Fibroblast Activation Protein-α as a Target in the Bench-to-Bedside Diagnosis and Treatment of Tumors: A Narrative Review

Cancer-Associated Fibroblasts as Players in Cancer Development and Progression and Their Role in Targeted Radionuclide Imaging and Therapy

(2021) Sofia Koustoulidou et al.   Cancers

68Ga-DOTA-FAPI-04 PET/MR in the evaluation of gastric carcinomas: comparison with 18F-FDG PET/CT

(2021) Chunxia Qin et al.   JOURNAL OF NUCLEAR MEDICINE

An ultra-high-affinity small organic ligand of fibroblast activation protein for tumor-targeting applications

(2021) Jacopo Millul et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

State-of-the-art of FAPI-PET imaging: a systematic review and meta-analysis

(2021) Martina Sollini et al.   EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING

Chimeric Antigen Receptor T Cell Therapy for Acute Lymphoblastic Leukemia

(2020) Talha Badar et al.   CURRENT TREATMENT OPTIONS IN ONCOLOGY

Molecular recognition of fibroblast activation protein for diagnostic and therapeutic applications

(2020) Adéla Šimková et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

Light-assisted hierarchical intratumoral penetration and programmed antitumor therapy based on tumor microenvironment (TME)-amendatory and self-adaptive polymeric nanoclusters

(2020) Jing Yan et al.   BIOMATERIALS

Recent advances in the development of activatable multifunctional probes for in vivo imaging of caspase-3

(2020) Pengzhan Wang et al.   CHINESE CHEMICAL LETTERS

Reactive oxygen species, thiols and enzymes activable AIEgens from single fluorescence imaging to multifunctional theranostics

(2020) Jun Li et al.   COORDINATION CHEMISTRY REVIEWS

Employment of enhanced permeability and retention effect (EPR): Nanoparticle-based precision tools for targeting of therapeutic and diagnostic agent in cancer

(2019) Dnyaneshwar Kalyane et al.   Materials Science & Engineering C-Materials for Biological Applications

Blockade of fibroblast activation protein in combination with radiation treatment in murine models of pancreatic adenocarcinoma

(2019) Andrew J. Gunderson et al.   PLoS One

Development of novel FAP-targeted radiotracers with improved tumor retention

(2019) Anastasia Loktev et al.   JOURNAL OF NUCLEAR MEDICINE

An Extendable Star-Like Nanoplatform for Functional and Anatomical Imaging-Guided Photothermal Oncotherapy

(2019) Xuexiang Han et al.   ACS Nano

Reshaping Prostate Tumor Microenvironment To Suppress Metastasis via Cancer-Associated Fibroblast Inactivation with Peptide-Assembly-Based Nanosystem

(2019) Jiayan Lang et al.   ACS Nano

IDH-wildtype glioblastomas and grade III/IV IDH-mutant gliomas show elevated tracer uptake in fibroblast activation protein–specific PET/CT

(2019) Manuel Röhrich et al.   EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING

Melanin-dot–mediated delivery of metallacycle for NIR-II/photoacoustic dual-modal imaging-guided chemo-photothermal synergistic therapy

(2019) Yue Sun et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Bioluminescent Probe for Monitoring Endogenous Fibroblast Activation Protein-Alpha

(2019) Yuxing Lin et al.   ANALYTICAL CHEMISTRY

In Situ Self-Assembled Nanofibers Precisely Target Cancer-Associated Fibroblasts for Improved Tumor Imaging

(2019) Xiao-Xiao Zhao et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Theranostics targeting fibroblast activation protein in the tumor stroma: 64Cu and 225Ac labelled FAPI-04 in pancreatic cancer xenograft mouse models

(2019) Tadashi Watabe et al.   JOURNAL OF NUCLEAR MEDICINE

Anti-tumour effects of a xenogeneic fibroblast activation protein-based whole cell tumour vaccine in murine tumour models

(2019) Meihua Chen et al.   Artificial Cells Nanomedicine and Biotechnology

Fibroblastic FAP promotes intrahepatic cholangiocarcinoma growth via MDSCs recruitment

(2019) Yuli Lin et al.   NEOPLASIA

Toxicological profile and safety pharmacology of a single dose of fibroblast activation protein-α-based doxorubicin prodrug

(2018) Sichao Huang et al.   ANTI-CANCER DRUGS

Polyphyllin I inhibits gastric cancer cell proliferation by downregulating the expression of fibroblast activation protein alpha (FAP) and hepatocyte growth factor (HGF) in cancer-associated fibroblasts

(2018) Ruizeng Dong et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Targeting fibroblast activation protein in cancer ndash Prospects and caveats

(2018) Aleksi Sedo   Frontiers in Bioscience-Landmark

Clinical significance of FAP-α on microvessel and lymphatic vessel density in lung squamous cell carcinoma

(2018) Ling Chen et al.   JOURNAL OF CLINICAL PATHOLOGY

Photosensitizer-Encapsulated Ferritins Mediate Photodynamic Therapy against Cancer-Associated Fibroblasts and Improve Tumor Accumulation of Nanoparticles

(2018) Lu Li et al.   MOLECULAR PHARMACEUTICS

Tissue analyses reveal a potential immune-adjuvant function of FAP-1 positive fibroblasts in non-small cell lung cancer

(2018) Thomas Karsten Kilvaer et al.   PLoS One

A novel fibroblast activation protein-targeted near-infrared fluorescent off–on probe for cancer cell detection, in vitro and in vivo imaging

(2018) Jie Xing et al.   Journal of Materials Chemistry B

Introduction of Z-GP scaffold into procarbazine reduces spermatoxicity and myelosuppression

(2018) Rikang Wang et al.   BIOORGANIC CHEMISTRY

A tumor-targeted activatable phthalocyanine-tetrapeptide-doxorubicin conjugate for synergistic chemo-photodynamic therapy

(2017) Mei-Rong Ke et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A novel FAPα-based Z-Gly-Pro epirubicin prodrug for improving tumor-targeting chemotherapy

(2017) Jun Wang et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Fibroblast activation protein-α promotes the growth and migration of lung cancer cells via the PI3K and sonic hedgehog pathways

(2017) Jun Jia et al.   INTERNATIONAL JOURNAL OF MOLECULAR MEDICINE

Pericyte-targeting prodrug overcomes tumor resistance to vascular disrupting agents

(2017) Minfeng Chen et al.   JOURNAL OF CLINICAL INVESTIGATION

Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity

(2017) Li-Juan Deng et al.   JOURNAL OF MEDICINAL CHEMISTRY

In Vivo Antitumoral Efficacy of PhAc-ALGP-Doxorubicin, an Enzyme-Activated Doxorubicin Prodrug, in Patient-Derived Soft Tissue Sarcoma Xenograft Models

(2017) Jasmien Cornillie et al.   MOLECULAR CANCER THERAPEUTICS

Protein Nanocage Mediated Fibroblast-Activation Protein Targeted Photoimmunotherapy To Enhance Cytotoxic T Cell Infiltration and Tumor Control

(2017) Zipeng Zhen et al.   NANO LETTERS

Fibroblast Activation Protein-α-Positive Fibroblasts Promote Gastric Cancer Progression and Resistance to Immune Checkpoint Blockade

(2017) Xuyang Wen et al.   ONCOLOGY RESEARCH

Roles of Fibroblast Activation Protein and Hepatocyte Growth Factor Expressions in Angiogenesis and Metastasis of Gastric Cancer

(2017) Li-Ming Gao et al.   PATHOLOGY & ONCOLOGY RESEARCH

The prognostic significance of cancer-associated fibroblasts in pancreatic ductal adenocarcinoma

(2017) Hyunjin Park et al.   TUMOR BIOLOGY

Cancer-associated fibroblasts enhance metastatic potential of lung cancer cells through IL-6/STAT3 signaling pathway

(2017) Limin Wang et al.   Oncotarget

FAP Promotes Immunosuppression by Cancer-Associated Fibroblasts in the Tumor Microenvironment via STAT3–CCL2 Signaling

(2016) Xuguang Yang et al.   CANCER RESEARCH

Cut to the chase: a review of CD26/dipeptidyl peptidase-4's (DPP4) entanglement in the immune system

(2016) C. Klemann et al.   CLINICAL AND EXPERIMENTAL IMMUNOLOGY

Fibroblast Activation Protein Cleaves and Inactivates Fibroblast Growth Factor 21

(2016) Diana Ronai Dunshee et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Targeting of cancer-associated fibroblasts enhances the efficacy of cancer chemotherapy by regulating the tumor microenvironment

(2016) MINMIN LI et al.   Molecular Medicine Reports

Iterative design of emetine-based prodrug targeting fibroblast activation protein (FAP) and dipeptidyl peptidase IV DPPIV using a tandem enzymatic activation strategy

(2016) Emmanuel S. Akinboye et al.   PROSTATE

Fibroblast activation protein alpha is expressed by transformed and stromal cells and is associated with mesenchymal features in glioblastoma

(2016) Petr Busek et al.   TUMOR BIOLOGY

Activation of the A2B adenosine receptor in B16 melanomas induces CXCL12 expression in FAP-positive tumor stromal cells, enhancing tumor progression

(2016) Claudia Sorrentino et al.   Oncotarget

Transformable Peptide Nanocarriers for Expeditious Drug Release and Effective Cancer Therapy via Cancer-Associated Fibroblast Activation

(2015) Tianjiao Ji et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Fibroblast activation protein-α-expressing fibroblasts promote the progression of pancreatic ductal adenocarcinoma

(2015) Tomoya Kawase et al.   BMC GASTROENTEROLOGY

Depletion of Carcinoma-Associated Fibroblasts and Fibrosis Induces Immunosuppression and Accelerates Pancreas Cancer with Reduced Survival

(2015) Berna C. Özdemir et al.   CANCER CELL

Mixed nanomicelles as potential carriers for systemic delivery of Z-GP-Dox, an FAPα-based doxorubicin prodrug: formulation and pharmacokinetic evaluation

(2015) Baojian Wu et al.   International Journal of Nanomedicine

Evaluation of the Radiolabeled Boronic Acid-Based FAP Inhibitor MIP-1232 for Atherosclerotic Plaque Imaging

(2015) Romana Meletta et al.   MOLECULES

Chimeric antigen receptor T cells: power tools to wipe out leukemia and lymphoma

(2015) Tobias Riet et al.   Expert Review of Hematology

Expression levels of seprase/FAPα and DPPIV/CD26 in epithelial ovarian carcinoma

(2015) MENGZHEN ZHANG et al.   Oncology Letters

Cancer Associated Fibroblasts in Stage I-IIIA NSCLC: Prognostic Impact and Their Correlations with Tumor Molecular Markers

(2015) Thomas K. Kilvaer et al.   PLoS One

Targeting Inhibition of Fibroblast Activation Protein-α and Prolyl Oligopeptidase Activities on Cells Common to Metastatic Tumor Microenvironments

(2015) Victoria J. Christiansen et al.   NEOPLASIA

FAP-α (Fibroblast activation protein-α) is involved in the control of human breast cancer cell line growth and motility via the FAK pathway

(2014) Jun Jia et al.   BMC CELL BIOLOGY

miR-21 Induces Myofibroblast Differentiation and Promotes the Malignant Progression of Breast Phyllodes Tumors

(2014) C. Gong et al.   CANCER RESEARCH

In vivo near-infrared fluorescence imaging of FAP-expressing tumors with activatable FAP-targeted, single-chain Fv-immunoliposomes

(2014) Ronny Rüger et al.   JOURNAL OF CONTROLLED RELEASE

Fibroblast Activation Protein (FAP) Is Essential for the Migration of Bone Marrow Mesenchymal Stem Cells through RhoA Activation

(2014) Kuei-Min Chung et al.   PLoS One

Downregulation of FAP suppresses cell proliferation and metastasis through PTEN/PI3K/AKT and Ras-ERK signaling in oral squamous cell carcinoma

(2014) H Wang et al.   Cell Death & Disease

Over-expression of fibroblast activation protein alpha increases tumor growth in xenografts of ovarian cancer cells

(2013) L. Yang et al.   ACTA BIOCHIMICA ET BIOPHYSICA SINICA

Challenges and Key Considerations of the Enhanced Permeability and Retention Effect for Nanomedicine Drug Delivery in Oncology

(2013) U. Prabhakar et al.   CANCER RESEARCH

Depletion of stromal cells expressing fibroblast activation protein-α from skeletal muscle and bone marrow results in cachexia and anemia

(2013) Edward W. Roberts et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Immune targeting of fibroblast activation protein triggers recognition of multipotent bone marrow stromal cells and cachexia

(2013) Eric Tran et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Treatment of malignant pleural mesothelioma by fibroblast activation protein-specific re-directed T cells

(2013) Petra C Schuberth et al.   Journal of Translational Medicine

Antitumor Effects of Chimeric Receptor Engineered Human T Cells Directed to Tumor Stroma

(2013) Sunitha Kakarla et al.   MOLECULAR THERAPY

Val-BoroPro Accelerates T Cell Priming via Modulation of Dendritic Cell Trafficking Resulting in Complete Regression of Established Murine Tumors

(2013) Meghaan P. Walsh et al.   PLoS One

Targeting CXCL12 from FAP-expressing carcinoma-associated fibroblasts synergizes with anti-PD-L1 immunotherapy in pancreatic cancer

(2013) C. Feig et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

High intratumoral expression of fibroblast activation protein (FAP) in colon cancer is associated with poorer patient prognosis

(2013) Maria L. Wikberg et al.   TUMOR BIOLOGY

Targeting Fibroblast Activation Protein in Tumor Stroma with Chimeric Antigen Receptor T Cells Can Inhibit Tumor Growth and Augment Host Immunity without Severe Toxicity

(2013) L.-C. S. Wang et al.   Cancer Immunology Research

Activatable Near-Infrared Fluorescent Probe for In Vivo Imaging of Fibroblast Activation Protein-alpha

(2012) Jinbo Li et al.   BIOCONJUGATE CHEMISTRY

Fibroblast activation protein

(2012) Rui Liu et al.   CANCER BIOLOGY & THERAPY

Identification of inhibitory scFv antibodies targeting fibroblast activation protein utilizing phage display functional screens

(2012) Jiping Zhang et al.   FASEB JOURNAL

Fibroblast activation protein regulates tumor-associated fibroblasts and epithelial ovarian cancer cells

(2012) DONGMEI LAI et al.   INTERNATIONAL JOURNAL OF ONCOLOGY

Rationale Behind Targeting Fibroblast Activation Protein-Expressing Carcinoma-Associated Fibroblasts as a Novel Chemotherapeutic Strategy

(2012) W. N. Brennen et al.   MOLECULAR CANCER THERAPEUTICS

Expression of fibroblast activation protein in human pancreatic adenocarcinoma and its clinicopathological significance

(2012) Min Shi   WORLD JOURNAL OF GASTROENTEROLOGY

Ovarian cancer-associated fibroblasts contribute to epithelial ovarian carcinoma metastasis by promoting angiogenesis, lymphangiogenesis and tumor cell invasion

(2011) Yuan Zhang et al.   CANCER LETTERS

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

(2011) Yan Huang et al.   CLINICAL & EXPERIMENTAL METASTASIS

Expression and role of fibroblast activation protein-alpha in microinvasive breast carcinoma

(2011) Xing Hua et al.   Diagnostic Pathology

Neuropeptide Y, B-type natriuretic peptide, substance P and peptide YY are novel substrates of fibroblast activation protein-α

(2011) Fiona M. Keane et al.   FEBS Journal

Cleavage-site specificity of prolyl endopeptidase FAP investigated with a full-length protein substrate

(2011) Chih-Hsiang Huang et al.   JOURNAL OF BIOCHEMISTRY

Chemical and Biological Evaluation of Dipeptidyl Boronic Acid Proteasome Inhibitors for Use in Prodrugs and Pro-Soft Drugs Targeting Solid Tumors

(2011) Lawrence J. Milo et al.   JOURNAL OF MEDICINAL CHEMISTRY

Expression and role of the cell surface protease seprase/fibroblast activation protein-α (FAP-α) in astroglial tumors

(2010) Rolf Mentlein et al.   BIOLOGICAL CHEMISTRY

Immunotherapy targeting fibroblast activation protein inhibits tumor growth and increases survival in a murine colon cancer model

(2010) Yuan Wen et al.   CANCER SCIENCE

Suppression of Antitumor Immunity by Stromal Cells Expressing Fibroblast Activation Protein- 

(2010) M. Kraman et al.   SCIENCE

Targeting fibroblast activation protein inhibits tumor stromagenesis and growth in mice

(2009) Angélica M. Santos et al.   JOURNAL OF CLINICAL INVESTIGATION

Fibroblast Activation Protein and Its Relationship to Clinical Outcome in Pancreatic Adenocarcinoma

(2009) Steven J. Cohen et al.   PANCREAS

Molecular Characterization of Human Breast Tumor Vascular Cells

(2008) Rajendra Bhati et al.   AMERICAN JOURNAL OF PATHOLOGY

Fibroblast Activation Protein Peptide Substrates Identified from Human Collagen I Derived Gelatin Cleavage Sites†

(2007) Saurabh Aggarwal et al.   BIOCHEMISTRY