Ecto-nucleotidase inhibitors

Recent developments in drug discovery

Research output: Contribution to journalArticle

18 Citations (Scopus)

Abstract

Ecto-nucleotidases are nucleotide metabolizing enzymes that are divided into four different families; nucleoside triphosphate diphosphohydrolases (NTPDases), ecto-5′-nucleotidase (ecto-5′-NT), nucleotide pyrophosphatase/phosphodiesterases (NPPs), and alkaline phosphatases (APs). These enzymes are responsible for the hydrolysis of nucleotidases (nucleoside 5′-triphosphates, 5′-diphosphates and 5′-monophosphates). Ecto-nucleotidases modulate P1- and P2-receptor-mediated signaling. Alterations in extracellular nucleotide and adenosine level can increase or decrease P1 and P2 activity. Potent and selective ligands for certain ectonucleotidase are important as pharmacological tools to investigate the (patho)physiological roles of these enzymes. Furthermore, such ligands are required to study their potential as novel drugs, e.g., as immunomodulatory agents, for the treatment of cancer, cardiovascular or central nervous system disorders. Hence, this review aims to provide an overview of ecto-nucleotidases inhibitors developed so far.

Original languageEnglish
Pages (from-to)21-33
Number of pages13
JournalMini-Reviews in Medicinal Chemistry
Volume15
Issue number1
Publication statusPublished - May 1 2015

Fingerprint

Diphosphates
Drug Discovery
Nucleosides
nucleotide pyrophosphatase
Enzymes
Nucleotides
Ligands
Central Nervous System Diseases
Phosphoric Diester Hydrolases
Adenosine
Alkaline Phosphatase
triphosphoric acid
Hydrolysis
Pharmacology
Pharmaceutical Preparations
Neoplasms

Keywords

  • ALPase
  • Cancer
  • CD39
  • CD73
  • E-NTPDase
  • Ecto-ATPase
  • Ectonucleotidases
  • ENPP
  • Platelet

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

Cite this

Ecto-nucleotidase inhibitors : Recent developments in drug discovery. / Baqi, Younis.

In: Mini-Reviews in Medicinal Chemistry, Vol. 15, No. 1, 01.05.2015, p. 21-33.

Research output: Contribution to journalArticle

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