The synthesis of peptidylfluoromethanes and their properties as inhibitors of serine proteinases and cysteine proteinases.

Synthesis and properties of peptidyl derivatives of arginylfluoromethanes.

Two peptide derivatives of arginylfluoromethane (Arg-CH2F), namely Bz(benzoyl)-Phe-ArgCH2F and D-Phe-Pro-Arg-CH2F, have been synthesized by extension of available methods, i.e. the Dakin-West reaction [Rasnick (1985) Anal. Biochem. 149, 461-465] or synthesis of a phthaloyl-blocked C-terminal fluoromethane [Rauber, Angliker, Walker & Shaw (1986) Biochem. J. 239, 633-640; Angliker, Wikström, Raub...

Compensatory proteolytic responses to dietary proteinase inhibitors in the red flour beetle, Tribolium castaneum (Coleoptera: Tenebrionidae).

Increasing levels of inhibitors that target cysteine and/or serine proteinases were fed to Tribolium castaneum larvae, and the properties of digestive proteinases were compared in vitro. Cysteine proteinases were the major digestive proteinase class in control larvae, and serine proteinase activity was minor. Dietary serine proteinase inhibitors had minimal effects on either the developmental t...

Synthesis of lysine-containing sulphonium salts and their properties as proteinase inhibitors.

Some sulphonium salts derived from lysine were synthesized with the general structure R-Lys-CH2S+-(alkyl)2. They were examined as inhibitors of the cysteine proteinase clostripain, which has a preference for cleaving peptide bonds at the carboxy group of basic amino acids, and of a number of trypsin-related serine proteinases. Clostripain was irreversibly inactivated by all reagents examined, b...

Bivalent DNA Vaccination with Genes Encoding Leishmania major Cysteine Proteinases Type I and II Protects Mice Against Infectious Challenge

Pathways of Insect Protein Digestion: Triatominae (Kissing Bugs)

The majority of insects use serine proteinases like trypsin and chymotrypsin as main enzymes to digest their food [1]. These types of peptidases develop their maximum activity under alkaline to neutral pH conditions [2]. In some insect groups the intestinal lumen is acidic and the digestion switched to cysteine-like proteinases such as cathepsin D or L [3,4]. Some Coleoptera groups (e.g. Bruchi...