Abstract: Methods of treating vascular leak, vascular inflammation, angiogenesis, ocular disorders, and/or inflammatory disorders in a patient are provided. The methods can include administering an ADP-ribosylation factor 6 (ARF6) inhibitor to the patient. The present disclosure also relates to new chemical entities and pharmaceutical compositions including ARF6 inhibitors. The ARF6 inhibitor may be a prodrug of an ARF6 inhibitor.

Abstract: Methods of treating vascular leak, vascular inflammation, angiogenesis, ocular disorders, and/or inflammatory disorders in a patient are provided. The methods can include administering an ADP-ribosylation factor 6 (ARF6) inhibitor to the patient. The present disclosure also relates to new chemical entities and pharmaceutical compositions including ARF6 inhibitors. The ARF6 inhibitor may be a prodrug of an ARF6 inhibitor.

Abstract: Disclosed herein are compounds and methods for inhibiting Arf6. Pharmaceutical compositions and methods for treating a subject with an inhibitor of Arf6 are also disclosed herein.

Abstract: Disclosed herein are compounds and methods for inhibiting Arf6. Pharmaceutical compositions and methods for treating a subject with an inhibitor of Arf6 are also disclosed herein.

Abstract: An assay and kit for determining the activity of an enzyme such as kinase, ATPase and GTPase is disclosed. The assay and kit are useful in drug screening to select modulators of such an enzyme.

Abstract: An assay and kit for determining the activity of an enzyme such as kinase, ATPase and GTPase is disclosed. The assay and kit are useful in drug screening to select modulators of such an enzyme.

Abstract: The present invention makes available a rapid, reproducible, robust assay system for screening and identifying pharmaceutically effective compounds that specifically interact with and modulate the activity of a cellular protein, e.g., a receptor or ion channel. The subject assay enables rapid screening of large numbers of compounds to identify those which act as an agonist or antagonist to the bioactivity of the cellular protein. In this system, the cell is treated with a compound, and functional interaction of this compound with a cellular receptor yields a detectable signal, which can be specifically measured. The subject assays include methods of identifying compounds which specifically modulate, for example, heterologous receptors coupled to the pheromone response pathway in yeast. The subject assays are particularly amenable to the identification of specific agonists and antagonists of G protein-coupled receptors.

Abstract: The present invention makes available a rapid, reproducible, robust assay system for screening and identifying pharmaceutically effective compounds that specifically interact with and modulate the activity of a cellular protein, e.g., a receptor or ion channel. The subject assay enables rapid screening of large numbers of compounds to identify those which act as an agonist or antagonist to the bioactivity of the cellular protein. In this system, the cell is treated with a compound, and functional interaction of this compound with a cellular receptor yields a detectable signal, which can be specifically measured. The subject assays include methods of identifying compounds which specifically modulate, for example, heterologous receptors coupled to the pheromone response pathway in yeast. The subject assays are particularly amenable to the identification of specific agonists and antagonists of G protein-coupled receptors.

Abstract: The present invention provides a mating-based yeast two-hybrid system for determining whether a test polypeptide interacts with another test polypeptide in the presence or absence of one or more test compounds. The system is useful in detecting protein-protein interactions and in identifying compounds capable of modulating protein-protein interactions.

Abstract: The present invention provides a mating-based yeast two-hybrid system for determining whether a test polypeptide interacts with another test polypeptide in the presence or absence of one or more test compounds. The system is useful in detecting protein-protein interactions and in identifying compounds capable of modulating protein-protein interactions.

Abstract: The invention provides yeast cells which comprise a mutation in an endogenous yeast stp22 gene and which express a heterologous G protein coupled receptor. The instant yeast cells display enhanced sensitivity to ligand induced stimulation of heterologous G protein coupled receptors and, therefore, show improved properties in drug screening assays.

Abstract: The invention provides isolated yeast cells which comprise a mutation in an endogenous yeast CAV1 gene, which exhibit increased signaling via the pheromone response pathway. In a preferred embodiment, the cav1 mutant yeast cells of the invention also express a heterologous G protein coupled receptor that functionally couples to the pheromone response pathway. The instant yeast cells display enhanced sensitivity to ligand induced stimulation of heterologous G protein coupled receptors and, therefore, show improved properties in drug screening assays.