Characterization of EHop-016, Novel Small Molecule Inhibitor of Rac GTPase
Brenda L. Montalvo-Ortiz,Linette Castillo-Pichardo,Eliud Hernandez,Tessa Humphries-Bickley,Alina De La Mota-Peynado,Luis A. Cubano,Cornelis P. Vlaar,Suranganie Dharmawardhane +7 more
TLDR
It is demonstrated that EHop-016 inhibits Rac activity in the MDA-MB-435 metastatic cancer cells that overexpress Rac and exhibits high endogenous Rac activity, and holds promise as a targeted therapeutic agent for the treatment of metastatic cancers with high Rac activity.About:
This article is published in Journal of Biological Chemistry.The article was published on 2012-04-13 and is currently open access. It has received 192 citations till now. The article focuses on the topics: Rac3 & PAK1.read more
Citations
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PI3K signaling in cancer: beyond AKT.
TL;DR: Three PI3K-dependent, but AKT-independent, signaling branches that have recently been shown to have important roles in promoting phenotypes associated with malignancy are highlighted.
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RAC1: An Emerging Therapeutic Option for Targeting Cancer Angiogenesis and Metastasis
TL;DR: In this article, the authors focus on one master regulator of cell motility, RAC1, and the existing data with regard to its role in cell motability, including particular roles for tumor angiogenesis and invasion/metastasis.
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Targeting Rac and Cdc42 GTPases in Cancer.
TL;DR: The regulatory mechanisms, inhibitory efficacy, and the anticancer potential of Rac- and Cdc42-targeting agents are summarized and an understanding of the regulatory mechanisms of these pivotal signaling intermediates is key for the development of effective inhibitors.
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Paving the Rho in cancer metastasis: Rho GTPases and beyond.
TL;DR: This review focuses on key discoveries in the regulation of epithelial-mesenchymal-transition, cell-cell junctions, formation of membrane protrusions, plasticity of cell migration and adaptation to a hypoxic environment and on crosstalk between Rho GTPase family members and other important oncogenic pathways.
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BNIP3 supports melanoma cell migration and vasculogenic mimicry by orchestrating the actin cytoskeleton.
Hannelore Maes,S Van Eygen,Dmitri V. Krysko,Peter Vandenabeele,Kris Nys,K Rillaerts,Abhishek D. Garg,Tom Verfaillie,Patrizia Agostinis +8 more
TL;DR: It is shown that BNIP3 supports cancer cell survival and long-term clonogenic growth, and an unprecedented pro-tumorigenic role of BnIP3 driving melanoma cell’s aggressive features, like migration and VM is unveiled.
References
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Journal ArticleDOI
Automated docking using a Lamarckian genetic algorithm and an empirical binding free energy function
Garrett M. Morris,David S. Goodsell,Robert Scott Halliday,Ruth Huey,William E. Hart,Richard K. Belew,Arthur J. Olson +6 more
TL;DR: It is shown that both the traditional and Lamarckian genetic algorithms can handle ligands with more degrees of freedom than the simulated annealing method used in earlier versions of AUTODOCK, and that the Lamarckia genetic algorithm is the most efficient, reliable, and successful of the three.
Journal ArticleDOI
Rho GTPases: Biochemistry and Biology
Aron B. Jaffe,Alan Hall +1 more
TL;DR: This review presents the best characterized of these biochemical pathways that control some of the most fundamental processes of cell biology common to all eukaryotes, including morphogenesis, polarity, movement, and cell division.
Journal ArticleDOI
Rho GTPases and their effector proteins.
Anne L. Bishop,Alan Hall +1 more
TL;DR: The main focus of this review will be Rho, Rac and Cdc42, the three best characterized mammalian Rho GTPases, though the genetic analysis of RhoGTPases in lower eukaryotes is making increasingly important contributions to this field.
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A semiempirical free energy force field with charge-based desolvation.
TL;DR: The authors describe the development and testing of a semiempirical free energy force field for use in AutoDock4 and similar grid‐based docking methods based on a comprehensive thermodynamic model that allows incorporation of intramolecular energies into the predicted free energy of binding.
Software News and Update A Semiempirical Free Energy Force Field with Charge-Based Desolvation
TL;DR: In this article, a semi-empirical free energy force field for use in AutoDock4 and similar grid-based docking methods is presented, based on a comprehensive thermodynamic model that allows incorporation of intramolecular energies into the predicted free energy of binding.