On the edge of validation--cancer protease fibroblast activation protein.
Numerous studies implicate the prolyl peptidase, fibroblast activation protein (FAP) in tumorigenesis; however, FAP-selective inhibitors have not yet been developed to fully validate FAP as a therapeutic target. Herein, we review recent efforts aimed at validating and inhibiting FAP for cancer therapy and highlight future directions for successful targeting of this prolyl peptidase.
Wolf
Beni B
BB
Department of Molecular Oncology, Protein Engineering and Medicinal Chemistry, Genentech, Inc., 1 DNA Way-MS42, South San Francisco, CA 94080, USA. bbwolf@gene.com
Quan
Clifford
C
Tran
Thuy
T
Wiesmann
Christian
C
Sutherlin
Daniel
D
D000951:Antigens, Neoplasm / Q000737:chemistry / Q000378:metabolism; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D014408:Biomarkers, Tumor / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D010450:Endopeptidases; D018093:Gelatinases; D006801:Humans; D008565:Membrane Proteins; D009369:Neoplasms / Q000201:enzymology; D012697:Serine Endopeptidases / Q000737:chemistry / Q000378:metabolism; D013379:Substrate Specificity; D000099167:Fibroblast Activation Protein Alpha
D000951:Antigens, Neoplasm; D000970:Antineoplastic Agents; D014408:Biomarkers, Tumor; D010450:Endopeptidases; D018093:Gelatinases; D008565:Membrane Proteins; D012697:Serine Endopeptidases; D000099167:Fibroblast Activation Protein Alpha