General Information of Target

Target ID LDTP08579
Target Name Protein KIBRA (WWC1)
Gene Name WWC1
Gene ID 23286
Synonyms
KIAA0869; Protein KIBRA; HBeAg-binding protein 3; Kidney and brain protein; KIBRA; WW domain-containing protein 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MPRPELPLPEGWEEARDFDGKVYYIDHTNRTTSWIDPRDRYTKPLTFADCISDELPLGWE
EAYDPQVGDYFIDHNTKTTQIEDPRVQWRREQEHMLKDYLVVAQEALSAQKEIYQVKQQR
LELAQQEYQQLHAVWEHKLGSQVSLVSGSSSSSKYDPEILKAEIATAKSRVNKLKREMVH
LQHELQFKERGFQTLKKIDKKMSDAQGSYKLDEAQAVLRETKAIKKAITCGEKEKQDLIK
SLAMLKDGFRTDRGSHSDLWSSSSSLESSSFPLPKQYLDVSSQTDISGSFGINSNNQLAE
KVRLRLRYEEAKRRIANLKIQLAKLDSEAWPGVLDSERDRLILINEKEELLKEMRFISPR
KWTQGEVEQLEMARKRLEKDLQAARDTQSKALTERLKLNSKRNQLVRELEEATRQVATLH
SQLKSLSSSMQSLSSGSSPGSLTSSRGSLVASSLDSSTSASFTDLYYDPFEQLDSELQSK
VEFLLLEGATGFRPSGCITTIHEDEVAKTQKAEGGGRLQALRSLSGTPKSMTSLSPRSSL
SSPSPPCSPLMADPLLAGDAFLNSLEFEDPELSATLCELSLGNSAQERYRLEEPGTEGKQ
LGQAVNTAQGCGLKVACVSAAVSDESVAGDSGVYEASVQRLGASEAAAFDSDESEAVGAT
RIQIALKYDEKNKQFAILIIQLSNLSALLQQQDQKVNIRVAVLPCSESTTCLFRTRPLDA
SDTLVFNEVFWVSMSYPALHQKTLRVDVCTTDRSHLEECLGGAQISLAEVCRSGERSTRW
YNLLSYKYLKKQSRELKPVGVMAPASGPASTDAVSALLEQTAVELEKRQEGRSSTQTLED
SWRYEETSENEAVAEEEEEEVEEEEGEEDVFTEKASPDMDGYPALKVDKETNTETPAPSP
TVVRPKDRRVGTPSQGPFLRGSTIIRSKTFSPGPQSQYVCRLNRSDSDSSTLSKKPPFVR
NSLERRSVRMKRPSSVKSLRSERLIRTSLDLELDLQATRTWHSQLTQEISVLKELKEQLE
QAKSHGEKELPQWLREDERFRLLLRMLEKRQMDRAEHKGELQTDKMMRAAAKDVHRLRGQ
SCKEPPEVQSFREKMAFFTRPRMNIPALSADDV
Target Bioclass
Other
Family
WWC family, KIBRA subfamily
Subcellular location
Cytoplasm
Function
Negative regulator of the Hippo signaling pathway, also known as the Salvador-Warts-Hippo (SWH) pathway. Enhances phosphorylation of LATS1 and YAP1 and negatively regulates cell proliferation and organ growth due to a suppression of the transcriptional activity of YAP1, the major effector of the Hippo pathway. Along with NF2 can synergistically induce the phosphorylation of LATS1 and LATS2 and function in the regulation of Hippo signaling pathway. Acts as a transcriptional coactivator of ESR1 which plays an essential role in DYNLL1-mediated ESR1 transactivation. Regulates collagen-stimulated activation of the ERK/MAPK cascade. Modulates directional migration of podocytes. Plays a role in cognition and memory performance. Plays an important role in regulating AMPA-selective glutamate receptors (AMPARs) trafficking underlying synaptic plasticity and learning.
Uniprot ID
Q8IX03
Ensemble ID
ENST00000265293.9
HGNC ID
HGNC:29435

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A431 Insertion: p.E158LfsTer4
SNV: p.E158K
.
COLO792 SNV: p.L919F .
COLO800 SNV: p.E1029D .
DU4475 SNV: p.E394K .
HCT15 SNV: p.L995M .
HEP3B217 SNV: p.E105V .
HT115 SNV: p.S1024G .
Ishikawa (Heraklio) 02 ER SNV: p.D880H .
LN18 SNV: p.E1020Q .
MDAMB453 SNV: p.E353Q .
NCIH1048 SNV: p.E346K .
OSRC2 SNV: p.V700M .
OZ SNV: p.S268G .
RH41 SNV: p.E310D .
SKMEL3 SNV: p.P704S .
SNU1 Insertion: p.L273AfsTer37 .
TKKK SNV: p.S268G .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 6 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info 
K246(1.89); K319(10.00)  LDD0277  [1]
DBIA
 Probe Info 
C940(2.07)  LDD3346  [2]
IA-alkyne
 Probe Info 
N.A.  LDD0165  [3]
NAIA_4
 Probe Info 
C497(0.00); C1082(0.00)  LDD2226  [4]
IPM
 Probe Info 
C1082(0.00); C940(0.00)  LDD0147  [5]
Acrolein
 Probe Info 
H420(0.00); K424(0.00)  LDD0217  [6]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C611(1.35)  LDD1702  [7]
 LDCM0576  Fragment14 Ramos C940(1.23)  LDD2193  [8]
 LDCM0580  Fragment21 Ramos C940(1.26)  LDD2195  [8]
 LDCM0578  Fragment27 Ramos C940(1.43)  LDD2197  [8]
 LDCM0586  Fragment28 Ramos C940(0.98)  LDD2198  [8]
 LDCM0589  Fragment31 Ramos C940(1.32)  LDD2200  [8]
 LDCM0468  Fragment33 Ramos C940(0.83)  LDD2202  [8]
 LDCM0596  Fragment38 Ramos C940(1.95)  LDD2203  [8]
 LDCM0610  Fragment52 Ramos C940(2.73)  LDD2204  [8]
 LDCM0614  Fragment56 Ramos C940(1.09)  LDD2205  [8]
 LDCM0022  KB02 786-O C230(2.91); C611(2.62); C940(3.74)  LDD2247  [2]
 LDCM0023  KB03 786-O C230(2.09); C611(3.57); C940(4.67)  LDD2664  [2]
 LDCM0024  KB05 NCI-H1666 C940(2.07)  LDD3346  [2]

References

1 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
2 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
3 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
4 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
5 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
6 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
7 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
8 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578