AR-V7 is the most clinically relevant androgen receptor (AR) splice variant associated with endocrine resistance and poor prognosis in patients with prostate cancer.
As Novartis AG’s approved prostate cancer therapy, Pluvicto (177Lu-PSMA-617), continues on a growth trajectory, the firm signed a licensing deal with Arvinas Inc. potentially valued at north of $1 billion for global development and commercialization of ARV-766, the latter’s second-generation proteolysis targeting chimera (PROTAC) androgen receptor degrader targeting the same disease.
Cullgen (Shanghai) Inc. has disclosed proteolysis targeting chimera (PROTAC) compounds comprising a DDB1- and CUL4-associated factor 1 (DCAF1) binding moiety covalently linked to target protein moiety (such as bromodomain-containing protein 4 [BRD4; HUNK1], cyclin-dependent kinase 4 [CDK4] and estrogen receptor α [ER-α; ESR1]) through a linker reported to be useful for the treatment of cancer.
It has been previously demonstrated that while cancer cells with defects in ataxia telangiectasia mutated kinase (ATM) signaling are susceptible to ataxia telangiectasia and Rad3-related (ATR) inhibition following treatment with DNA-damaging drugs, normal cells can tolerate ATR inhibition by activating an ATM-mediated compensatory DNA damage response.
Auron Therapeutics Inc. has described proteolysis targeting chimeras (PROTACs) comprising a cereblon (CRBN) E3 ubiquitin ligase-binding moiety covalently linked to a histone acetyltransferase KAT2A and/or KAT2B (PCAF)-targeting moiety through a linker.
Haisco Pharmaceutical Group Co. Ltd. has prepared proteolysis targeting chimera (PROTAC) compounds comprising a cereblon ligase-binding moiety coupled to an EGFR (HER1; erbB1)-targeting moiety through a linker.
Astellas Pharma Inc. has patented new proteolysis targeting chimeras (PROTACs) comprising a cereblon E3 ubiquitin ligase-binding moiety coupled to GTPase KRAS (G12V mutant)-targeting agent through a linker.
Researchers from Zjengzhou University reported on the discovery and preclinical characterization of a novel PROTAC agent aimed at overcoming paclitaxel (Taxol) resistance in non-small-cell lung cancer treatment.
Chia Tai Tianqing Pharmaceutical Group Co. Ltd. has patented proteolysis targeting chimera (PROTAC) compounds comprising cereblon (CRBN) ligands covalently bonded to a Bcl-2-like protein 1 (Bcl-xl; Bcl-X; BCL2L1)-targeting moiety through a linker.
