Overview of recent drug discovery approaches for new generation leukotriene A(4) hydrolase inhibitors

ÇALIŞKAN B., BANOĞLU E.

EXPERT OPINION ON DRUG DISCOVERY, cilt.8, sa.1, ss.49-63, 2013 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Derleme
  • Cilt numarası: 8 Sayı: 1
  • Basım Tarihi: 2013
  • Doi Numarası: 10.1517/17460441.2013.735228
  • Dergi Adı: EXPERT OPINION ON DRUG DISCOVERY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.49-63
  • Anahtar Kelimeler: aminopeptidase, hydrolase, inflammation, leukotriene A4, leukotriene B4, PGP, BIFUNCTIONAL ENZYME, POTENT INHIBITORS, PHARMACOLOGICAL CHARACTERIZATION, 5-LIPOXYGENASE INHIBITOR, AMINOPEPTIDASE ACTIVITY, SELECTIVE INHIBITOR, CRYSTAL-STRUCTURE, LIPID MEDIATORS, ACID HCL, MECHANISMS
  • Gazi Üniversitesi Adresli: Evet

Özet

Introduction: LTA(4)H is a bifunctional enzyme with hydrolase and aminopeptidase activities. The hydrolase function of this enzyme specifically catalyzes the rate-limiting step in the conversion of LTA(4) to LTB4, one of the most potent chemoattractant and activator of neutrophils. The wealth of in vitro and in vivo data favors in support of LTA(4)H as an appealing target for the discovery and development of anti-inflammatory drugs.