Human leukocyte and porcine pancreatic elastase: X-ray crystal structures, mechanism, substrate specificity, and mechanism-based inhibitors

Journal Article · Tue Mar 07 04:00:00 EST 1989 · Biochemistry; (USA)

DOI:https://doi.org/10.1021/bi00431a001· OSTI ID:5648172

Bode, W; Meyer, E Jr; Powers, J C ^[1]

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1. Max-Planck-Institut fur Biochemie, Martinsried (West Germany)

The serine protease family of enzymes is one of the most widely studied group of enzymes, as evidenced by the fact that more crystal structures are available for individuals of this superfamily than for any other homologous group of enzymes. These enzymes contain a conserved triad of catalytic residues including Ser-195, His-57, and Asp-102. The active-site serine is very nucleophilic, and serine proteases are inhibited by specific serine protease reagents such as diisopropyl phosphorofluoridate (DFP), phenylmethanesulfonyl fluoride, and 3,4-dichloroisocoumarin. Elastases are a group of proteases that possess the ability to cleave the important connective tissue protein elastin. Elastin has the unique property of elastic recoil, is widely distributed in vertebrate tissue, and is particularly abundant in the lungs, arteries, skin, and ligaments. Human neutrophil elastase and pancreatic elastase are two major serine proteases that cleave elastin. Neutrophil elastase is found in the dense granules of polymorphonuclear leukycytes and is essential for phagocytosis and defense against infection by invading microorganisms. Pancreatic elastase is stored as an inactive zymogen in the pancreas and is secreted into the intestines where it becomes activated by trypsin and then participates in digestion. Both elastases cleave substrates at peptide bonds where the P{sub 1} residue is an amino acid residue with a small alkyl side chain.

• OSTI ID: 5648172
• Journal Information: Biochemistry; (USA), Journal Name: Biochemistry; (USA) Vol. 28:5; ISSN 0006-2960; ISSN BICHA
• Country of Publication: United States
• Language: English

Related Subjects

550602* -- Medicine-- External Radiation in Diagnostics-- (1980-)
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMALS
BIOLOGICAL FUNCTIONS
BIOLOGICAL MATERIALS
BLOOD
BLOOD CELLS
BODY
BODY FLUIDS
COHERENT SCATTERING
CRYSTALLOGRAPHY
DIFFRACTION
DIGESTIVE SYSTEM
ENDOCRINE GLANDS
ENZYME ACTIVITY
ENZYME INHIBITORS
ENZYMES
FUNCTIONS
GLANDS
HYDROLASES
LEUKOCYTES
MAMMALS
MAN
MATERIALS
ORGANS
PANCREAS
PEPTIDE HYDROLASES
PRIMATES
SCATTERING
SERINE PROTEINASES
VERTEBRATES
X-RAY DIFFRACTION