Drug intelligence / Profile preview

Guangdong Univ. of Technology TrxR2 compound 23d

Development stage
Unknown
Lead developer
Guangdong University of Technology
Modality
Small Molecules
01

Overview

Guangdong Univ. of Technology TrxR2 compound 23d: sourced facts only. name: "To our knowledge, 23d is the first non-electrophilic ent-kaurane derivative to combine mitochondrial targeting with TrxR2 inhibition and in vivo antitumor efficacy, highlighting dual modification as a promising strategy integrating biodistribution engineering with activity optimization for anticancer drug development." [PMID:41812408]; target: "To our knowledge, 23d is the first non-electrophilic ent-kaurane derivative to combine mitochondrial targeting with TrxR2 inhibition and in vivo antitumor efficacy, highlighting dual modification as a promising strategy integrating biodistribution engineering with activity optimization for anticancer drug development." [PMID:41812408]; developer: "School of Biomedical and Pharmaceutical Sciences, Guangdong University of Technology, Guangzhou, 510006, China." [PMID:41812408]; modality: "28 triphenylphosphonium (TPP)-conjugated steviol derivatives were synthesized to enhance mitochondrial accumulation and modulate mitochondrial signaling." [PMID:41812408]; stage: "Conjugate 23d (C-13 TPP, C-19 benzyl ester) was the most potent (IC50 = 0.19 μM, SI = 15.42) and significantly suppressed Huh7 xenografts growth with favorable safety." [PMID:41812408]

02

Targets

TXNRD2 (Thioredoxin reductase 2)

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