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On the edge of validation--cancer protease fibroblast activation protein
Beni B Wolf1, Clifford Quan, Thuy Tran
1Department of Molecular Oncology, Protein Engineering and Medicinal Chemistry, Genentech, Inc., 1 DNA Way-MS42, South San Francisco, CA 94080, USA. bbwolf@gene.com
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.
Insights
Fibroblast activation protein (FAP) is implicated in cancer, but FAP-selective inhibitors are needed. This review covers recent progress in developing FAP inhibitors for cancer therapy and future research directions.
Area of Science:
- Biochemistry
- Oncology
- Drug Discovery
Background:
- Fibroblast activation protein (FAP) is a prolyl peptidase enzyme implicated in various stages of tumorigenesis.
- Despite its role in cancer, the lack of FAP-selective inhibitors has hindered its validation as a therapeutic target.
- Understanding FAP's function is crucial for developing effective cancer treatments.
Purpose of the Study:
- To review recent advancements in the development of fibroblast activation protein (FAP)-selective inhibitors.
- To discuss the progress made in validating FAP as a therapeutic target for cancer treatment.
- To highlight future research directions for successful FAP-targeted cancer therapy.
Main Methods:
- Literature review of recent studies on fibroblast activation protein (FAP) inhibitors.
- Analysis of research efforts focused on validating FAP as a therapeutic target.
- Synthesis of current findings and future perspectives in FAP-targeted cancer therapy.
Main Results:
- Recent research has focused on developing selective inhibitors for fibroblast activation protein (FAP).
- Progress has been made in validating FAP's role in cancer, paving the way for targeted therapies.
- Several strategies are being explored to effectively inhibit FAP for therapeutic benefit.
Conclusions:
- Fibroblast activation protein (FAP) inhibitors represent a promising avenue for cancer therapy.
- Further development of FAP-selective inhibitors is essential for clinical translation.
- Targeting FAP holds significant potential for improving outcomes in cancer patients.
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