PMID- 32335064
OWN - NLM
STAT- MEDLINE
DCOM- 20210204
LR  - 20210204
IS  - 1096-0309 (Electronic)
IS  - 0003-2697 (Linking)
VI  - 605
DP  - 2020 Sep 15
TI  - Inhibitors of blood coagulation factor XIII.
PG  - 113708
LID - S0003-2697(20)30240-2 [pii]
LID - 10.1016/j.ab.2020.113708 [doi]
AB  - 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.
CI  - Copyright (c) 2020 Elsevier Inc. All rights reserved.
FAU - Schmitz, Thomas
AU  - Schmitz T
AD  - Pharmaceutical Biochemistry and Bioanalytics, Pharmaceutical Institute, 
      University of Bonn, An der Immenburg 4, D-53121, Bonn, Germany.
FAU - Bauml, Charlotte A
AU  - Bauml CA
AD  - Pharmaceutical Biochemistry and Bioanalytics, Pharmaceutical Institute, 
      University of Bonn, An der Immenburg 4, D-53121, Bonn, Germany.
FAU - Imhof, Diana
AU  - Imhof D
AD  - Pharmaceutical Biochemistry and Bioanalytics, Pharmaceutical Institute, 
      University of Bonn, An der Immenburg 4, D-53121, Bonn, Germany. Electronic 
      address: dimhof@uni-bonn.de.
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Review
DEP - 20200423
PL  - United States
TA  - Anal Biochem
JT  - Analytical biochemistry
JID - 0370535
RN  - 0 (Enzyme Inhibitors)
RN  - 0 (Salivary Proteins and Peptides)
RN  - 0 (tridegin)
RN  - 9001-31-4 (Fibrin)
RN  - EC 2.3.2.13 (Factor XIIIa)
SB  - IM
MH  - Animals
MH  - Binding Sites
MH  - *Blood Coagulation
MH  - Cardiovascular Diseases/*blood
MH  - *Enzyme Inhibitors/chemistry/metabolism
MH  - Factor XIIIa/*antagonists & inhibitors
MH  - Fibrin/metabolism
MH  - Humans
MH  - Protein Binding
MH  - Salivary Proteins and Peptides/chemistry/metabolism
OTO - NOTNLM
OT  - Blood coagulation cascade
OT  - FXIIIa
OT  - FXIIIa inhibitor
OT  - Transglutaminase
OT  - Tridegin
EDAT- 2020/04/27 06:00
MHDA- 2021/02/05 06:00
CRDT- 2020/04/27 06:00
PHST- 2020/01/20 00:00 [received]
PHST- 2020/03/11 00:00 [revised]
PHST- 2020/03/30 00:00 [accepted]
PHST- 2020/04/27 06:00 [pubmed]
PHST- 2021/02/05 06:00 [medline]
PHST- 2020/04/27 06:00 [entrez]
AID - S0003-2697(20)30240-2 [pii]
AID - 10.1016/j.ab.2020.113708 [doi]
PST - ppublish
SO  - Anal Biochem. 2020 Sep 15;605:113708. doi: 10.1016/j.ab.2020.113708. Epub 2020 
      Apr 23.