition, in addition to the verified targets (such as IKZF1/3), molecular glues are also being developed to target new targets, such as Helios (IKZF2), GSPT1.

Reference materials:

[1] Targeted protein degraders crowd into the clinic.
Retrieved Mar 22, 2021, from