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The BET proteins play a crucial role in regulating gene expression as epigenetic regulators and are involved in cancer pathogenesis. PROTAC targeted degradation of BET proteins has recently attracted increasing interest in the field of cancer therapy. PROTAC technology offers many potential advantages, such as good ADME (absorption, distribution, metabolism and elimination) properties, overcoming target protein mutation-directed resistance, target various proteins including undruggable proteins. BOC Sciences is a leading CRO focused on the development of targeted protein degraders, and we have established comprehensive PROTACs development platform. We provide customized PROTAC development services based on the customer's PRTAC development needs for a particular target.
The bromodomain and extra-terminal structural domain (BET) proteins family has two tandem bromodomains and one extra-terminal structural domain, including members BRD2, BRD3, BRD4 and BRDT. BET proteins play a key role in regulating gene transcription during cell proliferation and differentiation through epigenetic interactions between bromodomains and acetylated histones. In addition, BET proteins are involved in tumorigenesis, as well as mediating viral infection in host cells. Blocking the BET bromodomain with PROTAC protein degraders selectively inhibits the transcriptional, and these PROTACs are expected to be potential therapeutic agents for a variety of cancers.
PROTAC (proteolysis-targeting chimera) is a heterobifunctional small molecule compound capable of drawing target protein and intracellular E3 ligases into close proximity, resulting in a target protein-PROTAC-E3 ligase ternary complex that subsequently mediates polyubiquitination of the target protein and finally degrades the target protein specifically using the proteasome in the organism. Due to their unique chemical and biological properties, PROTACs have unique advantages in cancer therapy, such as targeting undruggable proteins and overcoming traditional drug resistance.
Fig 1. BET-PROTAC degraders (Yang, 2019)
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