On the edge of validation - Cancer protease fibroblast activation protein

被引:31
作者
Wolf, Beni B. [1 ,2 ,3 ]
Quan, Clifford [1 ,2 ,3 ]
Tran, Thuy [1 ,2 ,3 ]
Wiesmann, Christian [1 ,2 ,3 ]
Sutherlin, Daniel [1 ,2 ,3 ]
机构
[1] Genentech Inc, Dept Mol Oncol, San Francisco, CA 94080 USA
[2] Genentech Inc, Dept Prot Engn, San Francisco, CA 94080 USA
[3] Genentech Inc, Dept Med Chem, San Francisco, CA 94080 USA
关键词
FAP; DPP4; dipeptidyl peptidase; prolyl peptidase; inhibitor; cancer;
D O I
10.2174/138955708784567449
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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.
引用
收藏
页码:719 / 727
页数:9
相关论文
共 58 条
[1]   Cloning, expression and chromosomal localization of a novel human dipeptidyl peptidase (DPP) IV homolog, DPP8 [J].
Abbott, CA ;
Yu, DMT ;
Woollatt, E ;
Sutherland, GR ;
McCaughan, GW ;
Gorrell, MD .
EUROPEAN JOURNAL OF BIOCHEMISTRY, 2000, 267 (20) :6140-6150
[2]   Fibroblast activation protein:: a serine protease expressed at the remodeling interface in idiopathic pulmonary flbrosis [J].
Acharya, PS ;
Zukas, A ;
Chandan, V ;
Katzenstein, ALA ;
Puré, E .
HUMAN PATHOLOGY, 2006, 37 (03) :352-360
[3]   PT-100, a small molecule dipeptidyl peptidase inhibitorg has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism [J].
Adams, S ;
Miller, GT ;
Jesson, MI ;
Watanabe, T ;
Jones, B ;
Wallner, BP .
CANCER RESEARCH, 2004, 64 (15) :5471-5480
[4]   Structural and kinetic analysis of the substrate specificity of human fibroblast activation protein α [J].
Aertgeerts, K ;
Levin, I ;
Shi, LH ;
Snell, GP ;
Jennings, A ;
Prasad, GS ;
Zhang, YM ;
Kraus, ML ;
Salakian, S ;
Sridhar, V ;
Wijnands, R ;
Tennant, MG .
JOURNAL OF BIOLOGICAL CHEMISTRY, 2005, 280 (20) :19441-19444
[5]   Dipeptidyl peptidase 9 has two forms, a broad tissue distribution, cytoplasmic localization and DPIV-like peptidase activity [J].
Ajami, K ;
Abbott, CA ;
McCaughan, GW ;
Gorrell, MD .
BIOCHIMICA ET BIOPHYSICA ACTA-GENE STRUCTURE AND EXPRESSION, 2004, 1679 (01) :18-28
[6]  
[Anonymous], 2004, SYST BIODIVERS, DOI DOI 10.1017/S1477200003001245
[7]   2-cyanopyrrolidides as potent, stable inhibitors of dipeptidyl peptidase IV [J].
Ashworth, DM ;
Atrash, B ;
Baker, GR ;
Baxter, AJ ;
Jenkins, PD ;
Jones, DM ;
Szelke, M .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1996, 6 (10) :1163-1166
[8]  
BACHOVCHIN WW, 2007, Patent No. 2007005991
[9]   Fibroblast activation protein is expressed by rheumatoid myofibroblast-like synoviocytes [J].
Bauer, Stefan ;
Jendro, Michael C. ;
Wadle, Andreas ;
Kleber, Sascha ;
Stenner, Frank ;
Dinser, Robert ;
Reich, Anja ;
Faccin, Erica ;
Goedde, Stefan ;
Dinges, Harald ;
Mueller-Ladner, Ulf ;
Renner, Christoph .
ARTHRITIS RESEARCH & THERAPY, 2006, 8 (06)
[10]   Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin [J].
Biftua, Tesfaye ;
Scapin, Giovanna ;
Singh, Suresh ;
Feng, Dennis ;
Becker, Joe W. ;
Eiermann, George ;
He, Hualbing ;
Lyons, Kathy ;
Patel, Sangita ;
Petrov, Aleksandr ;
Sinha-Roy, Ranabir ;
Zhang, Bei ;
Wu, Joseph ;
Zhang, Xiaoping ;
Doss, George A. ;
Thornberry, Nancy A. ;
Weber, Ann E. .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (12) :3384-3387