Affinage

KBTBD7

Kelch repeat and BTB domain-containing protein 7 · UniProt Q8WVZ9

Length
684 aa
Mass
77.2 kDa
Annotated
2026-06-10
18 papers in source corpus 9 papers cited in narrative 8 extracted findings
Cross-family judge vs UniProt: Affinage preferred faithfulness: 5/5 claims corpus-supported (100%)

Mechanistic narrative

Synthesis pass · prose summary of the discoveries below

KBTBD7 is a BTB-kelch substrate adaptor that confers target specificity on CUL3 RING ubiquitin ligase complexes, directing multiple substrates to ubiquitin-dependent proteasomal degradation (PMID:25684205, PMID:27308540). Acting with its paralog KBTBD6, it ubiquitylates the RAC1-specific GEF TIAM1; loss of KBTBD7 stabilizes TIAM1, elevates RAC1 activity, remodels actin, and enhances invasion, and its preferential binding to GABARAP via ATG8-interacting motifs spatially restricts this RAC1 signaling to GABARAP-containing vesicles (PMID:25684205, PMID:27308540). In the Wnt/PCP pathway, KBTBD7 is recruited by p97/VCP through UBA-UBX adaptors to ubiquitinate the core components Vangl1 and Vangl2 for ER-associated degradation, a step blocked by Wnt5a/CK1-induced Vangl phosphorylation, and it regulates convergent extension during zebrafish gastrulation (PMID:33990333). It additionally targets internalized DRD2 at five mapped lysines, controlling DRD2 abundance in vivo and modulating AKT/mTOR responses to dopamine agonists (PMID:32572597), and degrades PTEN to activate EGFR/PI3K/AKT signaling in lung cancer cells (PMID:35499228). Independently of its adaptor function, KBTBD7 physically interacts with MKK3/6 to promote p38 and NF-κB inflammatory signaling downstream of DAMPs, and it is a direct target of miR-21 (PMID:29991775); it also drives inflammatory programs through ubiquitination of the transcription factor KLF15 (PMID:39489209).

Mechanistic history

Synthesis pass · year-by-year structured walk · 7 steps
  1. 2010 Medium

    Initial characterization established KBTBD7 as a cytoplasmic BTB-kelch protein capable of modulating transcriptional output, the first functional readout for an otherwise uncharacterized gene.

    Evidence Western blot localization, GAL4-fusion and AP-1/SRE luciferase reporter assays with domain deletions and siRNA in COS-7/MCF-7 cells

    PMID:20132730

    Open questions at the time
    • Transcriptional activation measured only via artificial GAL4 fusion and reporter overexpression, not endogenous targets
    • No molecular mechanism connecting KBTBD7 to AP-1/SRE established
    • No ubiquitin ligase or substrate-adaptor role yet identified
  2. 2015 High

    Defined KBTBD7's core molecular identity as a CUL3 substrate adaptor that ubiquitylates TIAM1, resolving how it functions biochemically and linking it to spatial control of RAC1 signaling via GABARAP vesicles.

    Evidence Reciprocal Co-IP, ubiquitylation assays, siRNA with actin/invasion/proliferation readouts, ATG8-binding motif mutagenesis and vesicle recruitment assays

    PMID:25684205 PMID:27308540

    Open questions at the time
    • Generality of GABARAP-dependent recruitment to other substrates not tested
    • Relative contributions of KBTBD6 versus KBTBD7 not fully dissected
  3. 2020 High

    Extended the substrate repertoire to DRD2 with residue-level resolution and in vivo validation, showing KBTBD7 controls receptor abundance and downstream AKT/mTOR signaling.

    Evidence Yeast two-hybrid, Co-IP, ubiquitination site mapping (K221/226/241/251/258), CRISPR KO mice, cell-based signaling readouts

    PMID:32572597

    Open questions at the time
    • Whether DRD2 ubiquitination uses the same CUL3 complex as TIAM1 not directly shown
    • Tissue-specific determinants of substrate selection unclear
  4. 2021 High

    Connected KBTBD7 to ERAD and Wnt/PCP by showing p97/VCP-mediated recruitment drives Vangl1/2 degradation, establishing a phospho-regulated quality-control step controlling planar cell polarity in vivo.

    Evidence Co-IP (p97/VCP–KBTBD7, KBTBD7–Vangl), ubiquitination and ERAD assays, phospho-blocking mutants, zebrafish convergent-extension loss/rescue

    PMID:33990333

    Open questions at the time
    • How VCP-UBX recruitment relates to CUL3 adaptor function not reconciled
    • Structural basis of phospho-dependent escape from ubiquitination not resolved
  5. 2018 Medium

    Revealed a non-degradative signaling role: KBTBD7 binds and activates MKK3/6 to amplify DAMP-triggered p38/NF-κB inflammation, and is itself repressed by miR-21.

    Evidence Luciferase 3'UTR reporter, Co-IP (KBTBD7–MKK3/6), miR-21 KO mice, siRNA with cytokine/phospho-signaling readouts post-MI

    PMID:29991775

    Open questions at the time
    • Whether MKK3/6 activation requires ubiquitin ligase activity or is adaptor-independent unclear
    • Single Co-IP for the KBTBD7–MKK3/6 interaction without structural mapping
  6. 2022 Medium

    Added PTEN as a degradation substrate, positioning KBTBD7 as a driver of EGFR/PI3K/AKT signaling in lung cancer.

    Evidence Knockdown in NSCLC lines with PTEN level, ubiquitination assays, AKT/proliferation/invasion readouts

    PMID:35499228

    Open questions at the time
    • CUL3 dependence of PTEN ubiquitination not demonstrated
    • Single-lab, single-study evidence
  7. 2024 Medium

    Implicated KBTBD7 in inflammatory regulation through ubiquitination of KLF15 and an interaction with FOXA1, linking it to NLRP3/NF-κB signaling and ferroptosis in injury models.

    Evidence Co-IP (KBTBD7–KLF15, KBTBD7–FOXA1), ubiquitination assays, siRNA with NLRP3/NF-κB and ferroptosis/ROS readouts, epistasis rescue, sepsis/lung injury mouse models

    PMID:38652964 PMID:39489209

    Open questions at the time
    • FOXA1–SLC7A11 link inferred indirectly (idx 6 is Low confidence)
    • How KBTBD7 both degrades a transcription factor and stabilizes another (FOXA1) is mechanistically unreconciled
    • CUL3 dependence not established for KLF15

Open questions

Synthesis pass · forward-looking unresolved questions
  • It remains unknown how KBTBD7 selects among its diverse substrates and whether its non-degradative kinase-activating and transcriptional roles share a common structural mechanism.
  • No structural model of substrate or CUL3/VCP engagement
  • Substrate-selection determinants across tissues uncharacterized
  • Reconciliation of CUL3-adaptor versus VCP-recruited versus MKK3/6-activating activities unresolved

Mechanism profile

Synthesis pass · controlled-vocabulary classification · explore literature graph →
Molecular activity
GO:0140096 catalytic activity, acting on a protein 5 GO:0060089 molecular transducer activity 3 GO:0016874 ligase activity 2 GO:0098772 molecular function regulator activity 1
Localization
GO:0005783 endoplasmic reticulum 1 GO:0005829 cytosol 1 GO:0031410 cytoplasmic vesicle 1
Pathway
GO:0140096 catalytic activity, acting on a protein 3
Complex memberships
CUL3-RING ubiquitin ligase complex

Evidence

Reading pass · 8 per-paper findings extracted from the source corpus
Year Finding Method Journal Conf PMIDs
2015 KBTBD7 (together with KBTBD6) functions as a substrate adaptor for a CUL3 RING ubiquitin ligase complex that mediates ubiquitylation and proteasomal degradation of TIAM1, a RAC1-specific GEF. Depletion of KBTBD6/7 elevates TIAM1 abundance, increases RAC1 activity, alters actin morphology, causes loss of focal adhesions, reduces proliferation, and enhances invasion. KBTBD7 employs ATG8 family-interacting motifs to bind preferentially to GABARAP proteins, and ubiquitylation of TIAM1 by CUL3-KBTBD6/KBTBD7 depends on GABARAP binding, revealing that recruitment to GABARAP-containing vesicles spatially restricts RAC1 signaling. Co-immunoprecipitation, ubiquitylation assays, siRNA knockdown with actin morphology/invasion/proliferation readouts, ATG8-family binding motif mutagenesis, vesicle recruitment assays Molecular cell High 25684205 27308540
2021 KBTBD7 acts as an E3 ligase that is recruited by p97/VCP via UBA-UBX adaptors to promote ubiquitination and ERAD (endoplasmic reticulum-associated degradation) of the Wnt/PCP core components Vangl1 and Vangl2. Wnt5a/CK1-induced phosphorylation of Vangl prevents its ubiquitination by KBTBD7 and facilitates its export from the ER to the plasma membrane. In vivo, KBTBD7 regulates convergent extension during zebrafish gastrulation, consistent with its role in controlling Vangl abundance. Co-immunoprecipitation (p97/VCP–KBTBD7 and KBTBD7–Vangl interactions), ubiquitination assays, ERAD assays, phosphorylation-blocking mutants, zebrafish convergent-extension phenotype rescue/loss-of-function Science advances High 33990333
2020 KBTBD7 directly interacts with and ubiquitinates dopamine type 2 receptor (DRD2) at five specific lysine residues (K221, K226, K241, K251, K258), targeting internalized DRD2 for proteasomal degradation. KBTBD7 knockout mice show elevated DRD2 protein in pituitary, thalamus, and heart. KBTBD7-mediated DRD2 degradation attenuates cabergoline-induced inhibition of the AKT/mTOR pathway, and knockdown of KBTBD6/7 sensitizes pituitary tumor cells to dopamine agonist treatment. Yeast two-hybrid, Co-IP, ubiquitination site mapping, CRISPR-Cas9 knockout mice with DRD2 protein quantification, cell-based knockdown/overexpression with AKT/mTOR signaling readouts Acta neuropathologica High 32572597
2018 KBTBD7 is a direct target of miR-21 (validated by luciferase reporter assay) and promotes DAMP-triggered inflammatory responses in macrophages. KBTBD7 physically interacts with MKK3/6 and promotes their activation, which in turn enhances downstream p38 and NF-κB signaling induced by DAMPs (HMGB1 and HSP60). miR-21 deficiency elevates KBTBD7 expression and exacerbates this signaling axis post-MI. Luciferase reporter assay (miR-21 targeting of KBTBD7 3'UTR), Co-immunoprecipitation (KBTBD7–MKK3/6 interaction), miR-21 knockout mice, siRNA knockdown with cytokine and phospho-signaling readouts Cell death & disease Medium 29991775
2022 KBTBD7 promotes ubiquitin-dependent proteasomal degradation of PTEN in non-small cell lung cancer cells, thereby activating EGFR/PI3K/AKT signaling and promoting cell proliferation and invasion. KBTBD7 knockdown in NSCLC cell lines with PTEN protein level measurement, ubiquitination assays, downstream signaling (AKT) and proliferation/invasion readouts Cancer medicine Medium 35499228
2024 KBTBD7 acts as an E3 ubiquitin ligase that directly binds KLF15 transcription factor (confirmed by Co-IP) and catalyzes its ubiquitination and proteasomal degradation. Loss of KBTBD7 in LPS-treated microglia stabilizes KLF15, suppresses NLRP3 inflammasome and NF-κB signaling activation, and reduces pro-inflammatory cytokine release; KLF15 knockdown abolishes this anti-inflammatory effect. Co-immunoprecipitation (KBTBD7–KLF15), ubiquitination assays, siRNA knockdown with NLRP3/NF-κB signaling readouts, epistasis rescue experiment (KLF15 KD reverting KBTBD7 KD phenotype) Experimental cell research Medium 39489209
2024 KBTBD7 interacts with FOXA1 and promotes FOXA1 expression, which indirectly inhibits SLC7A11 transcription; this axis drives ferroptosis and mitochondrial dysfunction in LPS-treated alveolar epithelial cells. KBTBD7 knockdown reduces ROS production, ferroptosis markers, and inflammatory cytokines in vitro and in a septic lung injury mouse model. Co-immunoprecipitation (KBTBD7–FOXA1), siRNA knockdown in LPS-induced cells and in vivo CLP model with ferroptosis/ROS/cytokine readouts International immunopharmacology Low 38652964
2010 KBTBD7 protein (684 aa, 77 kDa) localizes to the cytoplasm in COS-7 cells. When fused to a GAL4 DNA-binding domain, KBTBD7 activates transcription; deletion analysis shows the BTB domain and kelch repeat motif are the main regions for transcriptional activation. Overexpression in MCF-7 cells activates AP-1 and SRE transcriptional activities, an effect reversed by siRNA knockdown. Western blot (expression/localization), GAL4-fusion transcription assay, deletion constructs, AP-1/SRE luciferase reporter assays, siRNA knockdown BMB reports Medium 20132730

Source papers

Stage 0 corpus · 18 papers · ranked by NIH iCite citations
Year Title Journal Citations PMID
2018 MicroRNA-21 prevents excessive inflammation and cardiac dysfunction after myocardial infarction through targeting KBTBD7. Cell death & disease 154 29991775
2015 CUL3-KBTBD6/KBTBD7 ubiquitin ligase cooperates with GABARAP proteins to spatially restrict TIAM1-RAC1 signaling. Molecular cell 71 25684205
2021 Regulation of Wnt/PCP signaling through p97/VCP-KBTBD7-mediated Vangl ubiquitination and endoplasmic reticulum-associated degradation. Science advances 40 33990333
2020 The KBTBD6/7-DRD2 axis regulates pituitary adenoma sensitivity to dopamine agonist treatment. Acta neuropathologica 29 32572597
2019 Berberine reduces inflammation of human dental pulp fibroblast via miR-21/KBTBD7 axis. Archives of oral biology 22 31837588
2020 Mutations of RNF213 are responsible for sporadic cerebral cavernous malformation and lead to a mulberry-like cluster in zebrafish. Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism 16 32248732
2025 Linear ubiquitination at damaged lysosomes induces local NFKB activation and controls cell survival. Autophagy 13 39744815
2009 New TFII-I family target genes involved in embryonic development. Biochemical and biophysical research communications 13 19527686
2010 KBTBD7, a novel human BTB-kelch protein, activates transcriptional activities of SRE and AP-1. BMB reports 12 20132730
2024 Knockdown of KBTBD7 attenuates septic lung injury by inhibiting ferroptosis and improving mitochondrial dysfunction. International immunopharmacology 9 38652964
2023 Study on Potential Differentially Expressed Genes in Idiopathic Pulmonary Fibrosis by Bioinformatics and Next-Generation Sequencing Data Analysis. Biomedicines 8 38137330
2022 Circ-GTF2I/miR-590-5p Axis Aggravates Myocardial Ischemia-Reperfusion Injury by Regulating Kelch Repeat and BTB Domain-Containing Protein 7. Evidence-based complementary and alternative medicine : eCAM 8 35668777
2022 Crocin inhibits KBTBD7 to prevent excessive inflammation and cardiac dysfunction following myocardial infarction. Molecular medicine reports 8 36484363
2020 Bioinformatics enrichment analysis of genes and pathways related to maternal type 1 diabetes associated with adverse fetal outcomes. Journal of diabetes and its complications 8 32046932
2022 KBTBD7 promotes non-small cell lung carcinoma progression by enhancing ubiquitin-dependent degradation of PTEN. Cancer medicine 6 35499228
2022 A transcriptome-wide association study of uterine fibroids to identify potential genetic markers and toxic chemicals. PloS one 6 36174000
2015 GABARAP proteins as scaffolds in localized TIAM1-RAC1 signaling. Molecular & cellular oncology 3 27308540
2024 Targeting of ubiquitination and degradation of KLF15 by E3 ubiquitin ligase KBTBD7 regulates LPS-induced septic brain injury in microglia. Experimental cell research 2 39489209

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