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Related Experiment Videos

Enzyme-controlling medicines: introduction

S Okamoto1, A Hijikata-Okunomiya, K Wanaka

  • 1Kobe Research Projects on Thrombosis and Haemostasis, Japan.

Seminars in Thrombosis and Hemostasis
|January 1, 1997
PubMed
Summary

Researchers discovered epsilon aminocaproic acid and tranexamic acid to inhibit plasmin. Further work led to argatroban, a selective thrombin inhibitor, showing promise for treating thrombosis.

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Medicinal Chemistry

Background:

  • The physiological role of fibrinolysis was not well-established in the 1950s.
  • Early research focused on identifying plasmin inhibitors.
  • Thrombin was later identified as a key enzyme target for control.

Purpose of the Study:

  • To discover compounds inhibiting plasmin activity.
  • To develop selective thrombin inhibitors through structure-activity relationship studies.
  • To minimize toxicity in drug candidates.

Main Methods:

  • Screening of approximately 200 lysine derivatives.
  • Structure-activity relationship studies using arginine as a scaffold.
  • Optimization of lead compounds to reduce toxicity.

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Main Results:

  • Discovery of epsilon aminocaproic acid (EACA) and tranexamic acid (t-AMCHA).
  • Identification of selective thrombin inhibitor No. 205 and subsequently argatroban (No. 805).
  • Argatroban demonstrated competitive and cofactor-independent thrombin inhibition with high selectivity.

Conclusions:

  • Epsilon aminocaproic acid and tranexamic acid are effective plasmin inhibitors.
  • Argatroban is a highly selective thrombin inhibitor with potential for clinical use in thrombosis treatment.
  • Recent work has identified novel plasmin and kallikrein inhibitors based on prior knowledge.