Recent Advances in the Design and Synthesis of SH2 Inhibitorsof Src, Grb2 and ZAP-70.

Title: Recent Advances in the Design and Synthesis of SH2 Inhibitorsof Src, Grb2 and ZAP-70.

Volume: 7 Issue: 10

Author(s): Chi B. Vu

Affiliation:

Abstract: A perspective is offered on the recent development of Src-homology 2 (SH2) antagonists of Src, Grb2 and ZAP-70. Inhibiting Src SH2 is believed to be a potentially attractive way of regulating bone resorption. Grb2 SH2 has been shown to be an important component of the mitogenic ras pathway; and thus might be of utility in cancer research. ZAP-70 is a tyrosine kinase that is expressed solely in T-cells and natural killer cells. Since inhibition of the tandem SH2 domains of ZAP-70 has been shown to block T-cell proliferation, antagonists for this particular protein could have implications in immune suppression. The emphasis of the article is placed on the structure-based design, synthesis and biological activity of a number of newly reported SH2 antagonists in each of the three areas.

Cite this article as:

Vu B. Chi, Recent Advances in the Design and Synthesis of SH2 Inhibitorsof Src, Grb2 and ZAP-70., Current Medicinal Chemistry 2000; 7 (10) . https://dx.doi.org/10.2174/0929867003374390