General Information of This Antigen (ID: TAR0TSBSL)
Antigen Name
Prolyl endopeptidase FAP (FAP)
Gene Name
FAP
Gene ID
2191
Synonym
170 kDa melanoma membrane-bound gelatinase;Dipeptidyl peptidase FAP;Fibroblast activation protein alpha;Gelatine degradation protease FAP;Integral membrane serine protease;Post-proline cleaving enzyme;Serine integral membrane protease;Surface-expressed protease
Sequence
MKTWVKIVFGVATSAVLALLVMCIVLRPSRVHNSEENTMRALTLKDILNGTFSYKTFFPN
WISGQEYLHQSADNNIVLYNIETGQSYTILSNRTMKSVNASNYGLSPDRQFVYLESDYSK
LWRYSYTATYYIYDLSNGEFVRGNELPRPIQYLCWSPVGSKLAYVYQNNIYLKQRPGDPP
FQITFNGRENKIFNGIPDWVYEEEMLATKYALWWSPNGKFLAYAEFNDTDIPVIAYSYYG
DEQYPRTINIPYPKAGAKNPVVRIFIIDTTYPAYVGPQEVPVPAMIASSDYYFSWLTWVT
DERVCLQWLKRVQNVSVLSICDFREDWQTWDCPKTQEHIEESRTGWAGGFFVSTPVFSYD
AISYYKIFSDKDGYKHIHYIKDTVENAIQITSGKWEAINIFRVTQDSLFYSSNEFEEYPG
RRNIYRISIGSYPPSKKCVTCHLRKERCQYYTASFSDYAKYYALVCYGPGIPISTLHDGR
TDQEIKILEENKELENALKNIQLPKEEIKKLEVDEITLWYKMILPPQFDRSKKYPLLIQV
YGGPCSQSVRSVFAVNWISYLASKEGMVIALVDGRGTAFQGDKLLYAVYRKLGVYEVEDQ
ITAVRKFIEMGFIDEKRIAIWGWSYGGYVSSLALASGTGLFKCGIAVAPVSSWEYYASVY
TERFMGLPTKDDNLEHYKNSTVMARAEYFRNVDYLLIHGTADDNVHFQNSAQIAKALVNA
QVDFQAMWYSDQNHGLSGLSTNHLYTHMTHFLKQCFSLSD

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Family
Peptidase S1 family
Function
Cell surface glycoprotein serine protease that participates in extracellular matrix degradation and involved in many cellular processes including tissue remodeling, fibrosis, wound healing, inflammation and tumor growth. 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, on substrate such as alpha-2-antiplasmin SERPINF2 and SPRY2. Degrade also gelatin, heat-denatured type I collagen, but not native collagen type I and IV, vitronectin, tenascin, laminin, fibronectin, fibrin or casein. Also has dipeptidyl peptidase activity, exhibiting the ability to hydrolyze the prolyl bond two residues from the N-terminus of synthetic dipeptide substrates provided that the penultimate residue is proline, with a preference for Ala-Pro, Ile-Pro, Gly-Pro, Arg-Pro and Pro-Pro. Natural neuropeptide hormones for dipeptidyl peptidase are the neuropeptide Y (NPY), peptide YY (PYY), substance P (TAC1) and brain natriuretic peptide 32 (NPPB). 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. Plays a role in tissue remodeling during development and wound healing. Participates in the cell invasiveness towards the ECM in malignant melanoma cancers. Enhances tumor growth progression by increasing angiogenesis, collagen fiber degradation and apoptosis and by reducing antitumor response of the immune system. 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.

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Uniprot Entry
SEPR_HUMAN
HGNC ID
HGNC:3590
KEGG ID
hsa:2191
Each Antibody-drug Conjugate and Its Component Related to This Antigen
Full List of The ADC Related to This Antigen
The Numbers of ADCs, Their Three Components, Payload Targets, and Corresponding Diseases for This Antigens
Anti-FAP mAb B11
ADC Name Payload Target Linker ADC Info
Anti-FAP B11-MC-VC-PABC-MMAE [1]
Monomethyl auristatin E
Microtubule (MT)
Anti-FAP B11-MC-VC-PABC-MMAE linker
Anti-FAP B11-AO-Cys-MC-VC-PABC-MMAE [1]
Monomethyl auristatin E
Microtubule (MT)
Anti-FAP B11-AO-Cys-MC-VC-PABC-MMAE linker
ADC Name Payload Target Linker ADC Info
HPS157-039-001 [2]
HPS157-039-001 payload
Undisclosed
HPS157-039-001 linker
HPS157-039-002 [2]
HPS157-039-002 payload
Undisclosed
HPS157-039-002 linker
HPS157-039-003 [2]
HPS157-039-003 payload
Undisclosed
HPS157-039-003 linker
HPS157-039-004 [2]
HPS157-039-004 payload
Undisclosed
HPS157-039-004 linker
HPS157-039-005 [2]
HPS157-039-005 payload
Undisclosed
HPS157-039-005 linker
ADC Name Payload Target Linker ADC Info
huB12-MMAE [3]
Monomethyl auristatin E
Microtubule (MT)
Mc-Val-Cit-PABC
huB12-MMAF [3]
Monomethyl auristatin F
Microtubule (MT)
Mc-Val-Cit-PABC
huB12-DM1 [3]
Mertansine DM1
Microtubule (MT)
Mc-Val-Cit-PABC
ADC Name Payload Target Linker ADC Info
OMTX705 [4]
TAM470
Microtubule (MT)
Mc-Val-Cit-PABC-PEG3
ADC Name Payload Target Linker ADC Info
OncoFAP-GlyPro-MMAE [5]
Monomethyl auristatin E
Microtubule (MT)
Maleimido Caproyl-GlyPro-PAB linker
OncoFAP-GlyPro-SN38 [5]
Undisclosed
Undisclosed
Maleimido Caproyl-GlyPro-PAB linker
OncoFAP-GlyPro-Dxd [5]
DX-8951 derivative (DXd)
DNA topoisomerase 1 (TOP1)
Maleimido Caproyl-GlyPro-PAB linker
sibrotuzumab
ADC Name Payload Target Linker ADC Info
NAPC-ADC [6]
Monomethyl auristatin E
Microtubule (MT)
MC-Radiation-responsive linker
Undisclosed
ADC Name Payload Target Linker ADC Info
OMTX-505 [7]
Undisclosed
Undisclosed
Undisclosed
References
Ref 1 Site-specific antibody-drug conjugation through glycoengineering.
Ref 2 Antibody-drug conjugates and immunotoxins.
Ref 3 Mechanistic Characterization of Cancer-associated Fibroblast Depletion via an Antibody-Drug Conjugate Targeting Fibroblast Activation Protein
Ref 4 Introduction to basic information on ADC drug IN30705.
Ref 5 In vivo activation of FAP-cleavable small molecule-drug conjugates for the targeted delivery of camptothecins and tubulin poisons to the tumor microenvironment
Ref 6 Radiotherapy activates picolinium prodrugs in tumours
Ref 7 Introduction to basic information on ADC drug OMTX-505.