Publications [#233247] of Andrew T. McPhail
Journal Articles
- Coval, SJ; Patton, RW; Petrin, JM; James, L; Rothofsky, ML; Lin, SL; Patel, M; Reed, JK; McPhail, AT; Bishop, WR, "A cembranolide diterpene farnesyl protein transferase inhibitor from the marine soft coral Lobophytum cristagalli", Bioorganic and Medicinal Chemistry LettersApril,, 1996, 6(7), 909-912, Elsevier BV [Gateway.cgi], [doi].
(last updated on 2026/01/21)Abstract:
A previously described cembranolide diterpene from Lobophytum cristagalli was identified as a potent (IC50 0.15 μM) inhibitor of farnesyl protein transferase (FPT). The compound showed selectivity for FPT as compared to the closely related enzyme geranylgeranyl protein transferase-1 (IC50 5.3 μM). Kinetic evaluation suggests that this compound competes with the protein/peptide farnesyl acceptor substrate, and not with farnesyl pyrophosphate for inhibition of FPT.