2xp8
DISCOVERY OF CELL-ACTIVE PHENYL-IMIDAZOLE PIN1 INHIBITORS BY STRUCTURE-GUIDED FRAGMENT EVOLUTIONDISCOVERY OF CELL-ACTIVE PHENYL-IMIDAZOLE PIN1 INHIBITORS BY STRUCTURE-GUIDED FRAGMENT EVOLUTION
Structural highlights
Publication Abstract from PubMedPin1 is an emerging oncology target strongly implicated in Ras and ErbB2-mediated tumourigenesis. Pin1 isomerizes bonds linking phospho-serine/threonine moieties to proline enabling it to play a key role in proline-directed kinase signalling. Here we report a novel series of Pin1 inhibitors based on a phenyl imidazole acid core that contains sub-muM inhibitors. Compounds have been identified that block prostate cancer cell growth under conditions where Pin1 is essential. Discovery of cell-active phenyl-imidazole Pin1 inhibitors by structure-guided fragment evolution.,Potter A, Oldfield V, Nunns C, Fromont C, Ray S, Northfield CJ, Bryant CJ, Scrace SF, Robinson D, Matossova N, Baker L, Dokurno P, Surgenor AE, Davis B, Richardson CM, Murray JB, Moore JD Bioorg Med Chem Lett. 2010 Nov 15;20(22):6483-8. Epub 2010 Sep 17. PMID:20932746[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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OCA- Homo sapiens
- Peptidylprolyl isomerase
- Baker, L.
- Bryant, C J.
- Davis, B E.
- Dokurno, P.
- Fromont, C.
- Matossova, N.
- Moore, J D.
- Murray, J B.
- Northfield, C J.
- Nunns, C.
- Oldfield, V.
- Potter, A.
- Ray, S.
- Richardson, C M.
- Robinson, D.
- Scrace, S F.
- Surgenor, A E.
- Cell cycle
- Isomerase
- Oncogenic transformation
- Proline directed kinase