ES2 peptide
Not For Human Use, Lab Use Only.
C190H355N101O37
Sequence 3 letters:
H-Pro-Arg-Lys-Gly-Gly-Arg-Arg-Arg-Arg-Ala-Trp-Gly-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Ala-Pro-Arg-Lys-Arg-Leu-Thr-Leu-Ala-OH
Sequence:
H-PRKGGRRRRAWGRRRRRRRRRRRRRRAPRKRLTLA-OH
Cas No. :
Molecular Formula:
C190H355N101O37
Molecular Weight:
4646.49
Description
ES2 can act as senolytics for eliminating senescent human cancer cells both in cell culture and in orthotopic mouse models. It disrupts FOXO4-TP53 foci, activates TP53 mediated apoptosis and preferentially binds FOXO4 compared to TP53. Intratumoural delivery of ES2 plus a BRAF inhibitor results in a significant increase in apoptosis and a survival advantage in mouse models of melanoma. Repeated systemic delivery of ES2 to older mice results in reduced senescent cell numbers in the liver with minimal toxicity. When compared with FOXO4-DRI peptide and found that, while FOXO4-DRI has minimal lytic activity in dividing cells, ES2 peptide had 3-7 times higher senolytic activity
Reference
- Hillary H. Le, Suleyman S. Cinaroglu, Elise C. Manalo, Aysegul Ors, Michelle M. Gomes, Burcin Duan Sahbaz, Karla Bonic, Carlos A. Origel Marmolejo, Arnaud Quentel, Justin S. Plaut, Taryn E. Kawashima, E. Sila Ozdemir, Sanjay V. Malhotra, Yavuz Ahiska, Ugur Sezerman, Gunseli Bayram Akcapinar, Joshua C. Saldivar, Emel Timucin, Jared M. Fischer, Molecular modelling of the FOXO4-TP53 interaction to design senolytic peptides for the elimination of senescent cancer cells, EBioMedicine, Volume 73, 2021, 103646, ISSN 2352-3964