Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T15739 Target Info
Target Name Cellular tumor antigen p53 (TP53)
Synonyms
Tumor suppressor p53; Phosphoprotein p53; P53; Antigen NY-CO-13
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Target Type Clinical trial Target
Gene Name TP53
UniProt ID
P53_HUMAN
Co-Targets of This Target  Top
Co-Target Name Ubiquitin-protein ligase E3 Mdm2 (MDM2) Clinical trial Target
UniProt ID MDM2_HUMAN
Gene Name MDM2
Synonyms
RING-type E3 ubiquitin transferase Mdm2; P53-binding protein Mdm2; Oncoprotein Mdm2; MDM2 protein; Hdm2; E3 ubiquitin-protein ligase Mdm2; Double minute 2 protein
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Representative Drug(s) HDM201 Drug Info Ki = 0.21 nM Click to Show More [1]
2 SAR-405838 Drug Info Ki = 0.88 nM [2]
3 APG-115 Drug Info Ki < 1 nM [3]
4 CGM097 Drug Info Ki = 1.3 nM [4]
References  Top
REF 1 The development of piperidinones as potent MDM2-P53 protein-protein interaction inhibitors for cancer therapy. Eur J Med Chem. 2018 Nov 5;159:1-9.
REF 2 Small-molecule inhibitors of the MDM2-p53 protein-protein interaction (MDM2 Inhibitors) in clinical trials for cancer treatment. J Med Chem. 2015 Feb 12;58(3):1038-52.
REF 3 Discovery of 4-((3'R,4'S,5'R)-6"-Chloro-4'-(3-chloro-2-fluorophenyl)-1'-ethyl-2"-oxodispiro[cyclohexane-1,2'-pyrrolidine-3',3"-indoline]-5'-carboxamido)bicyclo[2.2.2]octane-1-carboxylic Acid (AA-115/APG-115): A Potent and Orally Active Murine Double Minute 2 (MDM2) Inhibitor in Clinical Development. J Med Chem. 2017 Apr 13;60(7):2819-39.
REF 4 Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. J Med Chem. 2015 Aug 27;58(16):6348-58.

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