Drug intelligence / Profile preview

RDD-142

Development stage
Preclinical
Lead developer
University of Pisa
Modality
Small Molecules
Administration
In Vitro
01

Overview

RDD-142 is a **hydroxyethylamine derivative** and a synthetic precursor analog of the HIV-1 protease inhibitor darunavir. It has been studied for its anti-cancer properties, particularly in hepatocellular carcinoma cell lines. RDD-142 induces **apoptosis** mainly via dose-dependent activation of caspase-3 and PARP-1 cleavage, decreases cell survival through inhibition of the PI3K/AKT pathway, and causes cell cycle arrest at G2/M phase with reduction of CDK1 and cyclin B levels. Additionally, it strongly activates all three branches of the unfolded protein response (UPR): PERK, ATF6, and IRE1α, leading to ER stress and autophagy. Docking studies reveal RDD-142 binds with high affinity to the β1–β5 and β6–β7 inhibitor-binding sites of the 20S proteasome, suggesting **proteasome inhibition** as a key mechanism. RDD-142 is considered a lead compound for further development rather than an approved drug and is not an active HIV-1 protease inhibitor itself, but a precursor in that drug class[1][3][5].

Other names
RDD142RDD-142RDD 142hydroxyethylamine derivative of darunavir
02

Targets

26S proteasomeATF6 (Activating transcription factor 6 alpha)ERN1 (Inositol-requiring enzyme 1 alpha)EIF2AK3 (Pkr-like endoplasmic reticulum kinase)AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)PARP1 (Poly (adp-ribose) polymerase 1)

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