Fmoc-Ala-Glu-Asn-Lys-NH2 is a peptide inhibitor that selectively targets asparagine endopeptidase (AEP) and inhibits the cleavage of amyloid precursor protein (APP). AEP, a pH-controlled cysteine proteinase, plays a crucial role in the proteolytic processing of APP, and its activity is enhanced during the aging process [1].
Albizziin is amino acid analog which acts as a competitive inhibitor of asparagine synthetase with respect to glutamine. Albizziin has been used to isolate mutants of Chinese hamster ovary cells with alterations in levels of the target enzyme. Several classes of mutations can be distinguished on the basis of cross-resistance to beta-aspartyl hydroxamate, another amino acid analog. Studies on asparagine synthetase indicate that resistance to albizziin may be due to altered regulation of asparagine synthetase, structural mutations of the enzyme, and gene amplification.
GCN2iB is a GCN2 inhibitor. GCN2iB may be useful for the treatment of cancer. The inhibition of GCN2 sensitizes cancer cells with low basal-level expression of asparagine synthetase (ASNS) to the antileukemic agent L-asparaginase (ASNase) in vitro and in vivo.