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FAP

概要

Name:Prolyl endopeptidase FAP
Target Synonym:Post-Proline Cleaving Enzyme,FAPalpha,SIMP,Fibroblast Activation Protein, Alpha,Serine Integral Membrane Protease,Prolyl Endopeptidase FAP,EC 3.4.21.26,EC 3.4.14.5,EC 3.4.21.-,DPPIV,FAPA,170 kDa melanoma membrane-bound gelatinase,Seprase,Gelatine degradation protease FAP,Dipeptidyl peptidase FAP,Fibroblast activation protein alpha,APCE,Integral membrane serine protease,Surface-expressed protease,FAP
Number of Launched Drugs:0
Number of Drugs in Clinical Trials:26
Lastest Research Phase:Phase 2 Clinical

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生物活性データの一部

FAP-HP245-Cell-based assay
FACS assay shows that recombinant Biotinylated FACS

5e5 of anti-FAP CAR-293 cells were stained with 100 μL of 1:25 dilution (4 μL stock solution in 100 μL FACS buffer) of PE-Labeled Human FAP, His Tag (Cat. No. FAP-HP245) and negative control protein respectively. PE signal was used to evaluate the binding activity (QC tested).

FAP-HF263-Cell-based assay
 FAP FACS

2e5 of anti-FAP CAR-293 cells were stained with 100 μL of 3 μg/mL of FITC-Labeled Human FAP, Fc Tag (Cat. No. FAP-HF263) and negative control protein respectively, FITC signal was used to evaluate the binding activity (QC tested).

FAP-R5246-SPR
 FAP SPR

Anti-FAP Antibody, Mouse IgG2a (FAP5) captured on CM5 chip via anti-mouse antibodies surface can bind Rat FAP, His Tag (Cat. No. FAP-R5246) with an affinity constant of 0.839 nM as determined in a SPR assay (Biacore 8K) (Routinely tested).

FAP-C52H3-SPR
 FAP SPR

Anti-FAP Antibody, Mouse IgG2a (FAP5) captured on CM5 chip via anti-mouse antibodies surface can bind Cynomolgus FAP, His Tag (Cat. No. FAP-C52H3) with an affinity constant of 3.10 nM as determined in a SPR assay (Biacore 8K) (Routinely tested).

Synonym Name

FAP,FAPalpha,SIMP,Seprase,APCE

Background

FAP (also known as seprase) is a Type II transmembrane serine protease. Both plasma membrane and soluble forms exhibit post-proline cleaving endopeptidase activity, with a marked preference for Ala/Ser-Gly-Pro-Ser/Asn/Ala consensus sequences. Degrade also gelatin, heat-denatured type I collagen. Also has dipeptidyl peptidase activity, with a preference for Ala-Pro, Ile-Pro, Gly-Pro, Arg-Pro and Pro-Pro. The plasma membrane form, in association with either DPP4, PLAUR or integrins, is involved in the pericellular proteolysis of the extracellular matrix (ECM), and hence promotes cell adhesion, migration and invasion through the ECM. Promotes glioma cell invasion through the brain parenchyma by degrading the proteoglycan brevican. Acts as a tumor suppressor in melanocytic cells through regulation of cell proliferation and survival in a serine protease activity-independent manner.

Clinical and Translational Updates

臨床試験情報

Name Research Code Research Phase Company Indications Clinical Trials
FAP-DR5 RG-7386; RO-6874813 Millennium Pharmaceuticals Inc, F. Hoffmann-La Roche Ltd Details
Simlukafusp alfa FAP-IL2v; RG-7461; aFAP-IL2v; RO-6874281; FAP-IL2v FP F. Hoffmann-La Roche Ltd Details
177Lu-FAP-2286 177Lu-FAP-2286 Phase 2 Clinical 3B Pharmaceuticals GmbH Solid tumours Details
68Ga-FAP-2286 68Ga-FAP-2286; 68-Ga-FAP-2286 Phase 2 Clinical 3B Pharmaceuticals GmbH Solid tumours; Neoplasm Metastasis Details
Nectin4/FAP-targeted CAR-T cell therapy (The Sixth Affiliated Hospital of Wenzhou Medical University) Phase 1 Clinical Wenzhou Medical University, The Sixth Affiliated Hospital Of Wenzhou Medical University Solid tumours Details
OMTX-705 OMTX-705 Phase 1 Clinical Oncomatryx Biopharma Sl Solid tumours Details
RO-7300490 RO-7300490; RG-6189 Phase 1 Clinical F. Hoffmann-La Roche Ltd Solid tumours; Neoplasms Details
Talabostat PT-100; BXCL-701 Phase 2 Clinical Midatech Pharma Plc, Bioxcel Therapeutics Inc Neuroblastoma; Melanoma; Leukemia, Lymphocytic, Chronic, B-Cell; Adenocarcinoma; Neoplasms, Germ Cell and Embryonal; Carcinoma, Non-Small-Cell Lung; Neoplasm Metastasis; Carcinoma, Pancreatic Ductal; Lung Neoplasms; Carcinoma, Small Cell; Brain Neoplasms; Solid tumours; Sarcoma; Prostatic Neoplasms; Central Nervous System Neoplasms; Neuroendocrine Tumors; Skin Neoplasms; Pancreatic Neoplasms; Kidney Neoplasms; Ovarian Neoplasms; Liver Neoplasms Details
177Lu-PNT6555(Point Biopharma) PNT-6555 Phase 1 Clinical Point Biopharma Inc Solid tumours; Esophageal Neoplasms; Sarcoma; Colorectal Neoplasms; Carcinoma, Pancreatic Ductal; Melanoma Details
[18F]FAPI-74 FAPI-74; [18F]FAPI-74 Phase 2 Clinical Sofie Biliary Tract Neoplasms; Stomach Neoplasms; Pancreatic Neoplasms; Colorectal Neoplasms; Carcinoma, Hepatocellular Details
MP-0310 MP-0310; AMG-506 Phase 1 Clinical Molecular Partners Ag, Amgen Inc Solid tumours Details

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