Discoidin Domains as Emerging Therapeutic Targets

Trends Pharmacol Sci. 2016 Aug;37(8):641-659. doi: 10.1016/j.tips.2016.06.003. Epub 2016 Jun 29.


Discoidin (DS) domains are found in eukaryotic and prokaryotic extracellular and transmembrane multidomain proteins. These small domains play different functional roles and can interact with phospholipids, glycans, and proteins, including collagens. DS domain-containing proteins are often involved in cellular adhesion, migration, proliferation, and matrix-remodeling events, while some play a major role in blood coagulation. Mutations in DS domains have been associated with various disease conditions. This review provides an update on the structure, function, and modulation of the DS domains, with a special emphasis on two circulating blood coagulation cofactors, factor V and factor VIII, and the transmembrane neuropilin receptors that have been targeted for inhibition by biologics and small chemical compounds.

Keywords: blood coagulation; cancer; factor V; factor VIII; neuropilin; structural bioinformatics.

Publication types

  • Review

MeSH terms

  • Blood Coagulation / drug effects
  • Blood Coagulation / physiology
  • Discoidin Domain / physiology*
  • Factor V / antagonists & inhibitors
  • Factor V / chemistry
  • Factor V / physiology*
  • Factor VIII / antagonists & inhibitors
  • Factor VIII / chemistry
  • Factor VIII / physiology*
  • Humans
  • Models, Molecular
  • Molecular Targeted Therapy
  • Neuropilins / antagonists & inhibitors
  • Neuropilins / chemistry
  • Neuropilins / physiology*


  • Neuropilins
  • Factor V
  • Factor VIII