Regulation of small gtpases by gefs, gaps, and gdis
J Cherfils, M Zeghouf - Physiological reviews, 2013 - journals.physiology.org
Small GTPases use GDP/GTP alternation to actuate a variety of functional switches that are
pivotal for cell dynamics. The GTPase switch is turned on by GEFs, which stimulate …
pivotal for cell dynamics. The GTPase switch is turned on by GEFs, which stimulate …
ARF GTPases and their GEFs and GAPs: concepts and challenges
E Sztul, PW Chen, JE Casanova… - Molecular biology of …, 2019 - Am Soc Cell Biol
Detailed structural, biochemical, cell biological, and genetic studies of any gene/protein are
required to develop models of its actions in cells. Studying a protein family in the aggregate …
required to develop models of its actions in cells. Studying a protein family in the aggregate …
Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS–SOS1 interaction
RC Hillig, B Sautier, J Schroeder… - Proceedings of the …, 2019 - National Acad Sciences
Since the late 1980s, mutations in the RAS genes have been recognized as major
oncogenes with a high occurrence rate in human cancers. Such mutations reduce the ability …
oncogenes with a high occurrence rate in human cancers. Such mutations reduce the ability …
Haven't got a glue: protein surface variation for the design of molecular glue degraders
Molecular glue degraders are small, drug-like compounds that induce interactions between
an E3 ubiquitin ligase and a target, which result in ubiquitination and subsequent …
an E3 ubiquitin ligase and a target, which result in ubiquitination and subsequent …
Modulators of 14-3-3 protein–protein interactions
LM Stevers, E Sijbesma, M Botta… - Journal of medicinal …, 2017 - ACS Publications
Direct interactions between proteins are essential for the regulation of their functions in
biological pathways. Targeting the complex network of protein–protein interactions (PPIs) …
biological pathways. Targeting the complex network of protein–protein interactions (PPIs) …
Modulators of protein–protein interactions
LG Milroy, TN Grossmann, S Hennig… - Chemical …, 2014 - ACS Publications
Since Hedin's characterization of trypsin and antitrypsin in 1906,(1) arguably the first
account of a regulatory protein–protein interaction (PPI), contemporary understanding of …
account of a regulatory protein–protein interaction (PPI), contemporary understanding of …
Ras superfamily GEFs and GAPs: validated and tractable targets for cancer therapy?
D Vigil, J Cherfils, KL Rossman, CJ Der - Nature Reviews Cancer, 2010 - nature.com
There is now considerable and increasing evidence for a causal role for aberrant activity of
the Ras superfamily of small GTPases in human cancers. These GTPases function as GDP …
the Ras superfamily of small GTPases in human cancers. These GTPases function as GDP …
Topoisomerase I inhibitors: camptothecins and beyond
Y Pommier - Nature Reviews Cancer, 2006 - nature.com
Abstract Nuclear DNA topoisomerase I (TOP1) is an essential human enzyme. It is the only
known target of the alkaloid camptothecin, from which the potent anticancer agents …
known target of the alkaloid camptothecin, from which the potent anticancer agents …
GEFs and GAPs: critical elements in the control of small G proteins
JL Bos, H Rehmann, A Wittinghofer - Cell, 2007 - cell.com
Guanine nucleotide exchange factors (GEFs) and GTPase-activating proteins (GAPs)
regulate the activity of small guanine nucleotide-binding (G) proteins to control cellular …
regulate the activity of small guanine nucleotide-binding (G) proteins to control cellular …
Structural basis for the regulation of tubulin by vinblastine
B Gigant, C Wang, RBG Ravelli, F Roussi… - Nature, 2005 - nature.com
Vinblastine is one of several tubulin-targeting Vinca alkaloids that have been responsible for
many chemotherapeutic successes since their introduction in the clinic as antitumour drugs …
many chemotherapeutic successes since their introduction in the clinic as antitumour drugs …