General Information of This Target
Target ID
PATR0CODOT
Target Name
Nuclear factor NF-kappa-B p105 subunit (NFKB1)
Gene Name
NFKB1
Gene ID
4790
Synonym
DNA-binding factor KBF1 EBP-1
Sequence
MAEDDPYLGRPEQMFHLDPSLTHTIFNPEVFQPQMALPTDGPYLQILEQPKQRGFRFRYV
CEGPSHGGLPGASSEKNKKSYPQVKICNYVGPAKVIVQLVTNGKNIHLHAHSLVGKHCED
GICTVTAGPKDMVVGFANLGILHVTKKKVFETLEARMTEACIRGYNPGLLVHPDLAYLQA
EGGGDRQLGDREKELIRQAALQQTKEMDLSVVRLMFTAFLPDSTGSFTRRLEPVVSDAIY
DSKAPNASNLKIVRMDRTAGCVTGGEEIYLLCDKVQKDDIQIRFYEEEENGGVWEGFGDF
SPTDVHRQFAIVFKTPKYKDINITKPASVFVQLRRKSDLETSEPKPFLYYPEIKDKEEVQ
RKRQKLMPNFSDSFGGGSGAGAGGGGMFGSGGGGGGTGSTGPGYSFPHYGFPTYGGITFH
PGTTKSNAGMKHGTMDTESKKDPEGCDKSDDKNTVNLFGKVIETTEQDQEPSEATVGNGE
VTLTYATGTKEESAGVQDNLFLEKAMQLAKRHANALFDYAVTGDVKMLLAVQRHLTAVQD
ENGDSVLHLAIIHLHSQLVRDLLEVTSGLISDDIINMRNDLYQTPLHLAVITKQEDVVED
LLRAGADLSLLDRLGNSVLHLAAKEGHDKVLSILLKHKKAALLLDHPNGDGLNAIHLAMM
SNSLPCLLLLVAAGADVNAQEQKSGRTALHLAVEHDNISLAGCLLLEGDAHVDSTTYDGT
TPLHIAAGRGSTRLAALLKAAGADPLVENFEPLYDLDDSWENAGEDEGVVPGTTPLDMAT
SWQVFDILNGKPYEPEFTSDDLLAQGDMKQLAEDVKLQLYKLLEIPDPDKNWATLAQKLG
LGILNNAFRLSPAPSKTLMDNYEVSGGTVRELVEALRQMGYTEAIEVIQAASSPVKTTSQ
AHSLPLSPASTRQQIDELRDSDSVCDSGVETSFRKLSFTESLTSGASLLTLNKMPHDYGQ
EGPLEGKI

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Family
the NF-kappaB-related factor
Function
NF-kappa-B is a pleiotropic transcription factor present in almost all cell types and is the endpoint of a series of signal transduction events that are initiated by a vast array of stimuli related to many biological processes such as inflammation, immunity, differentiation, cell growth, tumorigenesis and apoptosis. NF-kappa-B is a homo- or heterodimeric complex formed by the Rel-like domain-containing proteins RELA/p65, RELB, NFKB1/p105, NFKB1/p50, REL and NFKB2/p52 and the heterodimeric p65-p50 complex appears to be most abundant one. The dimers bind at kappa-B sites in the DNA of their target genes and the individual dimers have distinct preferences for different kappa-B sites that they can bind with distinguishable affinity and specificity. Different dimer combinations act as transcriptional activators or repressors, respectively. NF-kappa-B is controlled by various mechanisms of post-translational modification and subcellular compartmentalization as well as by interactions with other cofactors or corepressors. NF-kappa-B complexes are held in the cytoplasm in an inactive state complexed with members of the NF-kappa-B inhibitor (I-kappa-B) family. In a conventional activation pathway, I-kappa-B is phosphorylated by I-kappa-B kinases (IKKs) in response to different activators, subsequently degraded thus liberating the active NF-kappa-B complex which translocates to the nucleus. NF-kappa-B heterodimeric p65-p50 and RelB-p50 complexes are transcriptional activators. The NF-kappa-B p50-p50 homodimer is a transcriptional repressor, but can act as a transcriptional activator when associated with BCL3. NFKB1 appears to have dual functions such as cytoplasmic retention of attached NF-kappa-B proteins by p105 and generation of p50 by a cotranslational processing. The proteasome-mediated process ensures the production of both p50 and p105 and preserves their independent function, although processing of NFKB1/p105 also appears to occur post-translationally. p50 binds to the kappa-B consensus sequence 5'-GGRNNYYCC-3', located in the enhancer region of genes involved in immune response and acute phase reactions. In a complex with MAP3K8, NFKB1/p105 represses MAP3K8-induced MAPK signaling; active MAP3K8 is released by proteasome-dependent degradation of NFKB1/p105.

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Uniprot Entry
NFKB1_HUMAN
HGNC ID
HGNC:7794
KEGG ID
hsa:4790
Full List of The ADC Related to This Target
Investigative
Click To Hide/Show 7 ADC Related to This Stage
ADC Info ADC Name Antibody Antigen Payload Linker Ref
Trastuzumab-L3-TL
Trastuzumab
ERBB2
Triptolide
BVP-PEG3-carbamate-PEG4
[1]
Trastuzumab-L2-TL
Trastuzumab
ERBB2
Triptolide
BVP-PEG3-diamine
[1]
Trastuzumab-L1-TL
Trastuzumab
ERBB2
Triptolide
BVP-PEG3-carbamate
[1]
Cet-TPL
Cetuximab
EGFR
Triptolide
N-hydroxysuccinimide based linker
[2]
Y-TR1 GMBS
Anti-CD26 mAb YS110
DPP4
Triptolide
N-gama-maleimidobutyryl-oxysuccinimide ester (GMBS)
[3]
Y-TR1 SPDP
Anti-CD26 mAb YS110
DPP4
Triptolide
N-succinimidyl 3-(2-pyridyldithio) propionate (SPDP)
[3]
Y-TR1 SMCC
Anti-CD26 mAb YS110
DPP4
Triptolide
Succinimidyl-4-(N-maleimidomethyl)cyclohexane-1-carboxylate (SMCC)
[3]
References
Ref 1 Site-specific construction of triptolide-based antibody-drug conjugates. Bioorg Med Chem. 2021 Dec 1;51:116497. doi: 10.1016/j.bmc.2021.116497. Epub 2021 Nov 10.
Ref 2 Cetuximab-Triptolide Conjugate Suppresses the Growth of EGFR-Overexpressing Lung Cancers through Targeting RNA Polymerase II. Mol Ther Oncolytics. 2020 Jul 6;18:304-316. doi: 10.1016/j.omto.2020.07.001. eCollection 2020 Sep 25.
Ref 3 Novel Antibody-Drug Conjugate with Anti-CD26 Humanized Monoclonal Antibody and Transcription Factor IIH (TFIIH) Inhibitor, Triptolide, Inhibits Tumor Growth via Impairing mRNA Synthesis. Cancers (Basel). 2019 Aug 8;11(8):1138. doi: 10.3390/cancers11081138.

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