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Pregled bibliografske jedinice broj: 1103728

Benzoxaboroles—Novel Autotaxin Inhibitors


Kristina Kraljić; Dubravko Jelić; Dinko Žiher; Adam Cvrtila; Snježana Dragojević Verona Sinkovi´c and Milan Mesi´c
Benzoxaboroles—Novel Autotaxin Inhibitors // Molecules, 24 (2019), 3419-3441 (međunarodna recenzija, članak, ostalo)


CROSBI ID: 1103728 Za ispravke kontaktirajte CROSBI podršku putem web obrasca

Naslov
Benzoxaboroles—Novel Autotaxin Inhibitors

Autori
Kristina Kraljić ; Dubravko Jelić ; Dinko Žiher ; Adam Cvrtila ; Snježana Dragojević Verona Sinkovi´c and Milan Mesi´c

Izvornik
Molecules (1420-3049) 24 (2019); 3419-3441

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, ostalo

Ključne riječi
Autotaxin (ATX) ; lysophosphaditic acid ; benzoxaboroles ; cancer

Sažetak
Autotaxin (ATX) is an extracellular enzyme that hydrolyses lysophosphatidylcholine (LPC) to lysophosphatidic acid (LPA), which has a role in the mediation of inflammation, fibrosis and cancer. ATX is a drug target that has been the focus of many research groups during the last ten years. To date, only one molecule, Ziritaxestat (GLPG1690) has entered the clinic ; it is currently in Phase 3 clinical trials for idiopathic pulmonary fibrosis. Other small molecules, with di erent binding modes, have been investigated as ATX inhibitors for cancer including compounds possessing a boronic acid motif such as HA155. In this work, we targeted new, improved inhibitors of ATX that mimic the important interactions of boronic acid using a benzoxaborole motif as the acidic warhead. Furthermore, we aimed to improve the plasma stability of the new compounds by using a more stable core spacer than that embedded in HA155. Compounds were synthesized, evaluated for their ATX inhibitory activity and ADME properties in vitro, culminating in a new benzoxaborole compound, 37, which retains the ATX inhibition activity of HA155 but has improved ADME properties (plasma protein binding, good kinetic solubility and rat/human plasma stability).

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Interdisciplinarne prirodne znanosti, Interdisciplinarne biotehničke znanosti, Biotehnologija u biomedicini (prirodno područje, biomedicina i zdravstvo, biotehničko područje)



POVEZANOST RADA


Ustanove:
Fidelta d.o.o.

Profili:

Avatar Url Dinko Žiher (autor)

Avatar Url Dubravko Jelić (autor)


Citiraj ovu publikaciju:

Kristina Kraljić; Dubravko Jelić; Dinko Žiher; Adam Cvrtila; Snježana Dragojević Verona Sinkovi´c and Milan Mesi´c
Benzoxaboroles—Novel Autotaxin Inhibitors // Molecules, 24 (2019), 3419-3441 (međunarodna recenzija, članak, ostalo)
Kristina Kraljić, Dubravko Jelić, Dinko Žiher, Adam Cvrtila & Snježana Dragojević Verona Sinkovi´c and Milan Mesi´c (2019) Benzoxaboroles—Novel Autotaxin Inhibitors. Molecules, 24, 3419-3441.
@article{article, year = {2019}, pages = {3419-3441}, keywords = {Autotaxin (ATX), lysophosphaditic acid, benzoxaboroles, cancer}, journal = {Molecules}, volume = {24}, issn = {1420-3049}, title = {Benzoxaboroles—Novel Autotaxin Inhibitors}, keyword = {Autotaxin (ATX), lysophosphaditic acid, benzoxaboroles, cancer} }
@article{article, year = {2019}, pages = {3419-3441}, keywords = {Autotaxin (ATX), lysophosphaditic acid, benzoxaboroles, cancer}, journal = {Molecules}, volume = {24}, issn = {1420-3049}, title = {Benzoxaboroles—Novel Autotaxin Inhibitors}, keyword = {Autotaxin (ATX), lysophosphaditic acid, benzoxaboroles, cancer} }

Časopis indeksira:


  • Current Contents Connect (CCC)
  • Web of Science Core Collection (WoSCC)
    • Science Citation Index Expanded (SCI-EXP)
    • SCI-EXP, SSCI i/ili A&HCI
  • Scopus
  • MEDLINE





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