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.
Department of Molecular Oncology, Protein Engineering and Medicinal Chemistry, Genentech, Inc., 1 DNA Way-MS42, South San Francisco, CA 94080, USA. bbwolf@gene.com
Beni B
BB
Wolf
Clifford
C
Quan
Thuy
T
Tran
Christian
C
Wiesmann
Daniel
D
Sutherlin
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