Inhibitors of blood coagulation factor XIII.

Animals Binding Sites Blood Coagulation Cardiovascular Diseases / blood Enzyme Inhibitors / chemistry Factor XIIIa / antagonists & inhibitors Fibrin / metabolism Humans Protein Binding Salivary Proteins and Peptides / chemistry
Blood coagulation cascade FXIIIa FXIIIa inhibitor Transglutaminase Tridegin

Journal

Analytical biochemistry
ISSN: 1096-0309
Titre abrégé: Anal Biochem
Pays: United States
ID NLM: 0370535

Informations de publication

Date de publication:
15 09 2020
Historique:
received: 20 01 2020
revised: 11 03 2020
accepted: 30 03 2020
pubmed: 27 4 2020
medline: 5 2 2021
entrez: 27 4 2020
Statut: ppublish

Résumé

The blood coagulation factor XIII (FXIII) plays an essential role in the stabilization of fibrin clots. This factor, belonging to the class of transglutaminases, catalyzes the final step of secondary hemostasis, i.e. the crosslinking of fibrin polymers. These crosslinks protect the clots against premature fibrinolysis. Consequently, FXIII is an interesting target for the therapeutic treatment of cardiovascular diseases. In this context, inhibitors can influence FXIII in the activation process of the enzyme itself or in its catalytic activity. To date, there is no FXIII inhibitor in medical application, but several studies have been conducted in the past. These studies provided a better understanding of FXIII and identified new lead structures for FXIII inhibitors. Next to small molecule inhibitors, the most promising candidates for the development of clinically applicable FXIII inhibitors are the peptide inhibitors tridegin and transglutaminase-inhibiting Michael acceptors (TIMAs) due to their selectivity towards activated FXIII (FXIIIa). In this review, select FXIII inhibitors and their pharmacological potential are discussed.

Identifiants

DOI: 10.1016/j.ab.2020.113708 PMID: 32335064
pubmed: 32335064
pii: S0003-2697(20)30240-2
doi: 10.1016/j.ab.2020.113708
pii:
doi:

Substances chimiques

Enzyme Inhibitors 0
Salivary Proteins and Peptides 0
tridegin 0
Fibrin 9001-31-4
Factor XIIIa EC 2.3.2.13

Types de publication

Journal Article Research Support, Non-U.S. Gov't Review

Langues

eng

Sous-ensembles de citation

IM

Pagination

113708

Informations de copyright

Copyright © 2020 Elsevier Inc. All rights reserved.

Auteurs

Thomas Schmitz (T)

Pharmaceutical Biochemistry and Bioanalytics, Pharmaceutical Institute, University of Bonn, An der Immenburg 4, D-53121, Bonn, Germany.

Charlotte A Bäuml (CA)

Pharmaceutical Biochemistry and Bioanalytics, Pharmaceutical Institute, University of Bonn, An der Immenburg 4, D-53121, Bonn, Germany.

Diana Imhof (D)

Pharmaceutical Biochemistry and Bioanalytics, Pharmaceutical Institute, University of Bonn, An der Immenburg 4, D-53121, Bonn, Germany. Electronic address: dimhof@uni-bonn.de.

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Inhibitors of blood coagulation factor XIII.
questionsmedicales.fr › Phénomènes chimiques › Phénomènes biochimiques › Sites de fixation › Inhibitors of blood coagulation factor XIII.
questionsmedicales.fr › Phénomènes physiologiques respiratoires et circulatoires › Phénomènes physiogiques du sang › Hémostase › Coagulation sanguine › Inhibitors of blood coagulation factor XIII.
questionsmedicales.fr › Maladies cardiovasculaires › Inhibitors of blood coagulation factor XIII.
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Inhibitors of blood coagulation factor XIII.
questionsmedicales.fr › Facteurs biologiques › Facteurs de la coagulation sanguine › Facteur XIII › Facteur XIIIa › Inhibitors of blood coagulation factor XIII.
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines du sang › Fibrine › Inhibitors of blood coagulation factor XIII.
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Inhibitors of blood coagulation factor XIII.
questionsmedicales.fr › Métabolisme › Liaison aux protéines › Inhibitors of blood coagulation factor XIII.
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines et peptides salivaires › Inhibitors of blood coagulation factor XIII.