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 originale | Inglese |
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pagine (da-a) | 132-144 |
Numero di pagine | 13 |
Rivista | European Journal of Medicinal Chemistry |
Volume | 91 |
DOI | |
Stato di pubblicazione | Pubblicato - 2015 |
Keywords
- kinase PIM1