Synthesis and Cytotoxicity on Human Lung Cancer Cell Lines of 2-Arylidene and Related Analogues of Malabaricol.

Malabaricol is a unique plant natural product, 3-keto tricarbocyclic triterpenoid, isolated from . Malabaricol underwent reaction with aromatic aldehydes under alkaline conditions to form 2-arylidene analogs. Indoles and pyrazine ring system fused to the 2,3-position of malabaricol were synthesized.

Human Naa50 Protein Displays Broad Substrate Specificity for Amino-terminal Acetylation: DETAILED STRUCTURAL AND BIOCHEMICAL ANALYSIS USING TETRAPEPTIDE LIBRARY.

Amino-terminal acetylation is a critical co-translational modification of the newly synthesized proteins in a eukaryotic cell carried out by six amino-terminal acetyltransferases (NATs). All NATs contain at least one catalytic subunit, and some contain one or two additional auxiliary subunits. For example, NatE is a complex of Naa10, Naa50, and Naa15 (auxiliary).

Discovery of a new genetic variant of methionine aminopeptidase from Streptococci with possible post-translational modifications: biochemical and structural characterization.

Protein N-terminal methionine excision is an essential co-translational process that occurs in the cytoplasm of all organisms. About 60-70% of the newly synthesized proteins undergo this modification. Enzyme responsible for the removal of initiator methionine is methionine aminopeptidase (MetAP), which is a dinuclear metalloprotease.

Identification, biochemical and structural evaluation of species-specific inhibitors against type I methionine aminopeptidases.

Methionine aminopeptidases (MetAPs) are essential enzymes that make them good drug targets in cancer and microbial infections. MetAPs remove the initiator methionine from newly synthesized peptides in every living cell. MetAPs are broadly divided into type I and type II classes.

Structure activity relationship studies of imidazo[1,2-a]pyrazine derivatives against cancer cell lines.

Designed novel imidazo[1,2-a]pyrazine based inhibitors, synthesized by condensing α-aminopyrazines with α-halocarbonyl compounds followed by electrophilic substitutions. Cytotoxic effects on four cancer cell lines evaluated. Based on preliminary data, imidazo[1,2-a]pyrazine template redesigned to improve activity.