Through a computational approach, five new compounds with potent and selective Rac inhibitory activity were identified. In particular, compound 4 was shown to selectively inhibit Rac activity in a concentration-dependent manner by affecting the GEF-dependent GDP-GTP exchange. This compound was more potent than the original inhibitors previously identified.
3-Aryl-N-aminoylsulfonylphenyl-1H-pyrazole-5-carboxamides : a new class of selective Rac inhibitors / N. Ferri, S.K. Bernini, A. Corsini, F. Clerici, E. Erba, S. Stragliotto, A. Contini. - In: MEDCHEMCOMM. - ISSN 2040-2503. - 4:3(2013), pp. 537-541. [10.1039/C2MD20328F]
3-Aryl-N-aminoylsulfonylphenyl-1H-pyrazole-5-carboxamides : a new class of selective Rac inhibitors
N. FerriPrimo
;A. Corsini;F. Clerici;E. Erba;S. StragliottoPenultimo
;A. ContiniUltimo
2013
Abstract
Through a computational approach, five new compounds with potent and selective Rac inhibitory activity were identified. In particular, compound 4 was shown to selectively inhibit Rac activity in a concentration-dependent manner by affecting the GEF-dependent GDP-GTP exchange. This compound was more potent than the original inhibitors previously identified.
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