Identification of FAK substrate peptides via colorimetric screening of a one‐bead one‐peptide combinatorial library

Peer Reviewedhttp://deepblue.lib.umich.edu/bitstream/2027.42/110814/1/psc2751.pd

Synthesis of Derivatives of 3-Aminoquinazolinone and 2\u27-Deoxyguanosine as Potential Protein Tyrosine Kinase Inhibitors

Protein kinases play an important role in post-translational cellular signaling by regulating cell growth, differentiation and apoptosis, among other cellular activities. Furthermore, protein kinase (PK) deregulation has been implicated in many diseases, including cancer. For this reason, there has been considerable interest in the development of PK inhibitors, which could lead to the discovery of new cancer-treating drugs. Derivatives of 3-aminoquinazolinone and 2\u27-deoxyguanosine were synthesized as potential ATP-competitive inhibitors of the Src and FAK protein tyrosine kinases, and the effectiveness of the synthesized derivatives as protein tyrosine kinase inhibitors was quantified using [γ-32P]ATP radioisotope assays. The results of the assays indicated that none of the compounds synthesized were as effective as other previously discovered inhibitors