Cutaneous mastocytosis

disease
On this page

Also known as CMCMCDcutaneous (skin) mastocytosiscutaneous mastocytosis (disease)mastocytosis, cutaneousmastocytosis, systemic, somatic

Summary

Cutaneous mastocytosis (MONDO:0019023) is a disease caused by KIT (GenCC Strong), with 14 cohort genes (25 GWAS associations across 3 studies) and 5 clinical trials.

At a glance

  • Prevalence: Unknown (Worldwide) [Orphanet-validated]
  • Causal gene: KIT (GenCC Strong)
  • Cohort genes: 14
  • GWAS associations: 25
  • ClinVar variants: 42
  • Clinical trials: 5

Clinical features

No curated clinical features (Orphanet) for this disease.

Identifiers

Disease identifiers

FieldValue
Canonical namecutaneous mastocytosis
Mondo IDMONDO:0019023
EFOEFO:1000886
MeSHD034701
OMIM154800
Orphanet66646
DOIDDOID:3663
ICD-10-CMD47.01
ICD-111300710062
NCITC7137
SNOMED CT397012002
UMLSC1136033
MedGen210143
GARD0007842
Is cancer (heuristic)no

Also known as: CM · CMCD · cutaneous (skin) mastocytosis · cutaneous mastocytosis · cutaneous mastocytosis (disease) · mastocytosis, cutaneous · mastocytosis, systemic, somatic

Data availability: 42 ClinVar variants · 25 GWAS associations (3 studies) · 2 GenCC gene-disease records · 1 HPO phenotype · 1 cell line.

Disease family

An umbrella term covering 3 Mondo subtypes.

Classification path: disease › human disease › disease by etiologic mechanism › cancer or benign tumorneoplastic disease or syndromeneoplasmskin neoplasmdermis tumorcutaneous mastocytosis

Related subtypes (7): cutaneous granular cell tumor, skin glomus tumor, leiomyoma cutis, malignant dermis tumor, cutaneous fibrous histiocytoma, juvenile hyaline fibromatosis, angioma serpiginosum

Subtypes (3): cutaneous mastocytoma, diffuse cutaneous mastocytosis, maculopapular cutaneous mastocytosis

Genetics & variants

GWAS landscape

25 GWAS associations across 3 studies. Top hits map to 21 distinct genes (as reported by GWAS).

Top associations by p-value

rsIDp-valueGeneRisk alleleOdds ratio
rs801388022e-30ABCA2C6.97
rs108380942e-25OR51B5, OR51Q1, HBG2, HBE1A0.16
rs118455377e-22RPL3P3, OTX2-AS1, LINC03059A6.59
rs98287585e-17PRDX5P1 - LINC02005T0.15
rs22793436e-13CYP2B6G0.18
rs76015113e-11TMEM182 - CRLF3P1G0.14
rs760151124e-09RPTNG
rs16112071e-08HLA-F-AS1, HCG4, HLA-V, HLA-VA2.01
rs32186423e-08POLQT3.98
rs80883404e-08MIR3976HGC4.68
rs19099366e-08FABP5 - PMP2C3.89
rs17781558e-08PDE4DIPT1.97
rs412712171e-07DYNC2I1G4.49
rs27280073e-07CNTN6 - RPL23AP38C3.75
rs131954023e-07BTN2A1T2.8
rs95303136e-07LINC00402A3.04
rs9732538e-07EGLN1C1.81

Top studies (by case count)

StudyLead authorYearCasesControlsTitle
GCST011381Nedoszytko B20201415,606Results from a Genome-Wide Association Study (GWAS) in Mastocytosis Reveal New Gene Polymorphisms Associated with WHO Subgroups.
GCST011379Nedoszytko B2020785,606Results from a Genome-Wide Association Study (GWAS) in Mastocytosis Reveal New Gene Polymorphisms Associated with WHO Subgroups.
GCST011380Nedoszytko B2020655,606Results from a Genome-Wide Association Study (GWAS) in Mastocytosis Reveal New Gene Polymorphisms Associated with WHO Subgroups.

Variant details and genetic-evidence tiers

Tier distribution (top 50 variants)

TierVariants
Tier 1: coding6
Tier 2: splice/UTR2
Tier 3: regulatory0
Tier 4: intronic/intergenic9

MAF distribution

BucketVariants
common (>=0.05)9
low_freq (0.01-0.05)8
rare (<0.01)0
unknown0

Functional consequences

ConsequenceCount
missense_variant5
intron_variant5
intergenic_variant2
synonymous_variant1
non_coding_transcript_exon_variant1
splice_polypyrimidine_tract_variant1
splice_donor_5th_base_variant1
stop_gained1

Top variants

rsIDChrPosAllelesMAFConsequenceGenep-valueTier
rs801388029137021488A>C,G0.024synonymous_variantABCA22e-30Tier 4: intronic/intergenic
rs10838094115422663G>A,C0.411missense_variantOR51B5, OR51Q1, HBG2, HBE12e-25Tier 1: coding
rs118455371456979555G>A,C0.015non_coding_transcript_exon_variantRPL3P3, OTX2-AS1, LINC030597e-22Tier 4: intronic/intergenic
rs9828758373668985C>G,T0.293intergenic_variantPRDX5P1 - LINC020055e-17Tier 4: intronic/intergenic
rs22793431941009358A>G,T0.248missense_variantCYP2B66e-13Tier 1: coding
rs76015112103382339C>G0.214intron_variantTMEM182 - CRLF3P13e-11Tier 4: intronic/intergenic
rs760151121152156618A>G,T0.214missense_variantRPTN4e-09Tier 1: coding
rs1611207629792099G>A,C,T0.381splice_polypyrimidine_tract_variantHLA-F-AS1, HCG4, HLA-V, HLA-V1e-08Tier 2: splice/UTR
rs32186423121488790G>A,C,T0.028missense_variantPOLQ3e-08Tier 1: coding
rs8088340185836383T>C,G0.017intron_variantMIR3976HG4e-08Tier 4: intronic/intergenic
rs1909936881333216T>C0.029intron_variantFABP5 - PMP26e-08Tier 4: intronic/intergenic
rs17781551149009657A>G0.454missense_variantPDE4DIP8e-08Tier 1: coding
rs412712177158914326A>G0.023splice_donor_5th_base_variantDYNC2I11e-07Tier 2: splice/UTR
rs272800731545467C>G,T0.028intergenic_variantCNTN6 - RPL23AP383e-07Tier 4: intronic/intergenic
rs13195402626463347G>A,C,T0.036stop_gainedBTN2A13e-07Tier 1: coding
rs95303131374424521A>C,G,T0.051intron_variantLINC004026e-07Tier 4: intronic/intergenic
rs9732531231385128C>G,T0.299intron_variantEGLN18e-07Tier 4: intronic/intergenic

ClinVar germline variants

42 retrieved; paginated sample, class counts are floors:

20 uncertain significance, 16 conflicting classifications of pathogenicity, 2 likely benign, 2 pathogenic, 1 pathogenic/likely pathogenic, 1 benign/likely benign

ClinVarVariant (HGVS)GeneClassificationReview
13865NM_000222.3(KIT):c.1676T>C (p.Val559Ala)KITPathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
375930NM_000222.3(KIT):c.2465A>T (p.Asn822Ile)KITPathogenicno assertion criteria provided
545643NM_000222.3(KIT):c.1598C>A (p.Ala533Asp)KITPathogenicno assertion criteria provided
134627NM_000222.3(KIT):c.2866C>T (p.Arg956Trp)KITConflicting classifications of pathogenicitycriteria provided, conflicting classifications
13852NM_000222.3(KIT):c.2447A>T (p.Asp816Val)KITConflicting classifications of pathogenicitycriteria provided, conflicting classifications
1500519NM_000222.3(KIT):c.1231+13A>TKITConflicting classifications of pathogenicitycriteria provided, conflicting classifications
1694457NM_000222.3(KIT):c.590C>T (p.Ser197Leu)KITConflicting classifications of pathogenicitycriteria provided, conflicting classifications
225286NM_000222.3(KIT):c.464C>T (p.Pro155Leu)KITConflicting classifications of pathogenicitycriteria provided, conflicting classifications
237233NM_000222.3(KIT):c.1109A>G (p.Asn370Ser)KITConflicting classifications of pathogenicitycriteria provided, conflicting classifications
409715NM_000222.3(KIT):c.2920G>A (p.Asp974Asn)KITConflicting classifications of pathogenicitycriteria provided, conflicting classifications
409716NM_000222.3(KIT):c.2848G>A (p.Val950Met)KITConflicting classifications of pathogenicitycriteria provided, conflicting classifications
409722NM_000222.3(KIT):c.148G>T (p.Val50Leu)KITConflicting classifications of pathogenicitycriteria provided, conflicting classifications
409758NM_000222.3(KIT):c.2663G>A (p.Arg888Gln)KITConflicting classifications of pathogenicitycriteria provided, conflicting classifications
458965NM_000222.3(KIT):c.749A>G (p.Asn250Ser)KITConflicting classifications of pathogenicitycriteria provided, conflicting classifications
576610NM_000222.3(KIT):c.2836C>T (p.Arg946Ter)KITConflicting classifications of pathogenicitycriteria provided, conflicting classifications
857642NM_000222.3(KIT):c.2564A>G (p.Tyr855Cys)KITConflicting classifications of pathogenicitycriteria provided, conflicting classifications
858552NM_000222.3(KIT):c.867G>A (p.Met289Ile)KITConflicting classifications of pathogenicitycriteria provided, conflicting classifications
947788NM_000222.3(KIT):c.2138C>T (p.Ser713Phe)KITConflicting classifications of pathogenicitycriteria provided, conflicting classifications
953437NM_000222.3(KIT):c.555T>G (p.His185Gln)KITConflicting classifications of pathogenicitycriteria provided, conflicting classifications
1016059NM_000222.3(KIT):c.1952T>A (p.Met651Lys)KITUncertain significancecriteria provided, multiple submitters, no conflicts
1760097NM_000222.3(KIT):c.767A>G (p.Gln256Arg)KITUncertain significancecriteria provided, multiple submitters, no conflicts
2568309NM_000222.3(KIT):c.1924A>C (p.Lys642Gln)KITUncertain significancecriteria provided, multiple submitters, no conflicts
3382507NM_000222.3(KIT):c.2449A>T (p.Ile817Phe)KITUncertain significancecriteria provided, single submitter
3590592NM_000222.3(KIT):c.458G>C (p.Gly153Ala)KITUncertain significancecriteria provided, single submitter
3590593NM_000222.3(KIT):c.689C>T (p.Thr230Ile)KITUncertain significancecriteria provided, multiple submitters, no conflicts
3590594NM_000222.3(KIT):c.1879C>G (p.Pro627Ala)KITUncertain significancecriteria provided, multiple submitters, no conflicts
3590596NM_000222.3(KIT):c.2781G>T (p.Gln927His)KITUncertain significancecriteria provided, multiple submitters, no conflicts
409732NM_000222.3(KIT):c.1900C>T (p.Arg634Trp)KITUncertain significancecriteria provided, multiple submitters, no conflicts
409795NM_000222.3(KIT):c.793G>A (p.Gly265Ser)KITUncertain significancecriteria provided, multiple submitters, no conflicts
458867NM_000222.3(KIT):c.1344G>C (p.Gln448His)KITUncertain significancecriteria provided, multiple submitters, no conflicts

Genes & proteins

Mendelian disease overlap and somatic drivers

GenCC: 15 · Orphanet: 23 · OMIM-shared: 0 · Dual-evidence (GWAS+Mendelian): 0

GenCC gene–disease validity (cohort genes)

the Disease column is the GenCC-asserted condition — a cohort gene’s strongest validity may be for a related predisposition syndrome.

GeneClassificationInheritanceDiseaseRecords
KITStrongAutosomal dominantmastocytosis15

Orphanet rare-disease linkage (cohort genes)

GeneOrphanet IDRare disease
KITOrphanet:102724Acute myeloid leukemia with t(8;21)(q22;q22) translocation
KITOrphanet:158766Typical urticaria pigmentosa
KITOrphanet:158769Plaque-form urticaria pigmentosa
KITOrphanet:158772Nodular urticaria pigmentosa
KITOrphanet:158775Smoldering systemic mastocytosis
KITOrphanet:158778Isolated bone marrow mastocytosis
KITOrphanet:280785Bullous diffuse cutaneous mastocytosis
KITOrphanet:280794Pseudoxanthomatous diffuse cutaneous mastocytosis
KITOrphanet:2884Piebaldism
KITOrphanet:44890Gastrointestinal stromal tumor
KITOrphanet:566393Acute mast cell leukemia
KITOrphanet:566396Chronic mast cell leukemia
KITOrphanet:79455Cutaneous mastocytoma
KITOrphanet:842Testicular seminomatous germ cell tumor
KITOrphanet:90389Telangiectasia macularis eruptiva perstans
KITOrphanet:98829Acute myeloid leukemia with abnormal bone marrow eosinophils inv(16)(p13q22) or t(16;16)(p13;q22)
KITOrphanet:98834Acute myeloblastic leukemia with maturation
KITOrphanet:98849Systemic mastocytosis with associated hematologic neoplasm
EGLN1Orphanet:247511Autosomal dominant secondary polycythemia
PRPF31Orphanet:791Retinitis pigmentosa
DYNC2I1Orphanet:474Jeune syndrome
DYNC2I1Orphanet:93271Short rib-polydactyly syndrome, Verma-Naumoff type
ABCA2Orphanet:88616Autosomal recessive non-syndromic intellectual disability

Cohort genes → proteins

14 cohort genes, 11 distinct canonical proteins.

Evidence partition

SubsetGenes
gwas_only13
multi_evidence1

Cohort genes (full)

SymbolHGNCEnsemblUniProtNameEvidence
KITHGNC:6342ENSG00000157404P10721Mast/stem cell growth factor receptor Kitgencc,clinvar
BTN2A1HGNC:1136ENSG00000112763Q7KYR7Butyrophilin subfamily 2 member A1gwas
EGLN1HGNC:1232ENSG00000135766Q9GZT9Egl nine homolog 1gwas
OR51Q1HGNC:14851ENSG00000167360Q8NH59Olfactory receptor 51Q1gwas
PRPF31HGNC:15446ENSG00000105618Q8WWY3U4/U6 small nuclear ribonucleoprotein Prp31gwas
PDE4DIPHGNC:15580ENSG00000178104Q5VU43Myomegalingwas
DYNC2I1HGNC:21862ENSG00000126870Q8WVS4Cytoplasmic dynein 2 intermediate chain 1gwas
HLA-VHGNC:23482ENSG00000181126major histocompatibility complex, class I, V (pseudogene)gwas
CYP2B6HGNC:2615ENSG00000197408P20813Cytochrome P450 2B6gwas
RPTNHGNC:26809ENSG00000215853Q6XPR3Repetingwas
ABCA2HGNC:32ENSG00000107331Q9BZC7ATP-binding cassette sub-family A member 2gwas
LINC00402HGNC:42732ENSG00000235532long intergenic non-protein coding RNA 402gwas
OTX2-AS1HGNC:43906ENSG00000248550OTX2 antisense RNA 1gwas
POLQHGNC:9186ENSG00000051341O75417DNA polymerase thetagwas

Cohort function summary

Lead sentence per gene, UniProt-curated.

SymbolProtein nameFunction (lead sentence)
KITMast/stem cell growth factor receptor KitTyrosine-protein kinase that acts as a cell-surface receptor for the cytokine KITLG/SCF and plays an essential role in the regulation of cell survival and proliferation, hematopoiesis, stem cell maintenance, gametogenesis, mast cell develo…
EGLN1Egl nine homolog 1Cellular oxygen sensor that catalyzes, under normoxic conditions, the post-translational formation of 4-hydroxyproline in hypoxia-inducible factor (HIF) alpha proteins.
OR51Q1Olfactory receptor 51Q1Odorant receptor.
PRPF31U4/U6 small nuclear ribonucleoprotein Prp31Involved in pre-mRNA splicing as component of the spliceosome.
PDE4DIPMyomegalinFunctions as an anchor sequestering components of the cAMP-dependent pathway to Golgi and/or centrosomes.
DYNC2I1Cytoplasmic dynein 2 intermediate chain 1Acts as one of several non-catalytic accessory components of the cytoplasmic dynein 2 complex (dynein-2 complex), a motor protein complex that drives the movement of cargos along microtubules within cilia and flagella in concert with the i…
CYP2B6Cytochrome P450 2B6A cytochrome P450 monooxygenase involved in the metabolism of endocannabinoids and steroids.
RPTNRepetinInvolved in the cornified cell envelope formation.
ABCA2ATP-binding cassette sub-family A member 2Probable lipid transporter that modulates cholesterol sequestration in the late endosome/lysosome by regulating the intracellular sphingolipid metabolism, in turn participates in cholesterol homeostasis.
POLQDNA polymerase thetaLow-fidelity DNA polymerase with a helicase activity that promotes microhomology-mediated end-joining (MMEJ), an alternative non-homologous end-joining (NHEJ) machinery required to repair double-strand breaks in DNA during mitosis.

Protein-family classification

Druggable: 5 · Difficult: 2 · Unknown: 7 · Druggable fraction: 0.36

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
Transporter15.6×0.836
Antibody/Immunoglobulin12.1×0.836
Kinase12.0×0.836
GPCR11.7×0.836
Scaffold/PPI11.2×0.836
Other/Unknown70.9×0.836
Enzyme (other)10.9×0.836
Transcription factor10.6×0.836

Per-gene assignment

SymbolFamilyDruggable?ECInterPro (top 3)
KITKinaseyes2.7.10.1Prot_kinase_dom, Ser-Thr/Tyr_kinase_cat_dom, Tyr_kinase_rcpt_3_CS
BTN2A1Antibody/ImmunoglobulinyesB30.2/SPRY, Ig_sub, SPRY_dom
EGLN1Transcription factorno1.14.11.2Znf_MYND, Oxoglu/Fe-dep_dioxygenase_dom, Pro_4_hyd_alph
OR51Q1GPCRyesGPCR_Rhodpsn, Olfact_rcpt, GPCR_Rhodpsn_7TM
PRPF31Other/UnknownnoNop_dom, NOSIC, Prp31_C
PDE4DIPOther/UnknownnoOlduvai_dom, Cnn_1N, MT-associated_AKAP9-binding
DYNC2I1Scaffold/PPInoWD40_rpt, WD40/YVTN_repeat-like_dom_sf, WD40_repeat_dom_sf
HLA-VOther/Unknownno
CYP2B6Enzyme (other)yes1.14.14.1Cyt_P450, Cyt_P450_E_grp-I, Cyt_P450_E_grp-I_CYP2B-like
RPTNOther/UnknownnoS100/CaBP7/8-like_CS, EF_hand_dom, EF-hand-dom_pair
ABCA2TransporteryesABC_transporter-like_ATP-bd, AAA+_ATPase, ABC2_TM
LINC00402Other/Unknownno
OTX2-AS1Other/Unknownno
POLQOther/UnknownnoDNA-dir_DNA_pol_A_palm_dom, Helicase_C-like, DNA_polymerase_A

Expression context

Cohort genes with no expression data: 0.

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

Breadth distribution (Bgee present_calls)

BucketGenes
narrow (1-5 tissues)1
moderate (6-20)0
broad (>20)13
unknown0

Top tissues across cohort

TissueCohort genes
male germ line stem cell (sensu Vertebrata) in testis4
oocyte2
secondary oocyte2
granulocyte2
gastrocnemius2
sural nerve2
apex of heart2
buccal mucosa cell2
lateral nuclear group of thalamus1
cerebellar hemisphere1
spleen1
adrenal tissue1
muscle of leg1
calcaneal tendon1
colonic epithelium1
stromal cell of endometrium1
ventricular zone1
hindlimb stylopod muscle1
right uterine tube1
sperm1

Per-gene tissue summary (top 30)

SymbolBgee breadthFANTOM5 breadthSCXATop tissues
KIT263broadmarkerlateral nuclear group of thalamus, secondary oocyte, oocyte
BTN2A1286ubiquitousmarkergranulocyte, spleen, cerebellar hemisphere
EGLN1214ubiquitousmarkergastrocnemius, muscle of leg, adrenal tissue
OR51Q12yessural nerve, colonic epithelium, calcaneal tendon
PRPF31134ubiquitousmarkerstromal cell of endometrium, granulocyte, ventricular zone
PDE4DIP292ubiquitousmarkerapex of heart, hindlimb stylopod muscle, gastrocnemius
DYNC2I1269ubiquitousmarkersural nerve, right uterine tube, sperm
HLA-V128tissue_specificyesapex of heart, male germ line stem cell (sensu Vertebrata) in testis, upper lobe of left lung
CYP2B6106tissue_specificmarkerright lobe of liver, liver, buccal mucosa cell
RPTN57tissue_specificmarkergingiva, gingival epithelium, tongue
ABCA2234ubiquitousmarkerC1 segment of cervical spinal cord, spinal cord, right hemisphere of cerebellum
LINC0040274tissue_specificmarkermale germ line stem cell (sensu Vertebrata) in testis, testis, lymph node
OTX2-AS1104broadmarkerbuccal mucosa cell, pigmented layer of retina, male germ line stem cell (sensu Vertebrata) in testis
POLQ166ubiquitousmarkersecondary oocyte, oocyte, male germ line stem cell (sensu Vertebrata) in testis

Protein interactions among cohort

Intra-cohort edges: 4.

Hub genes (top 10 by interactor count)

SymbolInteractor count
KIT6,087
PRPF313,427
PDE4DIP2,146
EGLN12,107
CYP2B61,954
POLQ1,785
ABCA21,678
RPTN1,413
DYNC2I1955
OR51Q1160

Intra-cohort edges

ABSources
ABCA2OR51Q1string_interaction
OR51Q1PDE4DIPstring_interaction
OR51Q1RPTNstring_interaction
PDE4DIPPRPF31biogrid_interaction, intact

Structural data

PDB: 7 · AlphaFold-only: 4 · No structure: 3

Cohort genes with PDB structures (top 30)

SymbolUniProtPDB entries
EGLN1Q9GZT964
KITP1072152
BTN2A1Q7KYR733
POLQO7541733
PRPF31Q8WWY330
CYP2B6P2081313
DYNC2I1Q8WVS44

AlphaFold-only cohort genes (top 30 by pLDDT)

SymbolUniProtpLDDT
OR51Q1Q8NH5985.83
ABCA2Q9BZC771.46
PDE4DIPQ5VU4358.74
RPTNQ6XPR342.63

Function

Pathway analysis

Distinct Reactome pathways touched by cohort: 56. Enrichment computed across 14 evidence-associated genes (10 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 10 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

PathwayCohort genesFoldFDRSample cohort genes
Dasatinib-resistant KIT mutants11142.0×0.004KIT
Imatinib-resistant KIT mutants11142.0×0.004KIT
KIT mutants bind TKIs11142.0×0.004KIT
Masitinib-resistant KIT mutants11142.0×0.004KIT
Nilotinib-resistant KIT mutants11142.0×0.004KIT
Regorafenib-resistant KIT mutants11142.0×0.004KIT
Signaling by kinase domain mutants of KIT11142.0×0.004KIT
Sunitinib-resistant KIT mutants11142.0×0.004KIT
Signaling by juxtamembrane domain KIT mutants11142.0×0.004KIT
Sorafenib-resistant KIT mutants11142.0×0.004KIT
Drug resistance of KIT mutants11142.0×0.004KIT
Signaling by extracellular domain mutants of KIT11142.0×0.004KIT
Signaling by KIT in disease1114.2×0.038KIT
CYP2E1 reactions195.2×0.040CYP2B6
HDR through MMEJ (alt-NHEJ)187.8×0.040POLQ
Butyrophilin (BTN) family interactions187.8×0.040BTN2A1
TFAP2 (AP-2) family regulates transcription of growth factors and their receptors176.1×0.042KIT
Fatty acids171.4×0.042CYP2B6
Transcriptional regulation by the AP-2 (TFAP2) family of transcription factors163.4×0.042KIT
Developmental Lineage of Mammary Gland Alveolar Cells163.4×0.042KIT
ABC transporters in lipid homeostasis160.1×0.042ABCA2
Regulation of KIT signaling160.1×0.042KIT
Signaling by phosphorylated juxtamembrane, extracellular and kinase domain KIT mutants151.9×0.047KIT
Xenobiotics149.6×0.047CYP2B6
Developmental Lineage of Mammary Gland Luminal Epithelial Cells145.7×0.049KIT
PI3K/AKT Signaling in Cancer136.8×0.058KIT
Negative regulation of the PI3K/AKT network127.9×0.073KIT
Signaling by SCF-KIT124.8×0.079KIT
Phase I - Functionalization of compounds122.0×0.086CYP2B6
Intraflagellar transport120.0×0.090DYNC2I1

GO biological processes by enrichment

Over-representation of cohort genes vs the genome-wide background (hypergeometric test, Benjamini-Hochberg FDR; fold = observed/expected over 10 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

GO termCohort genesFoldFDRSample cohort genes
glycosphingolipid metabolic process2481.5×1e-03KIT, ABCA2
negative regulation of intracellular cholesterol transport11685.2×0.010ABCA2
negative regulation of phospholipid biosynthetic process11685.2×0.010ABCA2
ribonucleoprotein complex localization11685.2×0.010PRPF31
negative regulation of sphingolipid biosynthetic process11685.2×0.010ABCA2
melanocyte adhesion11685.2×0.010KIT
positive regulation of pyloric antrum smooth muscle contraction11685.2×0.010KIT
positive regulation of colon smooth muscle contraction11685.2×0.010KIT
regulation of protein localization to cell periphery11685.2×0.010ABCA2
negative regulation of steroid metabolic process1842.6×0.011ABCA2
ceramide translocation1842.6×0.011ABCA2
regulation of post-translational protein modification1842.6×0.011ABCA2
negative regulation of hypoxia-inducible factor-1alpha signaling pathway1842.6×0.011EGLN1
positive regulation of vascular associated smooth muscle cell differentiation1842.6×0.011KIT
negative regulation of receptor-mediated endocytosis involved in cholesterol transport1842.6×0.011ABCA2
positive regulation of low-density lipoprotein particle receptor catabolic process1561.7×0.011ABCA2
Fc receptor signaling pathway1561.7×0.011KIT
Kit signaling pathway1561.7×0.011KIT
ketone metabolic process1561.7×0.011CYP2B6
melanocyte migration1561.7×0.011KIT
regulation protein catabolic process at postsynapse1561.7×0.011EGLN1
obsolete regulation of bile acid metabolic process1561.7×0.011KIT
positive regulation of small intestine smooth muscle contraction1561.7×0.011KIT
ganglioside metabolic process1421.3×0.012ABCA2
mast cell chemotaxis1421.3×0.012KIT
regulation of intracellular cholesterol transport1421.3×0.012ABCA2
hematopoietic stem cell migration1421.3×0.012KIT
mast cell differentiation1421.3×0.012KIT
positive regulation of dendritic cell cytokine production1337.0×0.012KIT
sphingomyelin metabolic process1337.0×0.012ABCA2

Therapeutics

Drug target analysis

Approved (phase 4): 4 · Phase ≥3: 4 · Phased (≥1): 5 · Undrugged: 9

Druggability breadth: 6 of 14 evidence-associated genes (43%) 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
KITPONATINIB
EGLN1ROXADUSTAT
CYP2B6PAZOPANIB
POLQNOVOBIOCIN

Top cohort targets by molecule count

SymbolMoleculesMax phase
KIT994
CYP2B6284
EGLN1114
PRPF3112
POLQ14
BTN2A100
OR51Q100
PDE4DIP00
DYNC2I100
HLA-V00

Drugs targeting cohort genes (top 30)

MoleculeMax phaseTargets in cohort
PONATINIB4KIT
FEDRATINIB4KIT
TIVOZANIB4KIT
LENVATINIB4KIT
AXITINIB4KIT
SORAFENIB4KIT
DASATINIB ANHYDROUS4KIT
NICLOSAMIDE4KIT
IMATINIB MESYLATE4KIT
RUXOLITINIB4KIT
INFIGRATINIB PHOSPHATE4KIT
INFIGRATINIB4KIT
REGORAFENIB4KIT
ENTRECTINIB4KIT
CABOZANTINIB4KIT
CERITINIB4KIT
VANDETANIB4KIT
NILOTINIB4KIT
BOSUTINIB4KIT
BRIGATINIB4KIT
PEXIDARTINIB4KIT
AVAPRITINIB4KIT
RIPRETINIB4KIT
PAZOPANIB4CYP2B6, KIT
NINTEDANIB4KIT
SUNITINIB4KIT
DASATINIB4KIT
ERLOTINIB4KIT
QUIZARTINIB4KIT
CRIZOTINIB4KIT

Bioactivity and enzyme data

Enzyme cohort genes (≥1 EC): 3.

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

SymbolAssaysType breakdown
KIT2,305Binding:2242, ADMET:32, Functional:22, Toxicity:9
CYP2B6861ADMET:851, Binding:10
EGLN1211Binding:211
POLQ46Binding:46
PRPF316Binding:6
BTN2A11Binding:1

Cohort enzymes (BRENDA EC)

SymbolEC numbersNames
KIT2.7.10.1receptor protein-tyrosine kinase
EGLN11.14.11.2, 1.14.11.29procollagen-proline 4-dioxygenase, hypoxia-inducible factor-proline dioxygenase
CYP2B61.14.14.1unspecific monooxygenase

Cohort genes with high screening signal

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

SymbolChEMBL assays
KIT2,305
EGLN1211
CYP2B6861

Pharmacogenomics

Cohort genes with a PharmGKB record: 12; with CPIC/DPWG dosing guidelines: 1.

Cohort genes with a CPIC/DPWG dosing guideline

SymbolCPIC guidelines
CYP2B61

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)
PONATINIB4KIT
FEDRATINIB4KIT
TIVOZANIB4KIT
LENVATINIB4KIT
AXITINIB4KIT
SORAFENIB4KIT
DASATINIB ANHYDROUS4KIT
NICLOSAMIDE4KIT
IMATINIB MESYLATE4KIT
RUXOLITINIB4KIT
INFIGRATINIB PHOSPHATE4KIT
INFIGRATINIB4KIT
REGORAFENIB4KIT
ENTRECTINIB4KIT
CABOZANTINIB4KIT
CERITINIB4KIT
VANDETANIB4KIT
NILOTINIB4KIT
BOSUTINIB4KIT
BRIGATINIB4KIT
PEXIDARTINIB4KIT
AVAPRITINIB4KIT
RIPRETINIB4KIT
PAZOPANIB4CYP2B6, KIT
NINTEDANIB4KIT
SUNITINIB4KIT
DASATINIB4KIT
ERLOTINIB4KIT
QUIZARTINIB4KIT
CRIZOTINIB4KIT

Druggability pyramid

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

TierDefinitionGenesSymbols
AApproved (phase 4 drug)4KIT, EGLN1, CYP2B6, POLQ
BPhased (≥1) drug, not yet approved1PRPF31
CDruggable family + PDB, no drug1BTN2A1
DDruggable family + AlphaFold only, no drug2OR51Q1, ABCA2
EDifficult family or no structure, no drug6PDE4DIP, DYNC2I1, HLA-V, RPTN, LINC00402, OTX2-AS1

Undrugged target profiles

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

SymbolChEMBL assaysDrugged partners (top 3)
BTN2A11
OR51Q10
PDE4DIP0
DYNC2I10
HLA-V0
RPTN0
ABCA20
LINC004020
OTX2-AS10

Clinical trials & evidence

Clinical trials

Clinical trials: 5.

Phase distribution (across all retrieved trials)

PhaseTrials
Not specified4
PHASE21

Top trials by phase / activity

NCTPhaseStatusTitle
NCT00457288PHASE2COMPLETEDEfficacy and Safety of TF002 in Cutaneous Mastocytosis
NCT07142473Not specifiedRECRUITINGMastocytosis From Pediatric Age to Adulthood: Local Registry of Cutaneous and Systemic Mastocytosis
NCT02761473Not specifiedCOMPLETEDCutaneous Mastocytosis in Children: Analysis of Somatic and Germline Mutations
NCT03632811Not specifiedCOMPLETEDAdaptation of the Questionnaire Regarding Patient’s Quality of Life With Mastocytosis in the French Language
NCT04377828Not specifiedUNKNOWNImprovement of Pigmented Skin Lesions in Patients With Mastocytosis After Performing 2 Sessions of Pigment Laser