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Targeting Ligand Cleavage to Inhibit the ErbB Pathway in Cancer
Author(s) -
ZHOU BINBING S.
Publication year - 2005
Publication title -
annals of the new york academy of sciences
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.712
H-Index - 248
eISSN - 1749-6632
pISSN - 0077-8923
DOI - 10.1196/annals.1339.022
Subject(s) - disintegrin , erbb , proteases , metalloproteinase , chemistry , transmembrane protein , signal transduction , microbiology and biotechnology , receptor , extracellular , matrix metalloproteinase , cancer research , biochemistry , biology , enzyme
A bstract : ADAMs (a disintegrin and metalloproteases) are zinc‐dependent transmembrane metalloproteases that shed the extracellular domains of membrane‐bound growth factors, cytokines, and receptors. Recently, ADAMs have emerged in ErbB signaling pathways as sheddases or multiple ErbB ligands. As the ErbB pathway is a validated target for anticancer drugs, upstream activators of ErbB ligands, their sheddases, become new drug targets in the ErbB pathway. We have identified selective small molecule inhibitors of ADAM proteases that block shedding and activation of multiple ErbB ligands, and we are planning to test the compounds in the clinic.