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

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

doi:10.1016/j.ejmech.2014.07.093

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

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

Risultato della ricerca: Contributo in rivista › Articolo

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
pagine (da-a)	132-144
Numero di pagine	13
Rivista	European Journal of Medicinal Chemistry
Volume	91
DOI	https://doi.org/10.1016/j.ejmech.2014.07.093
Stato di pubblicazione	Pubblicato - 2015

Keywords

kinase PIM1

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10.1016/j.ejmech.2014.07.093

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Persico, M., Petrella, L., Orteca, N., Di Dato, A., Mariani, M., Andreoli, M., De Donato, M., Scambia, G., Novellino, E., Ferlini, C., & Fattorusso, C. (2015). GTP is an allosteric modulator of the interaction between the guanylate-binding protein 1 and the prosurvival kinase PIM1. European Journal of Medicinal Chemistry, 91, 132-144. https://doi.org/10.1016/j.ejmech.2014.07.093

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

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.",

keywords = "kinase PIM1, kinase PIM1",

author = "M Persico and L Petrella and N Orteca and {Di Dato}, A and M Mariani and M Andreoli and {De Donato}, M and Giovanni Scambia and E Novellino and C Ferlini and C. Fattorusso",

year = "2015",

doi = "10.1016/j.ejmech.2014.07.093",

language = "English",

volume = "91",

pages = "132--144",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

publisher = "Elsevier Masson s.r.l.",

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Persico, M, Petrella, L, Orteca, N, Di Dato, A, Mariani, M, Andreoli, M, De Donato, M, Scambia, G, Novellino, E, Ferlini, C & Fattorusso, C 2015, 'GTP is an allosteric modulator of the interaction between the guanylate-binding protein 1 and the prosurvival kinase PIM1', European Journal of Medicinal Chemistry, vol. 91, pagg. 132-144. https://doi.org/10.1016/j.ejmech.2014.07.093

TY - JOUR

T1 - GTP is an allosteric modulator of the interaction between the guanylate-binding protein 1 and the prosurvival kinase PIM1

AU - Persico, M

AU - Petrella, L

AU - Orteca, N

AU - Di Dato, A

AU - Mariani, M

AU - Andreoli, M

AU - De Donato, M

AU - Scambia, Giovanni

AU - Novellino, E

AU - Ferlini, C

AU - Fattorusso, C.

PY - 2015

Y1 - 2015

N2 - 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.

AB - 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.

KW - kinase PIM1

UR - http://hdl.handle.net/10807/63185

UR - http://www.scopus.com/inward/record.url?eid=2-s2.0-84904711484&partnerid=40&md5=bdf98933eb11761339c7560d28765195

U2 - 10.1016/j.ejmech.2014.07.093

DO - 10.1016/j.ejmech.2014.07.093

M3 - Article

SN - 0223-5234

VL - 91

SP - 132

EP - 144

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

ER -

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

Abstract

Keywords

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