Bristol Myers Squibb Co. has described proteolysis targeting chimera (PROTAC) compounds comprising a E3 ubiquitin ligase-binding moiety coupled to a proto-oncogene tyrosine-protein kinase receptor Ret (RET; CDHF12; PTC) targeting moiety through a linker reported to be useful for the treatment of non-small-cell lung cancer.
Scientists at Bristol Myers Squibb Co. and Celgene Corp. have synthesized proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN) E3 ubiquitin ligase-binding moiety coupled to a protein-targeting moiety through a linker.
Celgene Corp. has divulged proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety covalently linked to a MAP kinase-activated protein kinase 2 (MAPKAPK2; MK2)-targeting moiety via a linker.
Purdue Research Foundation has synthesized proteolysis targeting chimeras (PROTACs) comprising a E3 ubiquitin ligase binding moiety covalently linked to a tyrosine-protein phosphatase non-receptor type 1 (PTPN1; PTP-1B) and 2 (PTPN2; TCPTP) dual targeting moiety reported to be useful for the treatment of cancer, type 2 diabetes and obesity.
Nanjing Mingde New Drug Research Co. Ltd. has divulged proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase-binding agent coupled to an estrogen receptor α (ER-α; ESR1)-targeting moiety via linker. They are reported to be useful for the treatment of breast cancer.
Beijing Tide Pharmaceutical Co. Ltd. has identified proteolysis targeting chimeras (PROTACs) comprising a cereblon E3 ubiquitin ligase binding moiety coupled to tyrosine-protein phosphatase non-receptor type 11 (PTPN11; PTP-2C; SHP-2) targeting agents through linkers reported to be useful for the treatment of cancer.
Mitsubishi Tanabe Pharma Corp. has divulged proteolysis targeting chimeras (PROTACs) comprising a cereblon E3 ubiquitin ligase (CRBN) binding moiety coupled to disease-associated protein targeting moiety through a linker reported to be useful for the treatment of cancer, inflammatory disorders, autoimmune disease, neurodegeneration and genetic disorders.
Risen (Shanghai) Pharma Eng Co. Ltd. and Risen (Suzhou) Pharma Tech Co. Ltd. have divulged proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding agents coupled to GTPase KRAS or its mutant targeting moiety through a linker reported to be useful for the treatment of cancer.
Beijing Neox Biotech Co. Ltd. has patented proteolysis targeting chimera (PROTACs) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to wee1-like protein kinase (Wee1) binding moiety through a linker reported to be useful for the treatment of cancer.
Chia Tai Tianqing Pharmaceutical Group Co. Ltd. has identified proteolysis targeting chimera (PROTAC) compounds comprising a E3 ubiquitin ligase-binding moiety coupled to RACα serine/threonine-protein kinase AKT targeting moiety through a linker reported to be useful for the treatment of prostate cancer.