Drug intelligence / Profile preview

MGP-39

Development stage
Preclinical
Lead developer
Chinese Academy of Medical Sciences and Peking Union Medical College
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules
01

Overview

MGP-39: sourced facts only. name: "Through design, computer-assisted optimization and SAR studies, we developed the first-in-class MELK-targeting PROTAC MGP-39, which promoted a rapid and potent degradation of MELK in RAMOS cells." [PMID:39026635]; target: "Through design, computer-assisted optimization and SAR studies, we developed the first-in-class MELK-targeting PROTAC MGP-39, which promoted a rapid and potent degradation of MELK in RAMOS cells." [PMID:39026635]; developer: "State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College Beijing 100050 China [email protected]." [PMID:39026635]; modality: "Through design, computer-assisted optimization and SAR studies, we developed the first-in-class MELK-targeting PROTAC MGP-39, which promoted a rapid and potent degradation of MELK in RAMOS cells." [PMID:39026635]; stage: "Notably, compared to MELK inhibitors, MGP-39 has better anti-cancer activity and lower toxicity, indicating the practical role of PROTACs in avoiding the side effects of traditional inhibitors." [PMID:39026635]

02

Targets

MELK (Maternal embryonic leucine zipper kinase)

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