Delving into the Latest Updates on BPTF-specific PROTAC 8d(University of Science & Technology of China) with Synapse

Overview

Basic Info

Drug Type

Proteolysis-targeting chimeras (PROTAC)

Synonyms-

Target

BPTF

Action

inhibitors

Mechanism

BPTF inhibitors(bromodomain PHD finger transcription factor inhibitors)

Therapeutic Areas

NeoplasmsDigestive System Disorders

Active Indication

Hepatocellular Carcinoma

Inactive Indication-

Originator Organization

University of Science & Technology of China

Active Organization

University of Science & Technology of China

Inactive Organization-

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Natural killer (NK) cell-based immunotherapy shows promise in cancer treatment, but its efficacy remains limited, necessitating the development of novel strategies. In this study, we demonstrate that the epigenetic factor bromodomain PHD-finger containing transcription factor (BPTF) hinders hepatocellular carcinoma (HCC) recognition by NK cells through its PHD finger's interpretation of H3K4me3. We have generated a small-molecule proteolysis-targeting chimera (PROTAC) that selectively degrades human and murine BPTF. The degradation of BPTF using PROTACs directly enhances the abundance of natural cytotoxicity receptor ligands on HCC cells, facilitating their recognition by NK cells and thereby augmenting NK cell cytotoxicity against HCC both in vitro and in vivo. Through multidisciplinary techniques, our findings establish targeting BPTF with PROTACs as a promising approach to overcome immune evasion of HCC from NK cells and provide a new strategy to enhance NK cell-based cancer immunotherapy.

100 Deals associated with BPTF-specific PROTAC 8d(University of Science & Technology of China)

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