Antigen Information

General Information of This Antigen (ID: TAR0TLUNC)
Antigen Name
Epidermal growth factor receptor (EGFR); Receptor tyrosine-protein kinase erbB-3 (HER3)
Gene Name
EGFR; HER3
Gene ID
1956 , 2065
Synonym1
ERBB, ERBB1, HER1
Synonym2
HER3
Sequence1
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEV
VLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALA
VLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDF
QNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGC
TGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYV
VTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFK
NCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAF
ENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKL
FGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCN
LLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVM
GENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVV
ALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGS
GAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGI
CLTSTVQLITQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAA
RNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSY
GVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPK
FRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQ
QGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTED
SIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLN
TVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRV
APQSSEFIGA

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Sequence2
MRANDALQVLGLLFSLARGSEVGNSQAVCPGTLNGLSVTGDAENQYQTLYKLYERCEVVM
GNLEIVLTGHNADLSFLQWIREVTGYVLVAMNEFSTLPLPNLRVVRGTQVYDGKFAIFVM
LNYNTNSSHALRQLRLTQLTEILSGGVYIEKNDKLCHMDTIDWRDIVRDRDAEIVVKDNG
RSCPPCHEVCKGRCWGPGSEDCQTLTKTICAPQCNGHCFGPNPNQCCHDECAGGCSGPQD
TDCFACRHFNDSGACVPRCPQPLVYNKLTFQLEPNPHTKYQYGGVCVASCPHNFVVDQTS
CVRACPPDKMEVDKNGLKMCEPCGGLCPKACEGTGSGSRFQTVDSSNIDGFVNCTKILGN
LDFLITGLNGDPWHKIPALDPEKLNVFRTVREITGYLNIQSWPPHMHNFSVFSNLTTIGG
RSLYNRGFSLLIMKNLNVTSLGFRSLKEISAGRIYISANRQLCYHHSLNWTKVLRGPTEE
RLDIKHNRPRRDCVAEGKVCDPLCSSGGCWGPGPGQCLSCRNYSRGGVCVTHCNFLNGEP
REFAHEAECFSCHPECQPMEGTATCNGSGSDTCAQCAHFRDGPHCVSSCPHGVLGAKGPI
YKYPDVQNECRPCHENCTQGCKGPELQDCLGQTLVLIGKTHLTMALTVIAGLVVIFMMLG
GTFLYWRGRRIQNKRAMRRYLERGESIEPLDPSEKANKVLARIFKETELRKLKVLGSGVF
GTVHKGVWIPEGESIKIPVCIKVIEDKSGRQSFQAVTDHMLAIGSLDHAHIVRLLGLCPG
SSLQLVTQYLPLGSLLDHVRQHRGALGPQLLLNWGVQIAKGMYYLEEHGMVHRNLAARNV
LLKSPSQVQVADFGVADLLPPDDKQLLYSEAKTPIKWMALESIHFGKYTHQSDVWSYGVT
VWELMTFGAEPYAGLRLAEVPDLLEKGERLAQPQICTIDVYMVMVKCWMIDENIRPTFKE
LANEFTRMARDPPRYLVIKRESGPGIAPGPEPHGLTNKKLEEVELEPELDLDLDLEAEED
NLATTTLGSALSLPVGTLNRPRGSQSLLSPSSGYMPMNQGNLGESCQESAVSGSSERCPR
PVSLHPMPRGCLASESSEGHVTGSEAELQEKVSMCRSRSRSRSPRPRGDSAYHSQRHSLL
TPVTPLSPPGLEEEDVNGYVMPDTHLKGTPSSREGTLSSVGLSSVLGTEEEDEDEEYEYM
NRRRRHSPPHPPRPSSLEELGYEYMDVGSDLSASLGSTQSCPLHPVPIMPTAGTTPDEDY
EYMNRQRDGGGPGGDYAAMGACPASEQGYEEMRAFQGPGHQAPHVHYARLKTLRSLEATD
SAFDNPDYWHSRLFPKANAQRT

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Family1
Tyr protein family
Family2
Tyr protein kinase family
Function1
Receptor tyrosine kinase binding ligands of the EGF family and activating several signaling cascades to convert extracellular cues into appropriate cellular responses. Known ligands include EGF, TGFA/TGF-alpha, AREG, epigen/EPGN, BTC/betacellulin, epiregulin/EREG and HBEGF/heparin- binding EGF. Ligand binding triggers receptor homo- and/or heterodimerization and autophosphorylation on key cytoplasmic residues. The phosphorylated receptor recruits adapter proteins like GRB2 which in turn activates complex downstream signaling cascades. Activates at least 4 major downstream signaling cascades including the RAS-RAF-MEK-ERK, PI3 kinase-AKT, PLCgamma-PKC and STATs modules. May also activate the NF-kappa-B signaling cascade. Also directly phosphorylates other proteins like RGS16, activating its GTPase activity and probably coupling the EGF receptor signaling to the G protein-coupled receptor signaling. Also phosphorylates MUC1 and increases its interaction with SRC and CTNNB1/beta-catenin. Positively regulates cell migration via interaction with CCDC88A/GIV which retains EGFR at the cell membrane following ligand stimulation, promoting EGFR signaling which triggers cell migration. Plays a role in enhancing learning and memory performance. Plays a role in mammalian pain signaling (long-lasting hypersensitivity).

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Function2
Tyrosine-protein kinase that plays an essential role as cell surface receptor for neuregulins. Binds to neuregulin-1 (NRG1) and is activated by it; ligand-binding increases phosphorylation on tyrosine residues and promotes its association with the p85 subunit of phosphatidylinositol 3-kinase. May also be activated by CSPG5. Involved in the regulation of myeloid cell differentiation.

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Uniprot Entry
EGFR_HUMAN , ERBB3_HUMAN
HGNC ID
HGNC:3236 , HGNC:3431
KEGG ID
hsa:1956 , hsa:2065
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-EGFR/HER3 bsAb
 Antibody Info 
ADC Name Payload Target Linker ADC Info
HDM2024
Exatecan
DNA topoisomerase 1 (TOP1)
A cleavable linker
 ADC Info 
IBI3005
NT1
DNA topoisomerase 1 (TOP1)
Undisclosed
 ADC Info 
BL-B16D1
WA-00
Microtubule (MT)
Undisclosed
 ADC Info 
JSKN021 [1]
MMAE; Alphatecan
DNA topoisomerase 1 (TOP1)+Microtubule (MT)
A cleavable linker
 ADC Info 
DB-1418 [2]
P1021
DNA topoisomerase 1 (TOP1)
Mc-Gly-Gly-Phe-Gly
 ADC Info 
BNT3212
TOP1 inhibitor
DNA topoisomerase 1 (TOP1)
A cleavable linker
 ADC Info 
JS212
Exatecan
DNA topoisomerase 1 (TOP1)
A cleavable linker
 ADC Info 
Anti-Lysozyme mAb
 Antibody Info 
ADC Name Payload Target Linker ADC Info
IgG1-ADC-07 [3]
IgG1-ADC-07 payload
Undisclosed
IgG1-ADC-07 linker
 ADC Info 
IgG1-ADC-04 [3]
IgG1-ADC-04 payload
Undisclosed
IgG1-ADC-04 linker
 ADC Info 
Anti-ody fragment (AF)
 Antibody Info 
ADC Name Payload Target Linker ADC Info
AF-GPL [4]
Gemcitabine and paclitaxel loaded liposome
Human Deoxyribonucleic acid (hDNA)
Undisclosed
 ADC Info 
Izalontamab
 Antibody Info 
ADC Name Payload Target Linker ADC Info
izalontamab brengitecan
Ed-04
DNA topoisomerase 1 (TOP1)
Gly-Mal-Gly-Gly-Phe-Gly
 ADC Info 
ADC Name Payload Target Linker ADC Info
N-D8-1508 [5]
AZ-1508
Microtubule (MT)
Cysteine D8
 ADC Info 
N-D6-1508 [5]
AZ-1508
Microtubule (MT)
Cysteine D6
 ADC Info 
N-D4-1508 [5]
AZ-1508
Microtubule (MT)
Cysteine D4
 ADC Info 
N-D2-1508 [5]
AZ-1508
Microtubule (MT)
Cysteine D2
 ADC Info 
ADC Name Payload Target Linker ADC Info
Sal5-DM4 [6]
Mertansine DM4
Microtubule (MT)
N-succinimidyl 4-(2-pyridyldithio) butanoate (SPDB)
 ADC Info 
Sal5-MMAE [6]
Monomethyl auristatin E
Microtubule (MT)
Mc-Val-Cit-PABC
 ADC Info 
Sal5-DuoDM [6]
DEAEA duocarmycin
Human Deoxyribonucleic acid (hDNA)
Mal-PEG4-Val-Cit-PABC
 ADC Info 
Targeted against E. coli mAb (hWN1)
 Antibody Info 
ADC Name Payload Target Linker ADC Info
ABC-1C [7]
Macrocyclic antimicrobial peptide 1C (AMP-1C)
Undisclosed
Undisclosed
 ADC Info 
ABC-2A [7]
Macrocyclic antimicrobial peptide 2A (AMP-2A)
Undisclosed
Undisclosed
 ADC Info 
ABC-3C [7]
Macrocyclic antimicrobial peptide 3C (AMP-3C)
Undisclosed
Undisclosed
 ADC Info 
ABC-3E [7]
Macrocyclic antimicrobial peptide 3E (AMP-3E)
Undisclosed
Undisclosed
 ADC Info 
Undisclosed
 Antibody Info 
ADC Name Payload Target Linker ADC Info
Tri-specific anti-Her1/Her3 Zybody [8]
Undisclosed
Undisclosed
Undisclosed
 ADC Info 
SIB-029A [9]
Undisclosed
Undisclosed
Undisclosed
 ADC Info 
SRB19 [10]
Undisclosed
Undisclosed
Undisclosed
 ADC Info 
PRN 201 [11]
Undisclosed
Undisclosed
Undisclosed
 ADC Info 
PRN 222 [11]
Undisclosed
Undisclosed
Undisclosed
 ADC Info 
PRN 211 [11]
Undisclosed
Undisclosed
Undisclosed
 ADC Info 
WTx-Immunostimulant [12]
Undisclosed
Undisclosed
Undisclosed
 ADC Info 
WTx-Combos [12]
Undisclosed
Undisclosed
Undisclosed
 ADC Info 
WTx-ABC [12]
Undisclosed
Undisclosed
Undisclosed
 ADC Info 
WTx-Proteasome inhibition [12]
Undisclosed
Undisclosed
Undisclosed
 ADC Info 
HuIgG1-19 [13]
PNU-159682
DNA topoisomerase 2-alpha (TOP2A)
Hydrophilic cleavable linker 19
 ADC Info 
HuIgG1-25 [13]
PNU-159682
DNA topoisomerase 2-alpha (TOP2A)
Alternative linker without basic amines linker 25
 ADC Info 
HuIgG1-26 [13]
PNU-159682
DNA topoisomerase 2-alpha (TOP2A)
Maleimide based noncleavable linker 26
 ADC Info 
HuIgG1-29 [13]
PNU-159682
DNA topoisomerase 2-alpha (TOP2A)
PNU-thiazole cleavable linker 29
 ADC Info 
KA-3123-LD38 [14]
Undisclosed
Undisclosed
Undisclosed
 ADC Info 
BR-2302 [15]
Undisclosed
Undisclosed
Undisclosed
 ADC Info 
References
Ref 1 JSKN021, an innovative site-specific dual-payload bispecific antibody drug conjugate targeting EGFR and HER3 exhibits potent preclinical activities
Ref 2 DB-1418, a bispecific antibody-drug conjugate (ADC) targeting EGFR and HER3, demonstrates superior and broad antitumor efficacy and favorable safety in preclinical models
Ref 3 Bioactive substance conjugate, preparation method therefor and use thereof; 2022-08-18.
Ref 4 Antibody fragment-conjugated gemcitabine and paclitaxel-based liposome for effective therapeutic efficacy in pancreatic cancer. Mater Sci Eng C Mater Biol Appl. 2018 Aug 1;89:328-335. doi: 10.1016/j.msec.2018.04.011. Epub 2018 Apr 11.
Ref 5 Design and Validation of Linkers for Site-Specific Preparation of Antibody-Drug Conjugates Carrying Multiple Drug Copies Per Cysteine Conjugation Site. Int J Mol Sci. 2020 Sep 19;21(18):6882. doi: 10.3390/ijms21186882.
Ref 6 APOMAB Antibody-Drug Conjugates Targeting Dead Tumor Cells are Effective In Vivo. Mol Cancer Ther. 2019 Feb;18(2):335-345. doi: 10.1158/1535-7163.MCT-18-0842. Epub 2018 Nov 9.
Ref 7 Antibody-Bactericidal Macrocyclic Peptide Conjugates To Target Gram-Negative Bacteria. Chembiochem. 2018 Oct 4;19(19):2039-2044. doi: 10.1002/cbic.201800295. Epub 2018 Sep 14.
Ref 8 Zyngenia biotherapeutics company product pipeline
Ref 9 Introduction to basic information on ADC drug SI-B-029A
Ref 10 Biology drives the discovery of bispecific antibodies as innovative therapeutics. Antib Ther. 2020 Feb 17;3(1):18-62. doi: 10.1093/abt/tbaa003. eCollection 2020 Jan.
Ref 11 ProEn therapeutic company product pipeline
Ref 12 Window therapeutic product pipeline
Ref 13 Evaluation of PNU-159682 antibody drug conjugates (ADCs). Bioorg Med Chem Lett. 2020 Dec 15;30(24):127640. doi: 10.1016/j.bmcl.2020.127640. Epub 2020 Oct 28.
Ref 14 KA-3123-LD38: a novel bispecific antibody-drug conjugate (ADC) targeting EGFR and B7H3 with a DNA topoisomerase I inhibitor payload
Ref 15 Preclinical studies of BR-2302: A HER3xEGFR bi-specific Exd-containing ADC