Drug intelligence / Profile preview

UBE2K siRNA

Development stage
Preclinical
Lead developer
Berg
Modality
Chemically Modified siRNA → Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Conjugated siRNA → Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics
01

Overview

UBE2K siRNA is a small interfering RNA (siRNA) designed to target and silence the expression of the UBE2K gene, which encodes the Ubiquitin-conjugating enzyme E2 K. This enzyme is a unique member of the ubiquitin-proteasome system (UPS) involved in protein homeostasis and quality control. In preclinical studies conducted by BERG using their Interrogative Biology platform, UBE2K siRNA was employed to validate UBE2K as a therapeutic target in various cancer models, including pancreatic (MIA PaCa2) and hepatocellular (SKHEP1, HepG2) carcinomas. The siRNA-mediated knockdown of UBE2K results in significant inhibition of cell proliferation, characterized by G2/M cell cycle arrest, stabilization of CyclinB1, and induction of apoptosis. These findings supported the development of small molecule modulators of UBE2K, such as BRG399, for oncology indications.

Other names
siRNA mediated knockdown of UBE2KUBE2K-targeting siRNAUBE-2K-targeting siRNAUBE 2K-targeting siRNA
02

Targets

UBE2K (Ubiquitin-conjugating enzyme E2 K)

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