Disclosed are cDNAs and genomic DNAs encoding protease-activated receptor 3 (PAR3) from mouse and human, and the recombinant polypeptides expressed from such cDNAs. The recombinant receptor polypeptides, receptor fragments and analogs expressed on the surface of cells are used in methods of screening candidate compounds for their ability to act as agonists or antagonists to the effects of interaction between thrombin and PAR3. Agonists are used as therapeutics to treat wounds, thrombosis, atherosclerosis, restenosis, inflammation, and other thrombin-activated disorders. Antagonists are used as therapeutics to control blood coagulation and thereby treating heart attack and stroke. Antagonists mediate inflammatory and proliferative responses to injury as occur in normal wound healing and variety of diseases including atherosclerosis, restenosis, pulmonary inflammation (ARDS) and glomerulosclerosis. Antibodies specific for a protease-activated receptor 3 (or receptor fragment or analog) and their use as a therapeutic are also disclosed.

The Regents of the University of California

Protease-activated receptor 3 and uses thereof

DNA encoding a protease-activated receptor 3

The invention provides compositions and methods for treating pulmonary conditions and for reducing the negative effects of pulmonary inflammation. Such compositions and methods employ protease inhibitors and a lung surfactant mixture. The compositions and methods can also include lipase inhibitors (e.g. a phospholipase inhibitors) and anti-oxidants.

The Scripps Research Institute

Compositions for treatment and prevention of pulmonary conditions

A method for treating pulmonary inflammation and alpha-1-antitrypsin deficiencies by the administration of an effective amount of microcrystalline alpha-1-antitrypsin, its salt or derivative by inhalation, alone or with other serine protease inhibitors, and the pharmaceutical compositions thereof.

Treatment of inflammation

4H-3,1-benzoxazin-4-one derivatives represented by formula (I) below: ##STR1## wherein R.sup.1 represents a lower alkyl group, R.sup.2 represents a lower alkyl group, a lower alkylthioalkyl group, or a lower alkanesulfinylalkyl group, R.sup.3 represents a hydrogen atom a hydroxyl group, a lower alkoxy group, or a lower acyloxy group, X represents an amino acid residue selected from the group consisting of alanine, valine, and phenylalanine, n represents an integer of 0, 1, or 2, and Y means a substituent selected from the group consisting of an alkanoyl group having 2 to 6 carbon atoms which may be substituted by a phenyl group, a benzyloxycarbonyl group, a lower alkoxycarbonyl group, a cinnamoyl group, and a methoxysuccinyl group. These derivatives exhibit a strong serine protease inhibiting effect, and are useful as effective components of agents for preventing and curing diseases caused by the excessive effect of serine proteases, e.g., pneumonia, pulmonary emphysema, fibroid lung, bronchitis, arthritis, pancreatitis, nephritis, shock, sepsis, and arteriosclerosis.

pneumonia/protease

Protease-activated receptor 3 and uses thereof

DNA encoding a protease-activated receptor 3

Compositions for treatment and prevention of pulmonary conditions

Treatment of inflammation

4H-3,1-benzoxazin-4-one derivative

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