Novel biologically active nonpeptidic inhibitors of myristoylCoA:protein N-myristoyltransferase

Journal of Medicinal Chemistry
B DevadasJ A Sikorski

Abstract

A new class of biologically active nonpeptidic inhibitors of Candida albicans NMT has been synthesized starting from the octapeptide ALYASKLS-NH2 (2). The synthetic strategy entailed the preparation of novel protected Ser-Lys mimics 9 and 12 from (S)- or (R)-3-iodotyrosine and then grafting key enzyme recognition elements in a stepwise manner. Like 2, compounds 16, 17, and 18 are competitive Candida NMT inhibitors that bind to the peptide recognition site of the enzyme. Moreover, 16-18 have an affinity comparable to that of 2 even though they are devoid of peptide bonds. In contrast to 2, these nonpeptidic inhibitors exhibit antifungal activity.

References

Dec 6, 1994·Proceedings of the National Academy of Sciences of the United States of America·J K LodgeJ I Gordon

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Citations

Apr 20, 2001·European Journal of Medicinal Chemistry·R G Karki, V M Kulkarni
Sep 18, 2003·Bioorganic & Medicinal Chemistry·Miyako MasubuchiNobuo Shimma
Mar 6, 1999·Current Opinion in Microbiology·N H Georgopapadakou
Oct 6, 1999·Current Opinion in Microbiology·B DiDomenico
Nov 26, 1999·Biochimica Et Biophysica Acta·R S BhatnagarJ I Gordon
May 19, 2000·The Biochemical Journal·R S GunaratneA A Holder
Sep 11, 2007·The Plant Cell·Michèle PierreThierry Meinnel
Nov 29, 2002·Eukaryotic Cell·Brian D ShawMichelle Momany
Jan 10, 2002·Analytical Biochemistry·Cynthia R PenniseDavid L Pompliano
Aug 2, 2002·Expert Opinion on Investigational Drugs·Nafsika H Georgopapadakou
Aug 16, 2014·ChemMedChem·Can Zhao, Shutao Ma
Feb 13, 2019·Analytical Sciences : the International Journal of the Japan Society for Analytical Chemistry·Rui ZhaoDongping Tao
Aug 31, 2001·The Journal of Biological Chemistry·T A FaraziJ I Gordon
Dec 2, 2019·International Journal of Biological Macromolecules·Shikha SharmaYusuf Akhter
Dec 7, 2002·Bioorganic & Medicinal Chemistry Letters·Ken-ichi KawasakiNobuo Shimma
Sep 11, 2013·Journal of Medicinal Chemistry·Ian H Gilbert
Nov 9, 2010·Biochimie·Dale D O MartinLuc G Berthiaume

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