Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.
肽基化合物包括含杂原子的三元环,能够高效且选择性地抑制N-末端亲核试剂(Ntn)
水解酶的特定活性。这些具有多种活性的Ntn的活性可以被所描述的化合物差异性地抑制。例如,创
蛋白酶样活性的20S
蛋白酶可以通过这种创新的化合物被选择性地抑制。这些肽基化合物包括
环氧化物或氮杂环,以及N-末端的官能化。除了其他治疗用途外,这些肽基化合物预计具有抗炎性和细胞增殖抑制作用。