Drug intelligence / Profile preview

Wuhan Univ. ERα compound P5

Development stage
Preclinical
Lead developer
Wuhan University
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules
01

Overview

Wuhan Univ. ERα compound P5: sourced facts only. name: "The lead compound P5 demonstrated high binding affinities for LBP and CBS sites, potent antiproliferative activity, and efficient ERα degradation efficacy across a panel of breast cancer cell lines via the ubiquitin-proteasome system." [PMID:42593925]; target: "The lead compound P5 demonstrated high binding affinities for LBP and CBS sites, potent antiproliferative activity, and efficient ERα degradation efficacy across a panel of breast cancer cell lines via the ubiquitin-proteasome system." [PMID:42593925]; developer: "Department of Hematology, Zhongnan Hospital of Wuhan University, School of Pharmaceutical Sciences, Wuhan University, Wuhan430071, China." [PMID:42593925]; modality: "we designed a series of ERα LBP/CBS dual-targeting proteolysis-targeting chimeras (PROTACs)" [PMID:42593925]; stage: "In vivo, P5 exhibited significant tumor growth inhibition in the LCC2 xenograft model, with efficacy comparable to fulvestrant, and a favorable safety profile." [PMID:42593925]

02

Targets

ESR1 (ERα)

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