Fibroblast activation protein-α in fibrogenic disorders and cancer: more than a prolyl-specific peptidase?

Anti-tumor effects of DNA vaccine targeting human fibroblast activation protein α by producing specific immune responses and altering tumor microenvironment in the 4T1 murine breast cancer model

(2016) Qiu Xia et al.   CANCER IMMUNOLOGY IMMUNOTHERAPY

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

(2016) Xuguang Yang et al.   CANCER RESEARCH

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

Cleavage of Type I Collagen by Fibroblast Activation Protein-α Enhances Class A Scavenger Receptor Mediated Macrophage Adhesion

(2016) Anna Mazur et al.   PLoS One

A multi-antigen vaccine in combination with an immunotoxin targeting tumor-associated fibroblast for treating murine melanoma

(2016) Jinxu Fang et al.   Molecular Therapy-Oncolytics

Human FGF-21 Is a Substrate of Fibroblast Activation Protein

(2016) Andrew L. Coppage et al.   PLoS One

Specific inhibition of fibroblast activation protein (FAP)-alpha prevents tumor progression in vitro

(2015) Volker Teichgräber et al.   Advances in Medical Sciences

A Randomized, Placebo-controlled Trial of Roflumilast. Effect on Proline-Glycine-Proline and Neutrophilic Inflammation in Chronic Obstructive Pulmonary Disease

(2015) J. Michael Wells et al.   AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE

Circulating FGF21 proteolytic processing mediated by fibroblast activation protein

(2015) E. Y. Zhen et al.   BIOCHEMICAL JOURNAL

The Dipeptidyl Peptidases 4, 8, and 9 in Mouse Monocytes and Macrophages: DPP8/9 Inhibition Attenuates M1 Macrophage Activation in Mice

(2015) Yannick Waumans et al.   INFLAMMATION

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

(2015) Jinxu Fang et al.   INTERNATIONAL JOURNAL OF CANCER

Fibroblast Activation Protein (FAP) Accelerates Collagen Degradation and Clearance from Lungs in Mice

(2015) Ming-Hui Fan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Prolyl Oligopeptidase Enhances α-Synuclein Dimerization via Direct Protein-Protein Interaction

(2015) Mari H. Savolainen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Functionalized bismuth ferrite harmonic nanoparticles for cancer cells labeling and imaging

(2015) Solène Passemard et al.   JOURNAL OF NANOPARTICLE RESEARCH

Fibroblast activation protein-α, a stromal cell surface protease, shapes key features of cancer associated fibroblasts through proteome and degradome alterations

(2015) M.M. Koczorowska et al.   Molecular Oncology

Fibrosis — A Common Pathway to Organ Injury and Failure

(2015) Don C. Rockey et al.   NEW ENGLAND JOURNAL OF MEDICINE

Therapeutic targets for treating fibrotic kidney diseases

(2015) So-Young Lee et al.   Translational Research

The Dipeptidyl Peptidase Family, Prolyl Oligopeptidase, and Prolyl Carboxypeptidase in the Immune System and Inflammatory Disease, Including Atherosclerosis

(2015) Yannick Waumans et al.   Frontiers in Immunology

Suppression of Tumor Growth in Mice by Rationally Designed Pseudopeptide Inhibitors of Fibroblast Activation Protein and Prolyl Oligopeptidase

(2015) Kenneth W. Jackson et al.   NEOPLASIA

The matrikine N- -PGP couples extracellular matrix fragmentation to endothelial permeability

(2015) C. S. Hahn et al.   Science Advances

A rare variant in human fibroblast activation protein associated with ER stress, loss of enzymatic function and loss of cell surface localisation

(2014) Brenna Osborne et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

Linagliptin-Mediated DPP-4 Inhibition Ameliorates Kidney Fibrosis in Streptozotocin-Induced Diabetic Mice by Inhibiting Endothelial-to-Mesenchymal Transition in a Therapeutic Regimen

(2014) Keizo Kanasaki et al.   DIABETES

Diverse functions of matrix metalloproteinases during fibrosis

(2014) M. Giannandrea et al.   Disease Models & Mechanisms

A Novel Proteolytic Cascade Generates an Extracellular Matrix-Derived Chemoattractant in Chronic Neutrophilic Inflammation

(2014) A. Gaggar et al.   JOURNAL OF IMMUNOLOGY

Extended Structure–Activity Relationship and Pharmacokinetic Investigation of (4-Quinolinoyl)glycyl-2-cyanopyrrolidine Inhibitors of Fibroblast Activation Protein (FAP)

(2014) Koen Jansen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Understanding fibroblast activation protein (FAP): Substrates, activities, expression and targeting for cancer therapy

(2014) Elizabeth J. Hamson et al.   Proteomics Clinical Applications

Selective inhibitors of fibroblast activation protein (FAP) with a xanthine scaffold

(2014) Koen Jansen et al.   MedChemComm

N-acetyl-seryl-aspartyl-lysyl-proline: a valuable endogenous anti-fibrotic peptide for combating kidney fibrosis in diabetes

(2014) Keizo Kanasaki et al.   Frontiers in Pharmacology

Overview of the cellular and molecular basis of kidney fibrosis

(2014) Allison A. Eddy   Kidney International Supplements

Short hairpin RNA targeting of fibroblast activation protein inhibits tumor growth and improves the tumor microenvironment in a mouse model

(2013) Fan Cai et al.   BMB Reports

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

Identification of Selective and Potent Inhibitors of Fibroblast Activation Protein and Prolyl Oligopeptidase

(2013) Sarah E. Poplawski et al.   JOURNAL OF MEDICINAL CHEMISTRY

Dipeptidyl Peptidase IV and Its Inhibitors: Therapeutics for Type 2 Diabetes and What Else?

(2013) Lucienne Juillerat-Jeanneret   JOURNAL OF MEDICINAL CHEMISTRY

Understanding the origin, activation and regulation of matrix-producing myofibroblasts for treatment of fibrotic disease

(2013) Rafael Kramann et al.   JOURNAL OF PATHOLOGY

Thymosin β4 and its degradation product, Ac-SDKP, are novel reparative factors in renal fibrosis

(2013) Yiqin Zuo et al.   KIDNEY INTERNATIONAL

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

(2013) Sunitha Kakarla et al.   MOLECULAR THERAPY

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

(2013) Koen Jansen et al.   ACS Medicinal Chemistry Letters

Quantitation of fibroblast activation protein (FAP)-specific protease activity in mouse, baboon and human fluids and organs

(2013) Fiona M. Keane et al.   FEBS Open Bio

Molecular dynamics, crystallography and mutagenesis studies on the substrate gating mechanism of prolyl oligopeptidase

(2012) Karol Kaszuba et al.   BIOCHIMIE

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

(2012) Jinbo Li et al.   BIOCONJUGATE CHEMISTRY

Acylated Gly-(2-cyano)pyrrolidines as inhibitors of fibroblast activation protein (FAP) and the issue of FAP/prolyl oligopeptidase (PREP)-selectivity

(2012) Oxana Ryabtsova et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Comparative analysis of the substrate preferences of two post-proline cleaving endopeptidases, prolyl oligopeptidase and fibroblast activation protein α

(2012) Kalyani Jambunathan et al.   FEBS LETTERS

Virtual Screening and Computational Optimization for the Discovery of Covalent Prolyl Oligopeptidase Inhibitors with Activity in Human Cells

(2012) Stéphane De Cesco et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting Carcinoma-Associated Fibroblasts Within the Tumor Stroma With a Fibroblast Activation Protein-Activated Prodrug

(2012) W. N. Brennen et al.   JNCI-Journal of the National Cancer Institute

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

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

Mechanisms of fibrosis: therapeutic translation for fibrotic disease

(2012) Thomas A Wynn et al.   NATURE MEDICINE

FAP-overexpressing fibroblasts produce an extracellular matrix that enhances invasive velocity and directionality of pancreatic cancer cells

(2011) Hyung-Ok Lee et al.   BMC CANCER

A new tumor vaccine: FAPτ-MT elicits effective antitumor response by targeting indolamine2,3-dioxygenase in antigen presenting cells

(2011) Yan-Mei Yi et al.   CANCER BIOLOGY & THERAPY

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

Fibroblast activation protein is induced by inflammation and degrades type I collagen in thin-cap fibroatheromata

(2011) Chad E. Brokopp et al.   EUROPEAN HEART JOURNAL

Low molecular weight inhibitors of Prolyl Oligopeptidase: a review of compounds patented from 2003 to 2010

(2011) Abraham López et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

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

Role of a propeller loop in the quaternary structure and enzymatic activity of prolyl dipeptidases DPP-IV and DPP9

(2011) Hung-Kuan Tang et al.   FEBS LETTERS

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

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

Use of Umbrella Sampling to Calculate the Entrance/Exit Pathway for Z-Pro-Prolinal Inhibitor in Prolyl Oligopeptidase

(2011) Jean-François St-Pierre et al.   Journal of Chemical Theory and Computation

Evaluation of the tumor targeting of a FAPα-based doxorubicin prodrug

(2011) Sichao Huang et al.   JOURNAL OF DRUG TARGETING

Pro-Soft Val-boroPro: A Strategy for Enhancing in Vivo Performance of Boronic Acid Inhibitors of Serine Proteases

(2011) Sarah E. Poplawski et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure–Activity Relationship Studies on Isoindoline Inhibitors of Dipeptidyl Peptidases 8 and 9 (DPP8, DPP9): Is DPP8-Selectivity an Attainable Goal?

(2011) Sebastiaan Van Goethem et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Coupled expression of dipeptidyl peptidase-IV and fibroblast activation protein-α in transformed astrocytic cells

(2011) Eva Balaziova et al.   MOLECULAR AND CELLULAR BIOCHEMISTRY

Structural Analysis of Prolyl Oligopeptidases Using Molecular Docking and Dynamics: Insights into Conformational Changes and Ligand Binding

(2011) Swati Kaushik et al.   PLoS One

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

Inhibition of prolyl oligopeptidase with a synthetic unnatural dipeptide

(2010) Daugirdas Tomas Racys et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Biological activities of thymosin β4 defined by active sites in short peptide sequences

(2010) Gabriel Sosne et al.   FASEB JOURNAL

The dipeptidyl peptidase IV family in cancer and cell biology

(2010) Denise M. T. Yu et al.   FEBS Journal

Fibroblast activation protein expression in Crohnʼs disease strictures

(2010) Laura Rovedatti et al.   INFLAMMATORY BOWEL DISEASES

Tumor-specific Crosslinking of GITR as Costimulation for Immunotherapy

(2010) Tanja Burckhart et al.   JOURNAL OF IMMUNOTHERAPY

Substituted 4-Carboxymethylpyroglutamic Acid Diamides as Potent and Selective Inhibitors of Fibroblast Activation Protein

(2010) Ting-Yueh Tsai et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibitors of Prolyl Oligopeptidases for the Therapy of Human Diseases: Defining Diseases and Inhibitors

(2010) Janice Lawandi et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

The Dipeptidyl-Peptidase-Like Protein DPP6 Determines the Unitary Conductance of Neuronal Kv4.2 Channels

(2009) Y. A. Kaulin et al.   JOURNAL OF NEUROSCIENCE

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

(2009) A. M. LeBeau et al.   MOLECULAR CANCER THERAPEUTICS

Seprase: An overview of an important matrix serine protease

(2008) Pamela O'Brien et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

Differential impact of TGF-β and EGF on fibroblast differentiation and invasion reciprocally promotes colon cancer cell invasion

(2008) Hannelore Denys et al.   CANCER LETTERS

Effective Immunoconjugate Therapy in Cancer Models Targeting a Serine Protease of Tumor Fibroblasts

(2008) E. Ostermann et al.   CLINICAL CANCER RESEARCH

Photodynamic Molecular Beacon Triggered by Fibroblast Activation Protein on Cancer-Associated Fibroblasts for Diagnosis and Treatment of Epithelial Cancers

(2008) Pui-Chi Lo et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2007) Saurabh Aggarwal et al.   BIOCHEMISTRY

Fibroblast activation protein and chronic liver disease

(2007) Xin Maggie Wang   Frontiers in Bioscience-Landmark

The role of CD26/dipeptidyl peptidase IV in cancer

(2007) Pamela et al.   Frontiers in Bioscience-Landmark