GTP is an allosteric modulator of the interaction between the guanylate-binding protein 1 and the prosurvival kinase PIM1

Giovanni Scambia, M Persico, L Petrella, N Orteca, A Di Dato, M Mariani, M Andreoli, M De Donato, E Novellino, C Ferlini, C. Fattorusso

Risultato della ricerca: Contributo in rivistaArticolo in rivista

Abstract

GBP1 and PIM1 are known to interact with a molar ratio 1:1. GBP1:PIM1 binding initiates a signaling pathway that induces resistance to common chemotherapeutics such as paclitaxel. Since GBP1 is a large GTPase which undergoes conformational changes in a nucleotide-dependent manner, we investigated the effect of GTP/GDP binding on GBP1:PIM1 interaction by using computational and biological studies. It resulted that only GTP decreases the formation of the GBP1:PIM1 complex through an allosteric mechanism, putting the bases for the identification of new compounds potentially able to revert resistance to paclitaxel.
Lingua originaleEnglish
pagine (da-a)1-13
Numero di pagine13
RivistaEuropean Journal of Medicinal Chemistry
Stato di pubblicazionePubblicato - 2014

Keywords

  • kinase PIM1

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