Bladder exstrophy-epispadias-cloacal exstrophy complex

disease
On this page

Also known as BEEC

Summary

Bladder exstrophy-epispadias-cloacal exstrophy complex (MONDO:0700039) is a disease with 29 cohort genes. The dominant Reactome pathway is Class B/2 (Secretin family receptors) (4 cohort genes).

At a glance

  • Cohort genes: 29
  • ClinVar variants: 34

Clinical features

No curated clinical features (Orphanet) for this disease.

Identifiers

Disease identifiers

FieldValue
Canonical namebladder exstrophy-epispadias-cloacal exstrophy complex
Mondo IDMONDO:0700039
OMIM600057
UMLSC1838703
MedGen374033
GARD0026333
Is cancer (heuristic)no

Also known as: BEEC

Data availability: 34 ClinVar variants.

Disease family

Classification path: disease › human disease › disease by body system or component › urinary system disorderkidney disorderexstrophy-epispadias complexbladder exstrophy-epispadias-cloacal exstrophy complex

Related subtypes (3): cloacal exstrophy, bladder exstrophy, epispadias

Genetics & variants

GWAS landscape

No GWAS associations recorded — common-variant (GWAS) studies don’t cover this disease (typical for Mendelian / rare diseases). See the curated gene cohort and Mendelian overlap below.

Variant details and genetic-evidence tiers

ClinVar germline variants

34 retrieved; paginated sample, class counts are floors:

22 uncertain significance, 5 conflicting classifications of pathogenicity, 3 benign, 2 benign/likely benign, 1 likely pathogenic, 1 likely benign

ClinVarVariant (HGVS)GeneClassificationReview
189347NM_030753.5(WNT3):c.271T>C (p.Cys91Arg)LRRC37A2Likely pathogenicno assertion criteria provided
3142105NM_001407.3(CELSR3):c.5875G>A (p.Ala1959Thr)CELSR3Conflicting classifications of pathogenicitycriteria provided, conflicting classifications
328424NM_173483.4(CYP4F22):c.160C>T (p.Arg54Cys)CYP4F22Conflicting classifications of pathogenicitycriteria provided, conflicting classifications
586256NM_001009944.3(PKD1):c.2192C>T (p.Pro731Leu)PKD1Conflicting classifications of pathogenicitycriteria provided, conflicting classifications
2184324NM_018419.3(SOX18):c.766C>T (p.Arg256Trp)SOX18Conflicting classifications of pathogenicitycriteria provided, conflicting classifications
189351NM_025216.3(WNT10A):c.487C>T (p.Arg163Trp)WNT10AConflicting classifications of pathogenicitycriteria provided, conflicting classifications
2245482NM_032208.3(ANTXR1):c.1331G>A (p.Arg444Gln)ANTXR1Uncertain significancecriteria provided, multiple submitters, no conflicts
2627998NM_001195637.2(CCDC179):c.25G>C (p.Glu9Gln)CCDC179Uncertain significancecriteria provided, single submitter
2628006NM_005232.5(EPHA1):c.256A>T (p.Ile86Phe)EPHA1Uncertain significancecriteria provided, single submitter
189354NM_003468.4(FZD5):c.267G>A (p.Met89Ile)FZD5Uncertain significanceno assertion criteria provided
373894NM_002202.3(ISL1):c.479-4G>AISL1Uncertain significancecriteria provided, single submitter
374407NM_002202.3(ISL1):c.137C>G (p.Ala46Gly)ISL1Uncertain significancecriteria provided, single submitter
2628007NM_006618.5(KDM5B):c.4364G>A (p.Arg1455His)KDM5BUncertain significancecriteria provided, multiple submitters, no conflicts
2628008NM_001306080.2(LMO7):c.1883G>C (p.Arg628Thr)LMO7Uncertain significancecriteria provided, single submitter
189350NM_004625.4(WNT7A):c.487G>A (p.Ala163Thr)LOC126806608Uncertain significanceno assertion criteria provided
189356NM_014045.5(LRP10):c.754G>A (p.Gly252Ser)LRP10Uncertain significanceno assertion criteria provided
189357NM_030753.5(WNT3):c.638G>A (p.Gly213Asp)LRRC37A2Uncertain significanceno assertion criteria provided
2628009NM_001004749.2(OR51A7):c.64C>T (p.His22Tyr)MMP26Uncertain significancecriteria provided, single submitter
2628010NM_023014.1(PRAMEF2):c.1195C>T (p.Arg399Cys)PRAMEF2Uncertain significancecriteria provided, single submitter
2628011NM_016277.5(RAB23):c.17T>G (p.Met6Arg)RAB23Uncertain significancecriteria provided, single submitter
2627996NM_006652.2(SPINT3):c.149C>T (p.Thr50Met)SPINT3Uncertain significancecriteria provided, single submitter
2627992NM_007271.4(STK38):c.630_631del (p.His210fs)STK38Uncertain significancecriteria provided, single submitter
2627993NM_001008536.2(TCHHL1):c.1529T>C (p.Val510Ala)TCHHL1Uncertain significancecriteria provided, single submitter
1402802NM_003722.5(TP63):c.1530G>T (p.Met510Ile)TP63Uncertain significancecriteria provided, multiple submitters, no conflicts
2627994NM_012217.3(TPSD1):c.282G>C (p.Arg94Ser)TPSD1Uncertain significancecriteria provided, single submitter
2627995NM_000369.5(TSHR):c.263C>T (p.Thr88Ile)TSHRUncertain significancecriteria provided, single submitter
3236723NM_001371589.1(WIZ):c.4637A>G (p.Gln1546Arg)WIZUncertain significancecriteria provided, single submitter
189352NM_004626.3(WNT11):c.947G>A (p.Arg316His)WNT11Uncertain significanceno assertion criteria provided
3236724NM_014482.3(BMP10):c.599C>G (p.Thr200Ser)BMP10Benign/Likely benigncriteria provided, multiple submitters, no conflicts
2672914NM_001378328.1(CELSR1):c.7313G>A (p.Arg2438Gln)CELSR1Benign/Likely benigncriteria provided, multiple submitters, no conflicts

Genes & proteins

Mendelian disease overlap and somatic drivers

GenCC: 0 · Orphanet: 36 · OMIM-shared: 0 · Dual-evidence (GWAS+Mendelian): 0

Orphanet rare-disease linkage (cohort genes)

GeneOrphanet IDRare disease
SOX18Orphanet:69735Hypotrichosis-lymphedema-telangiectasia-renal defect syndrome
TSHROrphanet:424Familial hyperthyroidism due to mutations in TSH receptor
TSHROrphanet:90673Hypothyroidism due to TSH receptor mutations
TSHROrphanet:95713Athyreosis
TSHROrphanet:95720Thyroid hypoplasia
TSHROrphanet:99819Familial gestational hyperthyroidism
WNT10AOrphanet:248Autosomal recessive hypohidrotic ectodermal dysplasia
WNT10AOrphanet:2721Odonto-onycho-dermal dysplasia
WNT10AOrphanet:50944Schöpf-Schulz-Passarge syndrome
WNT10AOrphanet:99798Oligodontia
RAB23Orphanet:65759Carpenter syndrome
TP63Orphanet:1072Ankyloblepharon filiforme adnatum-cleft palate syndrome
TP63Orphanet:141291Cleft lip and alveolus
TP63Orphanet:1896EEC syndrome
TP63Orphanet:199302Isolated cleft lip
TP63Orphanet:199306Cleft lip/palate
TP63Orphanet:2440Isolated split hand-split foot malformation
TP63Orphanet:69085Limb-mammary syndrome
TP63Orphanet:93930Classic bladder exstrophy
TP63Orphanet:978ADULT syndrome
KDM5BOrphanet:178469Autosomal dominant non-syndromic intellectual disability
KDM5BOrphanet:88616Autosomal recessive non-syndromic intellectual disability
CELSR1Orphanet:569816CELSR1-related late-onset primary lymphedema
ANTXR1Orphanet:2067GAPO syndrome
CYP4F22Orphanet:313Lamellar ichthyosis
FZD5Orphanet:98942Coloboma of choroid and retina
FZD5Orphanet:98943Coloboma of eye lens
FZD5Orphanet:98944Coloboma of iris
FZD5Orphanet:98945Coloboma of macula
FZD5Orphanet:98946Coloboma of eyelid
FZD5Orphanet:98947Coloboma of optic disc
ISL1Orphanet:93930Classic bladder exstrophy
PKD1Orphanet:730Autosomal dominant polycystic kidney disease
PKD1Orphanet:88924Autosomal dominant polycystic kidney disease type 1 with tuberous sclerosis
PRKD1Orphanet:276145Malignant epithelial tumor of salivary glands
PRKD1Orphanet:708019Congenital heart defect-ectodermal dysplasia- brachydactyly-telangiectasia syndrome

Cohort genes → proteins

29 cohort genes, 29 distinct canonical proteins.

Evidence partition

SubsetGenes
multi_evidence29

Cohort genes (full)

SymbolHGNCEnsemblUniProtNameEvidence
SOX18HGNC:11194ENSG00000203883P35713Transcription factor SOX-18clinvar
SPINT3HGNC:11248ENSG00000101446P49223Kunitz-type protease inhibitor 3clinvar
TSHRHGNC:12373ENSG00000165409P16473Thyrotropin receptorclinvar
WNT11HGNC:12776ENSG00000085741O96014Protein Wnt-11clinvar
WNT6HGNC:12785ENSG00000115596Q9Y6F9Protein Wnt-6clinvar
WNT10AHGNC:13829ENSG00000135925Q9GZT5Protein Wnt-10aclinvar
TPSD1HGNC:14118ENSG00000095917Q9BZJ3Tryptase deltaclinvar
MMP26HGNC:14249ENSG00000167346Q9NRE1Matrix metalloproteinase-26clinvar
RAB23HGNC:14263ENSG00000112210Q9ULC3Ras-related protein Rab-23clinvar
LRP10HGNC:14553ENSG00000197324Q7Z4F1Low-density lipoprotein receptor-related protein 10clinvar
TP63HGNC:15979ENSG00000073282Q9H3D4Tumor protein 63clinvar
STK38HGNC:17847ENSG00000112079Q15208Serine/threonine-protein kinase 38clinvar
KDM5BHGNC:18039ENSG00000117139Q9UGL1Lysine-specific demethylase 5Bclinvar
CELSR1HGNC:1850ENSG00000075275Q9NYQ6Cadherin EGF LAG seven-pass G-type receptor 1clinvar
BMP10HGNC:20869ENSG00000163217O95393Bone morphogenetic protein 10clinvar
ANTXR1HGNC:21014ENSG00000169604Q9H6X2Anthrax toxin receptor 1clinvar
CYP4F22HGNC:26820ENSG00000171954Q6NT55Ultra-long-chain fatty acid omega-hydroxylaseclinvar
PRAMEF2HGNC:28841ENSG00000120952O60811PRAME family member 2clinvar
WIZHGNC:30917ENSG00000011451O95785Protein Wizclinvar
TCHHL1HGNC:31796ENSG00000182898Q5QJ38Trichohyalin-like protein 1clinvar
CELSR3HGNC:3230ENSG00000008300Q9NYQ7Cadherin EGF LAG seven-pass G-type receptor 3clinvar
LRRC37A2HGNC:32404ENSG00000238083A6NM11Leucine-rich repeat-containing protein 37A2clinvar
EPHA1HGNC:3385ENSG00000146904P21709Ephrin type-A receptor 1clinvar
FZD5HGNC:4043ENSG00000163251Q13467Frizzled-5clinvar
CCDC179HGNC:44653ENSG00000255359H3BU77Coiled-coil domain-containing protein 179clinvar
ISL1HGNC:6132ENSG00000016082P61371Insulin gene enhancer protein ISL-1clinvar
LMO7HGNC:6646ENSG00000136153Q8WWI1LIM domain only protein 7clinvar
PKD1HGNC:9008ENSG00000008710P98161Polycystin-1clinvar
PRKD1HGNC:9407ENSG00000184304Q15139Serine/threonine-protein kinase D1clinvar

Cohort function summary

Lead sentence per gene, UniProt-curated.

SymbolProtein nameFunction (lead sentence)
SOX18Transcription factor SOX-18Transcriptional activator that binds to the consensus sequence 5’-AACAAAG-3’ in the promoter of target genes and plays an essential role in embryonic cardiovascular development and lymphangiogenesis.
TSHRThyrotropin receptorReceptor for the thyroid-stimulating hormone (TSH) or thyrotropin.
WNT11Protein Wnt-11Ligand for members of the frizzled family of seven transmembrane receptors.
WNT6Protein Wnt-6Ligand for members of the frizzled family of seven transmembrane receptors.
WNT10AProtein Wnt-10aLigand for members of the frizzled family of seven transmembrane receptors.
TPSD1Tryptase deltaTryptase is the major neutral protease present in mast cells and is secreted upon the coupled activation-degranulation response of this cell type.
MMP26Matrix metalloproteinase-26May hydrolyze collagen type IV, fibronectin, fibrinogen, beta-casein, type I gelatin and alpha-1 proteinase inhibitor.
RAB23Ras-related protein Rab-23The small GTPases Rab are key regulators of intracellular membrane trafficking, from the formation of transport vesicles to their fusion with membranes.
LRP10Low-density lipoprotein receptor-related protein 10Probable receptor, which is involved in the internalization of lipophilic molecules and/or signal transduction.
TP63Tumor protein 63Acts as a sequence specific DNA binding transcriptional activator or repressor.
STK38Serine/threonine-protein kinase 38Serine/threonine-protein kinase that acts as a negative regulator of MAP3K1/2 signaling.
KDM5BLysine-specific demethylase 5BHistone demethylase that demethylates ‘Lys-4’ of histone H3, thereby playing a central role in histone code.
CELSR1Cadherin EGF LAG seven-pass G-type receptor 1Receptor that may have an important role in cell/cell signaling during nervous system formation.
BMP10Bone morphogenetic protein 10Required for maintaining the proliferative activity of embryonic cardiomyocytes by preventing premature activation of the negative cell cycle regulator CDKN1C/p57KIP and maintaining the required expression levels of cardiogenic factors suc…
ANTXR1Anthrax toxin receptor 1Plays a role in cell attachment and migration.
CYP4F22Ultra-long-chain fatty acid omega-hydroxylaseA cytochrome P450 monooxygenase involved in epidermal ceramide biosynthesis.
WIZProtein WizMay link EHMT1 and EHMT2 histone methyltransferases to the CTBP corepressor machinery.
CELSR3Cadherin EGF LAG seven-pass G-type receptor 3Receptor that may have an important role in cell/cell signaling during nervous system formation.
EPHA1Ephrin type-A receptor 1Receptor tyrosine kinase which binds promiscuously membrane-bound ephrin-A family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells.
FZD5Frizzled-5Receptor for Wnt proteins.
ISL1Insulin gene enhancer protein ISL-1DNA-binding transcriptional activator.
PKD1Polycystin-1Component of a heteromeric calcium-permeable ion channel formed by PKD1 and PKD2 that is activated by interaction between PKD1 and a Wnt family member, such as WNT3A and WNT9B.
PRKD1Serine/threonine-protein kinase D1Serine/threonine-protein kinase that converts transient diacylglycerol (DAG) signals into prolonged physiological effects downstream of PKC, and is involved in the regulation of MAPK8/JNK1 and Ras signaling, Golgi membrane integrity and tr…

Protein-family classification

Druggable: 11 · Difficult: 6 · Unknown: 12 · Druggable fraction: 0.38

Family distribution

Cohort families vs a genome-wide background (hypergeometric, BH-FDR; fold = observed/expected). Counts kept; sorted by enrichment, so the catch-all Other/Unknown bucket no longer leads.

FamilyGenesFoldFDR
GPCR43.3×0.219
Kinase32.9×0.299
Transcription factor61.7×0.305
Protease22.5×0.328
Antibody/Immunoglobulin11.0×0.891
Other/Unknown120.7×0.960
Enzyme (other)10.4×0.960

Per-gene assignment

SymbolFamilyDruggable?ECInterPro (top 3)
SOX18Transcription factornoHMG_box_dom, Sox_C, Sox7/17/18_central
SPINT3Other/UnknownnoKunitz_BPTI, Prtase_inh_Kunz-CS, Kunitz_BPTI_sf
TSHRGPCRyesGPCR_Rhodpsn, Gphrmn_rcpt_fam, TSH_rcpt
WNT11Other/UnknownnoWnt, Wnt_CS, Wnt_C
WNT6Other/UnknownnoWnt, Wnt6, Wnt_CS
WNT10AOther/UnknownnoWnt, Wnt10, Wnt_CS
TPSD1ProteaseyesTrypsin_dom, Peptidase_S1A, Peptidase_S1_PA
MMP26Proteaseyes3.4.24.B7Pept_M10_metallopeptidase, Peptidase_Metallo, Pept_M10A
RAB23Other/UnknownnoSmall_GTPase, Small_GTP-bd, P-loop_NTPase
LRP10Other/UnknownnoCUB_dom, LDrepeatLR_classA_rpt, LDLR_class-A_CS
TP63Transcription factornoSAM, p53_tumour_suppressor, p53-like_TF_DNA-bd_sf
STK38Kinaseyes2.7.11.1Prot_kinase_dom, AGC-kinase_C, Ser/Thr_kinase_AS
KDM5BTranscription factorno1.14.11.67ARID_dom, Znf_PHD, JmjC_dom
CELSR1GPCRyesEGF-type_Asp/Asn_hydroxyl_site, GPS, EGF
BMP10Other/UnknownnoTGF-b_propeptide, TGF-b_C, TGF-beta-like
ANTXR1Other/UnknownnoVWF_A, Anthrax_toxin_rcpt_C, Anthrax_toxin_rcpt_extracel
CYP4F22Enzyme (other)yes1.14.14.177Cyt_P450, Cyt_P450_E_grp-I, Cyt_P450_CS
PRAMEF2Other/UnknownnoPRAME, LRR_dom_sf, LRRC14/PRAME
WIZTranscription factornoZnf_C2H2_type, Znf_C2H2_sf, Transcr_Reg_ZincFinger
TCHHL1Other/UnknownnoEF-hand-dom_pair, S100_Ca-bd_sub, S-100_dom
CELSR3GPCRyesGPS, EGF, GPCR_2_secretin-like
LRRC37A2Other/UnknownnoLeu-rich_rpt, Leu-rich_rpt_typical-subtyp, LRRC37
EPHA1Kinaseyes2.7.10.1Prot_kinase_dom, EPH_LBD, Ser-Thr/Tyr_kinase_cat_dom
FZD5GPCRyesFrizzled/Smoothened_7TM, Frizzled/SFRP, GPCR_2-like_7TM
CCDC179Other/Unknownno
ISL1Transcription factornoHD, Znf_LIM, Homeodomain-like_sf
LMO7Transcription factornoPDZ, CH_dom, Znf_LIM
PKD1Antibody/ImmunoglobulinyesGPS, LRRNT, PC1
PRKD1Kinaseyes2.7.11.13Prot_kinase_dom, PH_domain, PKC_DAG/PE

Expression context

Cohort genes with no expression data: 0.

23 cohort genes are a single-cell marker in ≥1 SCXA experiment.

Breadth distribution (Bgee present_calls)

BucketGenes
narrow (1-5 tissues)2
moderate (6-20)0
broad (>20)27
unknown0

Top tissues across cohort

TissueCohort genes
lower esophagus mucosa5
secondary oocyte3
ventricular zone3
sural nerve3
cerebellar hemisphere3
apex of heart2
right lung2
cauda epididymis2
male germ cell2
sperm2
bone marrow cell2
male germ line stem cell (sensu Vertebrata) in testis2
decidua2
stromal cell of endometrium2
upper arm skin2
palpebral conjunctiva2
left testis2
skin of leg2
colonic epithelium2
cortical plate2

Per-gene tissue summary (top 30)

SymbolBgee breadthFANTOM5 breadthSCXATop tissues
SOX18165broadmarkerapex of heart, right lung, left uterine tube
SPINT333tissue_specificmarkercauda epididymis, sperm, male germ cell
TSHR169broadmarkerright lobe of thyroid gland, left lobe of thyroid gland, thyroid gland
WNT11178broadmarkeromental fat pad, peritoneum, adipose tissue of abdominal region
WNT6152broadyesendometrium epithelium, tibial nerve, Brodmann (1909) area 10
WNT10A151broadmarkerprimordial germ cell in gonad, lower esophagus mucosa, bone marrow cell
TPSD1122tissue_specificmarkermucosa of transverse colon, right lung, lower esophagus muscularis layer
MMP2638tissue_specificmarkerbuccal mucosa cell, male germ line stem cell (sensu Vertebrata) in testis, endometrium
RAB23264ubiquitousmarkercauda epididymis, saphenous vein, secondary oocyte
LRP10284ubiquitousmarkerstromal cell of endometrium, decidua, right coronary artery
TP63207broadmarkerupper leg skin, skin of hip, upper arm skin
STK38288ubiquitousmarkerpalpebral conjunctiva, oocyte, secondary oocyte
KDM5B272ubiquitousmarkersperm, male germ cell, left testis
CELSR1224ubiquitousmarkerventricular zone, lower esophagus mucosa, bronchial epithelial cell
BMP1090tissue_specificmarkercardiac muscle of right atrium, right atrium auricular region, cardiac atrium
ANTXR1270ubiquitousmarkerstromal cell of endometrium, decidua, palpebral conjunctiva
CYP4F22103tissue_specificmarkerlower esophagus mucosa, upper arm skin, skin of leg
PRAMEF20yescolonic epithelium, sural nerve, ventricular zone
WIZ259ubiquitousmarkercortical plate, ganglionic eminence, right testis
TCHHL14tissue_specificmarkersural nerve, bone marrow cell, colonic epithelium
CELSR3209broadyesright hemisphere of cerebellum, cortical plate, cerebellar hemisphere
LRRC37A2134yesright uterine tube, right testis, cerebellar hemisphere
EPHA1160broadyeslower esophagus mucosa, esophagus mucosa, skin of leg
FZD5256ubiquitousmarkerjejunal mucosa, mucosa of sigmoid colon, colonic mucosa
CCDC17947tissue_specificyesmale germ line stem cell (sensu Vertebrata) in testis, left testis, testis
ISL1148broadmarkersecondary oocyte, cervix squamous epithelium, islet of Langerhans
LMO7214ubiquitousmarkersural nerve, lower esophagus mucosa, apex of heart
PKD1290markerright hemisphere of cerebellum, cerebellar hemisphere, cerebellar cortex
PRKD1239ubiquitousmarkerventricular zone, seminal vesicle, thoracic aorta

Protein interactions among cohort

Intra-cohort edges: 4.

Hub genes (top 10 by interactor count)

SymbolInteractor count
KDM5B3,722
EPHA12,975
TP632,893
STK382,465
PRAMEF22,317
PRKD12,131
ANTXR12,039
WNT112,017
LMO71,976
TSHR1,672

Intra-cohort edges

ABSources
FZD5WNT10Astring_interaction
FZD5WNT11string_interaction
FZD5WNT6string_interaction
PKD1PRKD1string_interaction

Structural data

PDB: 13 · AlphaFold-only: 16 · No structure: 0

Cohort genes with PDB structures (top 30)

SymbolUniProtPDB entries
KDM5BQ9UGL156
TP63Q9H3D426
PKD1P9816113
TSHRP164739
BMP10O953938
RAB23Q9ULC36
ANTXR1Q9H6X25
EPHA1P217094
FZD5Q134674
WIZO957853
STK38Q152082
CELSR1Q9NYQ62
LMO7Q8WWI11

AlphaFold-only cohort genes (top 30 by pLDDT)

SymbolUniProtpLDDT
CYP4F22Q6NT5593.59
SPINT3P4922393.13
WNT11O9601490.35
TPSD1Q9BZJ385.89
WNT6Q9Y6F983.62
WNT10AQ9GZT582.36
PRAMEF2O6081181.46
CCDC179H3BU7780.41
MMP26Q9NRE179.33
ISL1P6137172.57
PRKD1Q1513968.99
LRP10Q7Z4F167.84
SOX18P3571363.44
LRRC37A2A6NM1142.32
TCHHL1Q5QJ3842.28
CELSR3Q9NYQ7

Function

Pathway analysis

Distinct Reactome pathways touched by cohort: 87. Enrichment computed across 29 evidence-associated genes (18 with Reactome annotation).

Pathways by enrichment

Over-representation of cohort genes vs the genome-wide background (hypergeometric test, Benjamini-Hochberg FDR; fold = observed/expected over 18 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

PathwayCohort genesFoldFDRSample cohort genes
Class B/2 (Secretin family receptors)442.3×2e-04WNT11, WNT6, WNT10A, FZD5
WNT ligand biogenesis and trafficking370.5×4e-04WNT11, WNT6, WNT10A
Defective CYP4F22 causes ARCI51634.4×0.046CYP4F22
TFAP2 (AP-2) family regulates transcription of cell cycle factors1126.9×0.094KDM5B
Signaling by RNF43 mutants170.5×0.094FZD5
Activation of PUMA and translocation to mitochondria163.4×0.094TP63
Incretin synthesis, secretion, and inactivation157.7×0.094ISL1
Miscellaneous substrates152.9×0.094CYP4F22
Eicosanoids152.9×0.094CYP4F22
Hormone ligand-binding receptors152.9×0.094TSHR
Uptake and function of anthrax toxins152.9×0.094ANTXR1
TP53 Regulates Transcription of Caspase Activators and Caspases152.9×0.094TP63
TP53 Regulates Transcription of Death Receptors and Ligands152.9×0.094TP63
POU5F1 (OCT4), SOX2, NANOG activate genes related to proliferation148.8×0.094EPHA1
Synthesis, secretion, and inactivation of Glucose-dependent Insulinotropic Polypeptide (GIP)148.8×0.094ISL1
WNT5A-dependent internalization of FZD2, FZD5 and ROR2148.8×0.094FZD5
Regulation of TP53 Activity through Association with Co-factors145.3×0.094TP63
RHOBTB GTPase Cycle145.3×0.094STK38
TP53 regulates transcription of several additional cell death genes whose specific roles in p53-dependent apoptosis remain uncertain142.3×0.094TP63
Developmental Lineage of Mammary Stem Cells142.3×0.094TP63
Fatty acids139.6×0.094CYP4F22
Maternal to zygotic transition (MZT)139.6×0.094KDM5B
Ca2+ pathway219.8×0.094WNT11, FZD5
Transcriptional regulation by the AP-2 (TFAP2) family of transcription factors135.2×0.101KDM5B
Synthesis of Leukotrienes (LT) and Eoxins (EX)131.7×0.101CYP4F22
TP53 Regulates Transcription of Genes Involved in Cytochrome C Release130.2×0.101TP63
Developmental Lineage of Mammary Gland Myoepithelial Cells130.2×0.101TP63
Regulation of FZD by ubiquitination128.8×0.101FZD5
VxPx cargo-targeting to cilium128.8×0.101PKD1
Formation of the ureteric bud127.6×0.101WNT11

GO biological processes by enrichment

Over-representation of cohort genes vs the genome-wide background (hypergeometric test, Benjamini-Hochberg FDR; fold = observed/expected over 25 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

GO termCohort genesFoldFDRSample cohort genes
canonical Wnt signaling pathway530.6×2e-04WNT11, WNT6, WNT10A, FZD5, ISL1
cloacal septation2674.1×4e-04WNT11, TP63
mesonephric duct development2269.6×0.002WNT11, PKD1
positive regulation of sarcomere organization2224.7×0.002BMP10, PRKD1
negative regulation of mesenchymal cell proliferation2224.7×0.002WNT11, ISL1
Wnt signaling pathway, planar cell polarity pathway354.7×0.002WNT11, CELSR1, CELSR3
outflow tract morphogenesis336.8×0.004SOX18, WNT11, ISL1
cell fate commitment335.5×0.004WNT11, WNT6, WNT10A
neuron differentiation416.1×0.004WNT11, WNT6, WNT10A, FZD5
secondary heart field specification2122.6×0.004WNT11, ISL1
negative regulation of intracellular estrogen receptor signaling pathway289.9×0.007TP63, ISL1
establishment of planar polarity284.3×0.008TP63, CELSR1
positive regulation of gene expression57.8×0.011WNT6, WNT10A, KDM5B, BMP10, PRKD1
axonogenesis319.3×0.013CELSR1, CELSR3, ISL1
ventricular cardiac muscle tissue morphogenesis256.2×0.014BMP10, ISL1
angiogenesis410.0×0.015SOX18, EPHA1, FZD5, PRKD1
homophilic cell-cell adhesion316.9×0.016CELSR1, CELSR3, PKD1
ectoderm and mesoderm interaction1674.1×0.019TP63
axis specification1674.1×0.019WNT6
epidermal cell division1674.1×0.019TP63
thyroid-stimulating hormone signaling pathway1674.1×0.019TSHR
metanephric distal tubule morphogenesis1674.1×0.019PKD1
positive regulation of macrophage colony-stimulating factor production1674.1×0.019ISL1
cellular response to thyrotropin-releasing hormone1674.1×0.019TSHR
regulation of estradiol secretion1674.1×0.019KDM5B
hair follicle morphogenesis239.6×0.019WNT10A, TP63
skin development235.5×0.019WNT10A, PKD1
positive regulation of angiogenesis313.8×0.019EPHA1, ISL1, PRKD1
positive regulation of transcription by RNA polymerase II74.2×0.019SOX18, TP63, FZD5, ISL1, LMO7, PKD1, PRKD1
cell-cell adhesion mediated by cadherin232.9×0.021CELSR1, CELSR3

Therapeutics

Drug target analysis

Approved (phase 4): 4 · Phase ≥3: 6 · Phased (≥1): 6 · Undrugged: 23

Druggability breadth: 12 of 29 evidence-associated genes (41%) have a ChEMBL target (buckets above are over the deeply-mined display cohort).

Genes with an approved drug

The molecule shown is one approved compound that hits the gene — not necessarily a drug of choice or one indicated for this disease.

SymbolExample approved molecule
TSHRLEVOSALBUTAMOL
STK38FEDRATINIB
EPHA1PONATINIB
PRKD1INGENOL MEBUTATE

Top cohort targets by molecule count

SymbolMoleculesMax phase
TSHR3544
EPHA1374
PRKD1264
STK3894
MMP2623
KDM5B23
SOX1800
SPINT300
WNT1100
WNT600

Drugs targeting cohort genes (top 30)

MoleculeMax phaseTargets in cohort
LEVOSALBUTAMOL4TSHR
PROGESTERONE4TSHR
DICLOFENAC SODIUM4TSHR
CLOTRIMAZOLE4TSHR
DAPSONE4TSHR
COLCHICINE4TSHR
OXAPROZIN4TSHR
BUMETANIDE4TSHR
GLIPIZIDE4TSHR
CARBAMAZEPINE4TSHR
METHYL SALICYLATE4TSHR
PHENELZINE4TSHR
EDROPHONIUM4TSHR
SULFAPHENAZOLE4TSHR
AMOXAPINE4TSHR
PYRIDOSTIGMINE4TSHR
ACETAMINOPHEN4TSHR
DICYCLOMINE4TSHR
IODIPAMIDE4TSHR
TESTOSTERONE PROPIONATE4TSHR
TETRABENAZINE4TSHR
CELECOXIB4TSHR
PROPANTHELINE4TSHR
BENOXINATE4TSHR
NICARDIPINE HYDROCHLORIDE4TSHR
PYRITHIONE ZINC4TSHR
GUANABENZ ACETATE4TSHR
PROPIOLACTONE4TSHR
CHLOROTRIANISENE4TSHR
PHENOXYBENZAMINE HYDROCHLORIDE4TSHR

Bioactivity and enzyme data

Enzyme cohort genes (≥1 EC): 6.

Cohort genes with ChEMBL bioactivity (full, sorted by assay count)

SymbolAssaysType breakdown
PRKD1660Binding:650, Functional:10
EPHA1284Binding:284
STK38153Binding:153
KDM5B146Binding:146
TPSD135Binding:35
TSHR33Functional:24, Binding:9
PKD127Binding:27
WIZ15Binding:10, Functional:5
SOX1811Binding:11
MMP268Binding:8
FZD58Functional:6, Binding:2

Cohort enzymes (BRENDA EC)

SymbolEC numbersNames
MMP263.4.24.B7
STK382.7.11.1non-specific serine/threonine protein kinase
KDM5B1.14.11.67[histone H3]-trimethyl-L-lysine4 demethylase
CYP4F221.14.14.177ultra-long-chain fatty acid omega-hydroxylase
EPHA12.7.10.1receptor protein-tyrosine kinase
PRKD12.7.11.13protein kinase C

Cohort genes with high screening signal

≥100 ChEMBL assays — a studied-ness signal; see Therapeutics for approved-drug status.

SymbolChEMBL assays
STK38153
KDM5B146
EPHA1284
PRKD1660

Pharmacogenomics

Cohort genes with a PharmGKB record: 29; with CPIC/DPWG dosing guidelines: 0.

No cohort gene has a CPIC/DPWG genotype-guided dosing guideline (PharmGKB).

Chemical tractability of cohort targets

30 approved/phased compounds have measured bioactivity against a cohort gene (and aren’t yet in disease-level trials). This is a research / tractability signal, NOT a therapeutic recommendation — a bioactivity row often reflects off-target or screening binding (e.g. promiscuous kinase inhibitors against a cohort kinase), implying no disease mechanism.

CompoundMax phaseCohort target (bioactivity)
LEVOSALBUTAMOL4TSHR
PROGESTERONE4TSHR
DICLOFENAC SODIUM4TSHR
CLOTRIMAZOLE4TSHR
DAPSONE4TSHR
COLCHICINE4TSHR
OXAPROZIN4TSHR
BUMETANIDE4TSHR
GLIPIZIDE4TSHR
CARBAMAZEPINE4TSHR
METHYL SALICYLATE4TSHR
PHENELZINE4TSHR
EDROPHONIUM4TSHR
SULFAPHENAZOLE4TSHR
AMOXAPINE4TSHR
PYRIDOSTIGMINE4TSHR
ACETAMINOPHEN4TSHR
DICYCLOMINE4TSHR
IODIPAMIDE4TSHR
TESTOSTERONE PROPIONATE4TSHR
TETRABENAZINE4TSHR
CELECOXIB4TSHR
PROPANTHELINE4TSHR
BENOXINATE4TSHR
NICARDIPINE HYDROCHLORIDE4TSHR
PYRITHIONE ZINC4TSHR
GUANABENZ ACETATE4TSHR
PROPIOLACTONE4TSHR
CHLOROTRIANISENE4TSHR
PHENOXYBENZAMINE HYDROCHLORIDE4TSHR

Druggability pyramid

Cohort genes binned by druggability tier (high → low):

TierDefinitionGenesSymbols
AApproved (phase 4 drug)4TSHR, STK38, EPHA1, PRKD1
BPhased (≥1) drug, not yet approved2MMP26, KDM5B
CDruggable family + PDB, no drug3CELSR1, FZD5, PKD1
DDruggable family + AlphaFold only, no drug3TPSD1, CYP4F22, CELSR3
EDifficult family or no structure, no drug17SOX18, SPINT3, WNT11, WNT6, WNT10A, RAB23, LRP10, TP63, BMP10, ANTXR1 (+7 more)

Undrugged target profiles

23 cohort genes are undrugged. Ranked by ‘starting-point quality’ (assay depth + drugged-partner adjacency).

SymbolChEMBL assaysDrugged partners (top 3)
PKD127PRKD1
SOX1811
SPINT30
WNT110
WNT60
WNT10A0
TPSD135
RAB230
LRP100
TP630
CELSR10
BMP100
ANTXR10
CYP4F220
PRAMEF20
WIZ15
TCHHL10
CELSR30
LRRC37A20
FZD58
CCDC1790
ISL10
LMO70

Clinical trials & evidence

Clinical trials

Clinical trials: 0.