Structural basis for relief of autoinhibition of the DbI homology domain of proto-oncogene Vav by tyrosine phosphorylation

Article Abstract:

Results demonstrate that an N-terminal extension, containing Tyr174 Src-family kinase recognition site, inhibits mVav1 of the DbI homology domain by being released from the domain and becoming unstructured upon phosphorylation. Data suggest that inhibition of the domain is relieved by tyrosine phosphorylation, which exposes the domain leading to proto-oncogene Vav activation.

Structure-activity relationships (Biochemistry), Ras genes

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Src tyrosine kinase is a novel direct effector of G proteins

Article Abstract:

Research demonstrates that the cellular signal transducers, Src family tyrosine kinases are directly involved in the function of G proteins. Data show that Galpha-s and Galpha-i stimulate the kinase activity upon binding to the catalytic domain of Src that leads to a conformational change exposing active site access to substrates.

Enzymes, Cellular signal transduction, Genetic regulation, Genetic transcription, Transcription (Genetics), G proteins, Enzyme regulation

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SET-ting the stage for life and death

Article Abstract:

This article examines the regulation of programmed cell death of tumor cells or cells infected with virus mediated by T lymphocyte secreted enzymes granzymes. A tumor metastasis suppressor protein activated by granzyme A functions as a apoptosis-inducing DNase, which is inhibited by the oncoprotein SET.

Pharmaceutical Preparation Manufacturing, Pharmaceutical preparations, Enzyme Inhibitors, Metastasis, Cancer metastasis, Apoptosis

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