Currently, two ways are used to develop active ligands for metzincins: 1- targeting their active CDs or Exos with small molecules; 2- targeting with antibodies their CDs or Exo domains or either. Nowadays the major efforts in this Medicinal Chemistry field are directed to the inhibitors of active forms of CD and many families of structurally differentiated ligands have been disclosed. Anyway there are only few inhibitors that are in clinical trials such as Col-3 or more recently INCB7839, an ADAM- 17 inhibitor (phase II clinical trials for breast cancer, solid tumors and non Hodgkin’s Limphomas). see file in attach
A Medicinal Chemistry Approach to Synthetic Inhibitors of ADAM-10 and ADAM-17
ROSSELLO, ARMANDO
2016-01-01
Abstract
Currently, two ways are used to develop active ligands for metzincins: 1- targeting their active CDs or Exos with small molecules; 2- targeting with antibodies their CDs or Exo domains or either. Nowadays the major efforts in this Medicinal Chemistry field are directed to the inhibitors of active forms of CD and many families of structurally differentiated ligands have been disclosed. Anyway there are only few inhibitors that are in clinical trials such as Col-3 or more recently INCB7839, an ADAM- 17 inhibitor (phase II clinical trials for breast cancer, solid tumors and non Hodgkin’s Limphomas). see file in attachFile in questo prodotto:
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