[Natural and synthetic inhibitors of thrombin. II. Synthetic low-molecular-weight inhibitors].
The up-to-date problems, concerning the structure and properties of two types of inhibitors are reviewed. It is particularly considered properties of low-molecular weight thrombin inhibitors that have electrophilic groups capable to react with Ser-195 of thrombin (peptidyl-chloromethyl ketones, aldehydes, ketomethylene derivatives and derivatives of boric and phosphoric acids) and the competitive reversible thrombin inhibitors. The review focuses on methods of modification of the structure in the natural inhibitors and design of new peptidomimetics. The prospects for prophylaxis and treatment of diverse thromboembolic diseases are discussed.
Kibirev
V K
VK
Institute of Bioorganic Chemistry and Petrolchemistry, National Academy of Sciences of Ukraine, Kyiv.
Gershkovich
A A
AA
D000991:Antithrombins / Q000494:pharmacology / Q000502:physiology*; D001665:Binding Sites; D005343:Fibrinolytic Agents / Q000494:pharmacology*; D006801:Humans; D008970:Molecular Weight; D013329:Structure-Activity Relationship; D013923:Thromboembolism / Q000628:therapy
D000991:Antithrombins; D005343:Fibrinolytic Agents