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Literature DB >> 18537727

On the edge of validation--cancer protease fibroblast activation protein.

Beni B Wolf¹, Clifford Quan, Thuy Tran, Christian Wiesmann, Daniel Sutherlin.

Abstract

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.

Entities: Disease Gene

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Year: 2008 PMID： 18537727 DOI： 10.2174/138955708784567449

Source DB: PubMed Journal: Mini Rev Med Chem ISSN： 1389-5575 Impact factor: 3.862

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Cited

19 in total

Review 1. The pharmacological landscape and therapeutic potential of serine hydrolases.

Authors: Daniel A Bachovchin; Benjamin F Cravatt
Journal: Nat Rev Drug Discov Date: 2012-01-03 Impact factor: 84.694

2. Targeting the cancer stroma with a fibroblast activation protein-activated promelittin protoxin.

Authors: Aaron M LeBeau; W Nathaniel Brennen; Saurabh Aggarwal; Samuel R Denmeade
Journal: Mol Cancer Ther Date: 2009-05-05 Impact factor: 6.261

3. Fibroblast activation protein-α promotes tumor growth and invasion of breast cancer cells through non-enzymatic functions.

Authors: Yan Huang; Avis E Simms; Anna Mazur; Sophie Wang; Noel R León; Barry Jones; Nazneen Aziz; Thomas Kelly
Journal: Clin Exp Metastasis Date: 2011-05-22 Impact factor: 5.150

4. Selective Inhibitors of Fibroblast Activation Protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine Scaffold.

Authors: Koen Jansen; Leen Heirbaut; Jonathan D Cheng; Jurgen Joossens; Oxana Ryabtsova; Paul Cos; Louis Maes; Anne-Marie Lambeir; Ingrid De Meester; Koen Augustyns; Pieter Van der Veken
Journal: ACS Med Chem Lett Date: 2013-03-18 Impact factor: 4.345

10. Cancer associated fibroblasts promote tumor growth and metastasis by modulating the tumor immune microenvironment in a 4T1 murine breast cancer model.

Authors: Debbie Liao; Yunping Luo; Dorothy Markowitz; Rong Xiang; Ralph A Reisfeld
Journal: PLoS One Date: 2009-11-23 Impact factor: 3.240

On the edge of validation--cancer protease fibroblast activation protein.

Review 1. The pharmacological landscape and therapeutic potential of serine hydrolases.

2. Targeting the cancer stroma with a fibroblast activation protein-activated promelittin protoxin.

3. Fibroblast activation protein-α promotes tumor growth and invasion of breast cancer cells through non-enzymatic functions.

4. Selective Inhibitors of Fibroblast Activation Protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine Scaffold.

Review 5. Stromal biomarkers in breast cancer development and progression.

6. The SUMO1-E67 interacting loop peptide is an allosteric inhibitor of the dipeptidyl peptidases 8 and 9.

7. Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase.

8. Using substrate specificity of antiplasmin-cleaving enzyme for fibroblast activation protein inhibitor design.

9. A potent immunotoxin targeting fibroblast activation protein for treatment of breast cancer in mice.

10. Cancer associated fibroblasts promote tumor growth and metastasis by modulating the tumor immune microenvironment in a 4T1 murine breast cancer model.