Ian Collins

TL;DR: The structure-based design, synthesis, structure-activity relationships and pharmacokinetics of potent small-molecule inhibitors of Hsp90 based on the 4,5-diarylisoxazole scaffold are described and analogues from this series have high affinity for HSp90, as measured in a fluorescence polarization (FP) competitive binding assay, and are active in cancer cell lines.

TL;DR: It is shown how chemical biology approaches offer techniques for interconnecting elements of the traditional linear progression from gene to drug, thereby providing a basis for increasing speed and success in cancer drug discovery.

TL;DR: The effects of macrocyclization upon potency, selectivity and physicochemical properties are discussed, concentrating on recent case histories in oncology drug discovery.

TL;DR: It is shown that the expression of vCD44 varies greatly among different human tumors and that some express either very low levels of v CD44 or no CD44 at all, which argues against a ubiquitous role for vCD 44 isoforms in promoting tumor growth and metastasis.

TL;DR: Current understanding of CHK2 function in tumour cells, in both a biological and genetic context, suggests that targeted modulation of the active kinase or exploitation of its loss in tumours could prove to be effective anti-cancer strategies.