TY - JOUR
T1 - Towards small-molecule CXCR3 ligands with clinical potential
AU - Wijtmans, M.
AU - Verzijl, D.
AU - Leurs, R.
AU - de Esch, I.J.P.
AU - Smit, M.J.
PY - 2008
Y1 - 2008
N2 - The CXCR3 chemokine receptor was first discovered in 1996 and has been shown to play an important role in several diseases, most of which are related to inflammation. This review describes in detail the development of small CXCR3 ligands and their therapeutic potential. Classes of CXCR3 antagonists with strikingly variable core structures have emerged. Some of these compounds have confirmed the beneficial role of CXCR3 antagonism in animal models of disease. One of the compounds, AMG487, progressed to Phase II clinical trials but has been withdrawn because of lack of efficacy. New antagonist classes are being developed to reveal the full therapeutic potential of CXCR3. © 2008 Wiley-VCH Verlag GmbH & Co. KGaA.
AB - The CXCR3 chemokine receptor was first discovered in 1996 and has been shown to play an important role in several diseases, most of which are related to inflammation. This review describes in detail the development of small CXCR3 ligands and their therapeutic potential. Classes of CXCR3 antagonists with strikingly variable core structures have emerged. Some of these compounds have confirmed the beneficial role of CXCR3 antagonism in animal models of disease. One of the compounds, AMG487, progressed to Phase II clinical trials but has been withdrawn because of lack of efficacy. New antagonist classes are being developed to reveal the full therapeutic potential of CXCR3. © 2008 Wiley-VCH Verlag GmbH & Co. KGaA.
UR - https://www.scopus.com/pages/publications/48149111878
UR - https://www.scopus.com/inward/citedby.url?scp=48149111878&partnerID=8YFLogxK
U2 - 10.1002/cmdc.200700365
DO - 10.1002/cmdc.200700365
M3 - Article
SN - 1860-7179
VL - 3
SP - 861
EP - 872
JO - ChemMedChem
JF - ChemMedChem
IS - 6
ER -
