Abstract
Abstract The Src homology-2 domain-containing protein tyrosine phosphatase-2 (SHP2) is a positive transducer of growth factor, cytokine, integrin, and hormone signaling pathways which regulates processes such as cell proliferation, differentiation, adhesion, migration, and apoptosis and plays a pivotal role in growth factor and cytokine signaling. Gain-of-function SHP2 mutations are associated with various kinds of leukemia, and solid tumors. This makes SHP2 an attractive target for anticancer therapy. We are developing SHP2 inhibitors as novel anticancer drugs. Previously, we have reported on SPI-112 and its methyl ester prodrug SPI-112Me. However, the poor solubility of SPI-112Me has become an obstacle for in vivo studies. In ongoing study, we generate SPI-112 analogs to further improve physicochemical properties of these SHP2 inhibitors, such as solubility and cell permeability. To this aim, we synthesized SPI-112 derivatives containing various phosphotyrosine mimics and their prodrugs. SPI-112 derivatives of SHP2 inhibitors having improved properties have been obtained in this effort. Citation Format: {Authors}. {Abstract title} [abstract]. In: Proceedings of the 103rd Annual Meeting of the American Association for Cancer Research; 2012 Mar 31-Apr 4; Chicago, IL. Philadelphia (PA): AACR; Cancer Res 2012;72(8 Suppl):Abstract nr 2912. doi:1538-7445.AM2012-2912
Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
