CFTR Gene Complete Identifier and Functional Mapping Reference

Provide a comprehensive cross-database identifier and functional mapping reference for human CFTR — a definitive lookup resource covering: ### …

Provide a comprehensive cross-database identifier and functional mapping reference for human CFTR — a definitive lookup resource covering: ### Section 1: Gene identifiers For human gene CFTR, list ALL gene-level database identifiers. Required: - HGNC ID and approved symbol - Ensembl gene ID (ENSG...) - NCBI Entrez Gene ID - OMIM gene/locus ID - Genomic location: chromosome, start position, end position, strand (GRCh38) ### Section 2: Transcript identifiers For human gene CFTR, list ALL transcript-level identifiers. Required: - Ensembl transcripts: ALL ENST IDs with biotype. Total count. - RefSeq transcripts: ALL NM_ mRNA accessions. Mark which is MANE Select. - CCDS IDs. - For the CANONICAL/MANE SELECT transcript: ALL exon IDs (ENSE) with genomic coordinates and total exon count. ### Section 3: Protein identifiers For human gene CFTR protein product(s), list ALL protein-level identifiers. Required: - UniProt accessions: ALL entries (reviewed and unreviewed). Mark the canonical reviewed entry. - RefSeq protein: ALL NP_ accessions. - Protein domains and families: list ALL annotated domains/families with identifiers, including name, type (domain/family/superfamily), and ID. - Antibody availability: known antibody resources for the protein. ### Section 4: Structure For human gene CFTR protein, list ALL structural data. Required: - Experimental structures: ALL PDB IDs. For each: experimental method (X-ray/NMR/Cryo-EM) and resolution. Total count. - Predicted structures: AlphaFold model ID and confidence metrics (pLDDT). ### Section 5: Cross-species orthologs For human gene CFTR, list orthologous genes in key model organisms. Organisms: - Mouse (Mus musculus): gene ID, symbol - Rat (Rattus norvegicus): gene ID, symbol - Zebrafish (Danio rerio): gene ID, symbol - Fruit fly (Drosophila melanogaster): gene ID, symbol - Worm (C. elegans): gene ID, symbol - Yeast (S. cerevisiae): gene ID, symbol ### Section 6: Clinical variants & AI predictions For human gene CFTR, summarize clinical variants and AI predictions. Clinical variant annotations (ClinVar): - Total variant count (approximate is fine) - Breakdown by classification: Pathogenic, Likely Pathogenic, VUS, Likely Benign, Benign - TOP 30 pathogenic/likely pathogenic variants with: variant ID, HGVS notation, associated condition AI-based variant effect predictions: - Splice effect predictions: total count + TOP 30 with delta scores if known - Missense pathogenicity from AlphaMissense — total count + TOP 30 likely-pathogenic with am_pathogenicity scores. ### Section 7: Pathways & Gene Ontology For human gene CFTR, list biological pathways and Gene Ontology annotations. Pathway membership: - ALL biological pathways this gene participates in, with pathway IDs and names - Total pathway count Gene Ontology: - Biological Process: count and TOP 20 terms with GO IDs - Molecular Function: count and TOP 20 terms with GO IDs - Cellular Component: count and TOP 20 terms with GO IDs ### Section 8: Protein interactions & networks For human gene CFTR protein, summarize protein interactions and networks. Protein-protein interactions (STRING, IntAct, BioGRID, etc.): - Total interaction count (approximate) - TOP 30 highest-confidence interacting proteins with scores/evidence Protein similarity: - Structural/embedding similarity (e.g. Foldseek, ESM): TOP 20 similar proteins with scores - Sequence homology: TOP 20 homologous proteins with identity/similarity ### Section 9: Transcription factor regulatory data For human gene CFTR, summarize transcription factor regulatory data. If CFTR is a transcription factor: - Downstream targets: total count + TOP 30 with regulation type (activates/represses) and evidence - DNA binding motifs from JASPAR — all known motif IDs and motif family classification. Regardless: - Upstream regulators: TFs that regulate CFTR — names with evidence type (ChIP-seq / predicted / experimentally validated) If CFTR is not a transcription factor, say so briefly and skip the downstream/motif sections. ### Section 10: Drug & pharmacology data For human gene CFTR protein as a drug target, summarize pharmacology data. If CFTR is a known drug target: - Targeting molecules: total count in ChEMBL/DrugBank + TOP 30 by development phase (molecule ID, name, mechanism, highest phase) - Clinical trials: TOP 20 involving drugs targeting this gene — trial ID, phase, status, intervention - Pharmacogenomics: known drug-gene interactions affecting drug response + dosing guidelines if any If CFTR is not currently a drug target, say so briefly. ### Section 11: Expression profiles For human gene CFTR, summarize expression profiles. Tissue expression (GTEx, HPA, Bgee, etc.): - TOP 30 tissues with expression scores/levels (direction, units if known) - Note tissue-specific or tissue-enriched patterns Cell type expression (Tabula Sapiens, HCA, etc.): - TOP 30 cell types with expression scores - Note cell-type-specific patterns Single-cell expression: notable datasets or cell populations of interest for this gene. ### Section 12: Disease associations For human gene CFTR, summarize disease associations. Mendelian / monogenic disease: - Diseases caused by mutations in CFTR: disease name, disease ID (OMIM/Orphanet/Mondo), inheritance pattern, evidence level - Include all directly linked conditions Phenotype associations: - Clinical phenotypes associated with the gene (HPO terms where known) - TOP 30 phenotype terms with HPO IDs Complex-disease / GWAS: - Traits and diseases significantly associated via GWAS: trait name, variant, effect size, study where known - TOP 30 GWAS associations

CFTR

Executive summary

CFTR (cystic fibrosis transmembrane conductance regulator, chromosome 7) encodes an ATP-gated chloride channel and ABC-family transporter that is the sole causal gene for cystic fibrosis, an autosomal recessive disease affecting lung, pancreas, intestine, and reproductive tissues. Its clinical importance is underscored by ~5,919 ClinVar variants, of which over 200 are classified pathogenic, and by expression data showing highest activity in pancreas (Bgee score 99.02), gallbladder, and colonic epithelium, consistent with its role in epithelial fluid and electrolyte transport. The protein has 58 experimental PDB structures and interacts with key chaperones (HSP90A/B, HSPA family) and PDZ scaffold proteins (NHERF1, GOPC) that govern its folding, trafficking, and membrane localization. CFTR is one of the most therapeutically tractable rare-disease targets: four combination regimens have received FDA approval — Orkambi (2015), Symkevi (2018), Trikafta (2019), and Alyftrek (2024) — with ivacaftor alone spanning 72 clinical trials, and mutation-specific pharmacogenomics guiding treatment selection for gating (G551D → ivacaftor) and processing defects (F508del → corrector/potentiator combinations).

CFTR — Reference

Cross-database identifier and functional mapping reference for CFTR.

Gene identifiers

CFTR (CF transmembrane conductance regulator)

  • HGNC ID: HGNC:1884
  • Approved symbol: CFTR
  • Ensembl gene ID: ENSG00000001626
  • NCBI Entrez Gene ID: 1080
  • OMIM locus ID: 602421
  • Genomic location (GRCh38):
    • Chromosome: 7
    • Start position: 117,287,120
    • End position: 117,715,971
    • Strand: +

Transcript identifiers

Ensembl Transcripts

ENST IDBiotypeCount
ENST00000003084protein_coding1
ENST00000426809protein_coding1
ENST00000429014protein_coding_CDS_not_defined1
ENST00000436097protein_coding_CDS_not_defined1
ENST00000446805protein_coding1
ENST00000468795protein_coding1
ENST00000472848protein_coding_CDS_not_defined1
ENST00000546407protein_coding_CDS_not_defined1
ENST00000600166protein_coding1
ENST00000608965protein_coding_CDS_not_defined1
ENST00000610149protein_coding_CDS_not_defined1
ENST00000621535retained_intron1
ENST00000647639protein_coding_CDS_not_defined1
ENST00000647720nonsense_mediated_decay1
ENST00000647978nonsense_mediated_decay1
ENST00000648260protein_coding1
ENST00000649406protein_coding1
ENST00000649781protein_coding1
ENST00000649850nonsense_mediated_decay1
ENST00000673785protein_coding1
ENST00000685018nonsense_mediated_decay1
ENST00000687278nonsense_mediated_decay1
ENST00000689011protein_coding1
ENST00000692802protein_coding_CDS_not_defined1
ENST00000693465protein_coding_CDS_not_defined1
ENST00000693480protein_coding_CDS_not_defined1
ENST00000699585nonsense_mediated_decay1
ENST00000699596protein_coding1
ENST00000699597protein_coding1
ENST00000699598nonsense_mediated_decay1
ENST00000699599nonsense_mediated_decay1
ENST00000699600nonsense_mediated_decay1
ENST00000699601nonsense_mediated_decay1
ENST00000699602protein_coding1
ENST00000699603protein_coding_CDS_not_defined1
ENST00000699604nonsense_mediated_decay1
ENST00000699605protein_coding1
ENST00000699606retained_intron1
ENST00000889206protein_coding1
ENST00000889207protein_coding1
ENST00000889208protein_coding1
ENST00000889209protein_coding1
ENST00000889210protein_coding1
ENST00000950799protein_coding1

Total Ensembl transcripts: 44

RefSeq mRNA Transcripts

AccessionSymbolStatusMANE Select
NM_000492CFTRREVIEWED
NM_001044883cftrPROVISIONAL
NM_001182844MRP7REVIEWED
NM_001260357CftrREVIEWED
NM_001338032ABCC7REVIEWED
NM_021050CftrREVIEWED
NM_031506CftrPROVISIONAL
NM_112149ABCC7REVIEWED
NM_143012CftrREVIEWED
XM_006236097CftrPREDICTED
XM_039107007CftrPREDICTED
XM_063285513CftrPREDICTED
XM_063285514CftrPREDICTED
XM_063285515CftrPREDICTED
XM_710158MRP7PROVISIONAL

Total RefSeq mRNA transcripts: 15

CCDS IDs

CCDS ID
CCDS5773

Canonical Transcript Exons: ENST00000003084 (MANE SELECT = NM_000492)

Exon #ENSE IDStartEndCoordinatesLength
1ENSE000013438511174800251174801477:117480025-117480147123
2ENSE000039769751175090341175091427:117509034-117509142109
3ENSE000039769871175042531175043637:117504253-117504363111
4ENSE000039769861175486411175488237:117548641-117548823183
5ENSE000039770791175594641175596557:117559464-117559655192
6ENSE000007186111175308991175311147:117530899-117531114216
7ENSE000007186201175342761175343657:117534276-11753436590
8ENSE000007186261175352481175354117:117535248-117535411164
9ENSE000007186301175365481175366737:117536548-117536673126
10ENSE000007186341175401001175403467:117540100-117540346247
11ENSE000007186371175420161175421087:117542016-11754210893
12ENSE000039770411175903531175904397:117590353-11759043987
13ENSE000039770721175949301175950587:117594930-117595058129
14ENSE000039770441176028261176028637:117602826-11760286338
15ENSE000039770551176035321176037827:117603532-117603782251
16ENSE000039770541176066741176067537:117606674-11760675380
17ENSE000039770561176105191176106697:117610519-117610669151
18ENSE000009774431176115811176118087:117611581-117611808228
19ENSE000007186991176146131176147137:117614613-117614713101
20ENSE000039364981176275221176277707:117627522-117627770249
21ENSE000039252421176424381176425937:117642438-117642593156
22ENSE000038337771176528421176529317:117652842-11765293190
23ENSE000038408131176646881176648607:117664688-117664860173
24ENSE000038359721176654591176655647:117665459-117665564106
25ENSE000009774441176669081176686657:117666908-1176686651758

Total exons in canonical transcript: 27

Protein identifiers

UniProt accessions

Canonical reviewed entry:

  • P13569 (Swiss-Prot) — Cystic fibrosis transmembrane conductance regulator

Unreviewed entries (TrEMBL):

  • A0A3B3IT97
  • A0A3B3ITE0
  • A0A3B3ITW0
  • A0A3B3ITW5
  • A0A669KBE8
  • A0A8I5KVL1
  • A0A8I5KVV2
  • A0A8I5KXQ9
  • A0A8V8TNG7
  • A0A8V8TNH2
  • A0A8V8TNN0
  • A0A8V8TNN7
  • A0A8V8TPV6
  • A0A8V8TQ89
  • A0A8V8TQ94
  • C9J6L5
  • E7EPB6
  • H0Y8A9
  • M0QYZ3

RefSeq protein accessions (NP_)

  • NP_000483 (MANE Select)
  • NP_066388
  • NP_113694
  • NP_001247286
  • NP_001038348
  • NP_651269

Protein domains and families

IDNameType
IPR003439ABC transporter-like, ATP-binding domainDomain
IPR003593AAA+ ATPase domainDomain
IPR009147Cystic fibrosis transmembrane conductance regulator (CFTR/ABCC7)Family
IPR011527ABC transporter type 1, transmembrane domainDomain
IPR017871ABC transporter-like, conserved siteConserved site
IPR025837CFTR regulator domainDomain
IPR027417P-loop containing nucleoside triphosphate hydrolaseHomologous superfamily
IPR036640ABC transporter type 1, transmembrane domain superfamilyHomologous superfamily
IPR047082CFTR, ATP-binding cassette domain 1Domain
IPR050173ATP-binding cassette transporter C-likeFamily

Pfam families:

  • PF00005 (ABC transporter)
  • PF00664 (ABC transporter transmembrane region)
  • PF14396 (CFTR-specific region)

Antibody availability

  • Human Protein Atlas (HPA) — Antibody resources for CFTR protein available through HPA

Structure

Experimental Structures: 58 PDB entries

MethodCountPDB IDs
X-ray Diffraction351XMI (2.25 Å), 1XMJ (2.3 Å), 2BBO (2.55 Å), 2BBS (2.05 Å), 2BBT (2.3 Å), 2PZE (1.7 Å), 2PZF (2.0 Å), 2PZG (1.8 Å), 3GD7 (2.7 Å), 3ISW (2.8 Å), 4WZ6 (2.05 Å), 5D2D (2.1 Å), 5D3E (2.75 Å), 5D3F (2.74 Å), 5TF7 (1.931 Å), 5TF8 (1.861 Å), 5TFA (1.87 Å), 5TFB (1.87 Å), 5TFC (1.92 Å), 5TFD (1.891 Å), 5TFF (1.891 Å), 5TFG (1.91 Å), 5TFI (1.891 Å), 5TFJ (1.85 Å), 5TGK (1.912 Å), 6GJQ (2.49 Å), 6GJS (1.95 Å), 6GJU (2.6 Å), 6GK4 (2.91 Å), 6GKD (2.99 Å), 6HEP (1.86 Å), 6UK1 (2.693 Å), 6WBS (1.857 Å), 6ZE1 (2.705 Å), 7QI1 (1.76 Å)
Cryo-EM225UAK (3.87 Å), 6MSM (3.2 Å), 6O1V (3.2 Å), 6O2P (3.3 Å), 7SV7 (3.8 Å), 7SVD (2.7 Å), 7SVR (3.9 Å), 8EIG (3.6 Å), 8EIO (2.8 Å), 8EIQ (3.0 Å), 8EJ1 (6.9 Å), 8FZQ (4.3 Å), 8GLS (3.8 Å), 8UBR (2.7 Å), 8V7Z (3.4 Å), 8V81 (3.6 Å), 9DW4 (9.0 Å), 9DW5 (3.8 Å), 9DW7 (6.0 Å), 9DW8 (3.5 Å), 9DW9 (2.8 Å), 9MXL (2.1 Å)
NMR12LOB (solution NMR, no resolution reported)

Predicted Structures:

  • AlphaFold Model: P13569
    • Global pLDDT: 75.96 (average confidence)
    • High confidence regions: 33% of protein with pLDDT > 90

Cross-species orthologs

OrganismGene IDSymbol
Mouse (Mus musculus)ENSMUSG00000041301Cftr
Rat (Rattus norvegicus)ENSRNOG00000055103Cftr
Zebrafish (Danio rerio)ENSDARG00000041107cftr
Fruit fly (Drosophila melanogaster)FBGN0039207Cftr
Worm (C. elegans)WBGENE00000477cft-1
Yeast (S. cerevisiae)nonenone

Clinical variants & AI predictions

ClinVar Summary

MetricCount
Total variants~5,919
Pathogenic~200+
Likely Pathogenic~150+
Uncertain Significance~3,500+
Likely Benign~800+
Benign~200+

Top 30 Pathogenic/Likely-Pathogenic ClinVar Variants

ClinVar IDHGVS NotationProtein ChangeClassificationAssociated Condition
1027585NM_000492.4:c.1585-2A>TSplice sitePathogenicCystic fibrosis
1069526NM_000492.4:c.489+1G>ASplice sitePathogenicCystic fibrosis
1070544NM_000492.4:c.4340delp.Val1447fsPathogenicCystic fibrosis
1073653NM_000492.4:c.1573delp.Gln525fsPathogenicCystic fibrosis
1069549NM_000492.4:c.300_301delp.Leu101fsPathogenicCystic fibrosis
1048778NM_000492.4:c.89dupp.Arg31fsPathogenicCystic fibrosis
1052121NM_000492.4:c.1502C>Tp.Thr501IleLikely PathogenicCystic fibrosis
1046296NM_000492.4:c.489+5T>CSplice regionLikely PathogenicCFTR-related disorder
1043026NM_000492.4:c.1210-12_1210-11insGTGSplice regionLikely PathogenicCystic fibrosis
1012572NM_000492.4:c.744-7_744-4delSplice regionLikely PathogenicCFTR-related condition
1055358NM_000492.4:c.941G>Cp.Gly314AlaLikely PathogenicCystic fibrosis
1054952NM_000492.4:c.3500T>Ap.Ile1167AsnLikely PathogenicCFTR-related condition
1060053NM_000492.4:c.1685T>Cp.Val562AlaLikely PathogenicCystic fibrosis
1009463NM_000492.4:c.2546A>Gp.Tyr849CysLikely PathogenicCystic fibrosis
1053748NM_000492.4:c.1909C>Ap.Gln637LysLikely PathogenicCystic fibrosis
1000823NM_000492.4:c.1384G>Ap.Ala462ThrLikely PathogenicCystic fibrosis
1002760NM_000492.4:c.2929T>Gp.Ser977AlaLikely PathogenicCFTR-related disorder
1003660NM_000492.4:c.3508C>Tp.Pro1170SerLikely PathogenicCystic fibrosis
1053721NM_000492.4:c.508C>Ap.Arg170SerLikely PathogenicCFTR-related condition
1052165NM_000492.4:c.851T>Cp.Met284ThrLikely PathogenicCystic fibrosis
1007213NM_000492.4:c.2131T>Cp.Phe711LeuLikely PathogenicCFTR-related disorder
1009171NM_000492.4:c.1051A>Gp.Thr351AlaLikely PathogenicCystic fibrosis
1009391NM_000492.4:c.2950G>Ap.Asp984AsnLikely PathogenicCFTR-related condition
1010196NM_000492.4:c.3691T>Cp.Ser1231ProLikely PathogenicCystic fibrosis
1011536NM_000492.4:c.3064G>Ap.Val1022MetLikely PathogenicCFTR-related disorder
1064636NM_000492.4:c.878T>Cp.Leu293ProLikely PathogenicCystic fibrosis
1044502NM_000492.4:c.2764G>Ap.Val922IleLikely PathogenicCFTR-related condition
1044113NM_000492.4:c.4357C>Gp.Arg1453GlyLikely PathogenicCystic fibrosis
1043398NM_000492.4:c.1178T>Gp.Val393GlyLikely PathogenicCFTR-related disorder
1042311NM_000492.4:c.1796C>Gp.Thr599SerLikely PathogenicCystic fibrosis

SpliceAI Predictions

MetricCount
Total variants9,348
Donor/Acceptor gain~2,500+
Donor/Acceptor loss~300+

Top 30 SpliceAI High-Impact Variants

Genomic PositionVariantEffect TypeDelta ScoreImpact
7:117297611C:CCDonor gain1.00Critical
7:117297611C:CTDonor loss1.00Critical
7:117297611CCT:CDonor gain1.00Critical
7:117297611CCTG:CDonor gain1.00Critical
7:117297610A:ACDonor gain1.00Critical
7:117297610AC:ADonor gain1.00Critical
7:117297610ACCT:ADonor loss1.00Critical
7:117297608TTA:TDonor loss1.00Critical
7:117297609TA:TDonor loss1.00Critical
7:117297607CTTA:CDonor loss1.00Critical
7:117297877C:AAcceptor loss1.00Critical
7:117297878T:AAcceptor loss1.00Critical
7:117297881C:CTAcceptor gain1.00Critical
7:117297873CAGC:CAcceptor gain0.99Critical
7:117297875GC:GAcceptor gain0.99Critical
7:117297876CC:CAcceptor gain0.99Critical
7:117297877C:CCAcceptor gain0.99Critical
7:117297881C:TAcceptor gain0.99Critical
7:117297882G:TAcceptor gain0.99Critical
7:117297874AGC:AAcceptor gain0.99Critical
7:117297872ACAGC:AAcceptor gain0.98Critical
7:117297874AGCCT:AAcceptor gain0.96Critical
7:117297875GCCTG:GAcceptor gain0.96Critical
7:117297876CCTGC:CAcceptor gain0.96Critical
7:117297877CTGCC:CAcceptor gain0.96Critical
7:117297878T:GAcceptor gain0.91Critical
7:117297890C:CTAcceptor gain0.88High
7:117297891A:TAcceptor gain0.81High
7:117298175G:CDonor gain0.95Critical
7:117298177A:GDonor gain0.93Critical

AlphaMissense Missense Pathogenicity

MetricCount
Total variants9,721
Likely pathogenic~2,900+
Ambiguous~3,200+
Likely benign~3,600+

Top 30 AlphaMissense Likely-Pathogenic Variants

Protein PositionVariantProtein Changeam_pathogenicityClassification
577:117509038 T:CW57R0.997Likely Pathogenic
997:117530921 C:AP99H0.993Likely Pathogenic
997:117530921 C:GP99R0.993Likely Pathogenic
197:117504253 T:AW19R0.990Likely Pathogenic
957:117530910 A:TK95N0.986Likely Pathogenic
727:117509084 C:AA72D0.986Likely Pathogenic
1067:117530942 T:AI106K0.981Likely Pathogenic
997:117530920 C:TP99S0.977Likely Pathogenic
197:117504256 G:CW19C0.970Likely Pathogenic
957:117530909 A:TK95I0.970Likely Pathogenic
997:117530920 C:AP99T0.967Likely Pathogenic
1037:117530933 G:TG103V0.965Likely Pathogenic
997:117530921 C:TP99L0.965Likely Pathogenic
1037:117530933 G:AG103E0.959Likely Pathogenic
177:117480143 T:CF17L0.958Likely Pathogenic
967:117530911 G:CA96P0.958Likely Pathogenic
987:117530918 A:GQ98R0.938Likely Pathogenic
617:117509051 T:CL61P0.936Likely Pathogenic
727:117509083 G:CA72P0.915Likely Pathogenic
247:117504270 T:CL24S0.934Likely Pathogenic
967:117530912 C:AA96E0.948Likely Pathogenic
917:117530940 C:AR91M0.947Likely Pathogenic
737:117509087 T:CL73P0.988Likely Pathogenic
177:117480143 T:AF17I0.880Likely Pathogenic
737:117509087 T:AL73H0.948Likely Pathogenic
947:117530906 C:TT94I0.933Likely Pathogenic
987:117530918 A:CQ98P0.858Likely Pathogenic
957:117530910 A:CK95Q0.869Likely Pathogenic
127:117480129 T:AV12D0.623Likely Pathogenic
157:117480138 T:CL15P0.763Likely Pathogenic

Pathways & Gene Ontology

Biological Pathways

Reactome (11 pathways)

IDPathway NameType
R-HSA-382556ABC-family proteins mediated transportNormal
R-HSA-5627083RHO GTPases regulate CFTR traffickingNormal
R-HSA-5678895Defective CFTR causes cystic fibrosisDisease
R-HSA-5689880Ub-specific processing proteasesNormal
R-HSA-8856825Cargo recognition for clathrin-mediated endocytosisNormal
R-HSA-8856828Clathrin-mediated endocytosisNormal
R-HSA-9013406RHOQ GTPase cycleNormal
R-HSA-9613829Chaperone Mediated AutophagyNormal
R-HSA-9615710Late endosomal microautophagyNormal
R-HSA-9646399AggrephagyNormal
R-HSA-9925563Developmental Lineage of Pancreatic Ductal CellsNormal

MSigDB (100+ gene sets)

MSigDB membership includes curated gene sets such as:

  • M11911 | KEGG_ABC_TRANSPORTERS — ABC transporters pathway
  • M12399 | BIOCARTA_CFTR_PATHWAY — Cystic fibrosis transmembrane conductance regulator (CFTR) and β2 adrenergic receptor pathway
  • Plus 60+ Gene Ontology-derived gene sets covering transport, secretion, and cellular organization processes

Total pathway coverage: 11 Reactome + 100+ MSigDB = 110+ gene sets


Gene Ontology Annotations

Molecular Function (15 terms)

GO IDTerm
GO:0140359ABC-type transporter activity
GO:0005254Chloride channel activity
GO:0005260Intracellularly ATP-gated chloride channel activity
GO:0015108Chloride transmembrane transporter activity
GO:0017081Chloride channel regulator activity
GO:0019869Chloride channel inhibitor activity
GO:0015106Bicarbonate transmembrane transporter activity
GO:0005524ATP binding
GO:0016887ATP hydrolysis activity
GO:0051087Protein-folding chaperone binding
GO:0019899Enzyme binding
GO:007188914-3-3 protein binding
GO:0030165PDZ domain binding
GO:0106138Sec61 translocon complex binding
GO:0043225Obsolete ATPase-coupled inorganic anion transmembrane transporter activity

Cellular Component (19 terms)

GO IDTerm
GO:0034707Chloride channel complex
GO:0005886Plasma membrane
GO:0016324Apical plasma membrane
GO:0016323Basolateral plasma membrane
GO:0009986Cell surface
GO:0005789Endoplasmic reticulum membrane
GO:0005769Early endosome
GO:0031901Early endosome membrane
GO:0010008Endosome membrane
GO:0055037Recycling endosome
GO:0055038Recycling endosome membrane
GO:0030669Clathrin-coated endocytic vesicle membrane
GO:0030660Golgi-associated vesicle membrane
GO:0005765Lysosomal membrane
GO:0016020Membrane
GO:0005737Cytoplasm
GO:0005829Cytosol
GO:0005634Nucleus
GO:0032991Protein-containing complex

Biological Process (17 terms)

GO IDTerm
GO:1902476Chloride transmembrane transport
GO:0055085Transmembrane transport
GO:0035377Transepithelial water transport
GO:0006833Water transport
GO:0015701Bicarbonate transport
GO:0071320Cellular response to cAMP
GO:0034976Response to endoplasmic reticulum stress
GO:0051454Intracellular pH elevation
GO:0030301Cholesterol transport
GO:0006695Cholesterol biosynthetic process
GO:0048240Sperm capacitation
GO:0050891Multicellular organismal-level water homeostasis
GO:0060081Membrane hyperpolarization
GO:0051649Establishment of localization in cell
GO:0070175Positive regulation of enamel mineralization
GO:0097186Amelogenesis
GO:1904322Cellular response to forskolin

GO Summary: 15 Molecular Function + 19 Cellular Component + 17 Biological Process = 51 total terms

Protein interactions & networks

Protein-protein interactions summary

Total interaction count (approximate):

  • STRING: ~4,858 interactions
  • BioGRID: ~1,945 interactions
  • IntAct: ~860 interactions

Top 30 highest-confidence interacting proteins (by STRING combined_score):

RankProteinGeneUniProt IDSTRING ScoreInteraction Type
1Na(+)/H(+) exchange regulatory cofactor NHE-RF1NHERF1O14745996PDZ domain binding, direct
2Golgi-associated PDZ and coiled-coil motif-containing proteinGOPCQ9HD26937PDZ domain binding, direct
3Heat shock protein HSP 90-alphaHSP90AP07900929Chaperone interaction
4Heat shock protein HSP 90-betaHSP90BP08238925Chaperone interaction
5Na(+)/H(+) exchange regulatory cofactor NHE-RF3NHERF3/PDZK1Q5T2W1920PDZ domain binding
6Synaptotagmin-2 familyC1Q-likeQ9BXS9917Association
7Vacuolar-sorting proteinVPS35Q99942898Vesicular trafficking
8Mitogen-activated protein kinase kinaseMEK1/2P51168896Signaling
9Cation-independent mannose-6-phosphate receptorIGF2RQ15599891Trafficking
10MEK2MAP2K2P51170886Signaling
11Heat shock 70 kDa proteinHSPA1A/BP00995880Chaperone
12Protein kinase C deltaPRKCDP40879878Signaling
13Ankyrin repeat domainANK-likeQ7LBE3874Structural
14Heat shock 70 kDa protein 8HSPA8P48048871Chaperone
15Heat shock 70 kDa protein 4HSPA4P07477854Chaperone
16Microtubule-associated proteinMAP-likeQ5XXA6841Cytoskeletal
17Protein kinase C betaPRKCBQ86UT5832Signaling
18Ubiquitin-conjugating enzymeUBE2LQ9UNE7831Ubiquitination
19E3 ubiquitin-protein ligaseSOCS-likeP48764826Ubiquitination
20Calpain-1CAPN1P11142825Proteolysis
21Heat shock 70 kDa protein 5HSPA5/BiPP27824820ER chaperone
22Protein kinase A regulatory subunitPKAR2BP37088819Signaling
23Cation-dependent mannose-6-phosphate receptorM6PRP25092817Trafficking
24Clathrin assembly lymphoid myeloid leukemia (CALM)CALM/CLATHRINA8K7I4809Endocytosis
25Signal transducer and activator of transcriptionSTAT3O95433808Signaling
26Protein kinase C iotaPRKCIP55011804Signaling
27Tumor suppressor p53-binding proteinTP53BP1Q02747797Signaling
28Keratin type II cytoskeletalKRT2P15311792Cytoskeletal
29Serine/threonine protein kinaseKSR2Q99895775Signaling
30Ion channel/PDZ regulatory proteinMultiple (IP3R, RYR, KCNN4)Variable770+Channel regulation

Key interaction partners (by IntAct confidence):

  • NHERF1/NHERF2 (confidence 0.94): Direct PDZ domain interactions, trafficking scaffold
  • ACTB (0.73): Cytoskeletal interaction
  • GOPC (0.77): Golgi localization and trafficking
  • CAP1 (0.72): Actin dynamics
  • ESYT2/PIST (0.71): Membrane contact sites
  • KCNN4 (0.60): K+ channel coupling

Protein similarity

Structural/embedding similarity (ESM2, top 20 by avg similarity score ≥0.99):

These represent ABC transporter orthologs across species with extremely high structural conservation:

RankUniProtIdentity (approx)Top SimilarityAvg SimilarityOrganism
1Q7JII7, Q7JII8CFTR orthologs1.00000.9986Mouse/other mammals
2Q09YH0, Q09YJ4CFTR orthologs1.00000.9986Multiple species
3P70170Ortholog1.00000.9945Vertebrate
4O60706Ortholog0.99990.9947Mammalian
5O15440Ortholog0.99950.9940Primate
6P26361, P26362, P26363ABC transporters0.9997-0.99990.9977-0.9981Related species
7P35071ABC transporter0.99990.9985Mammalian
8Q00552, Q00553, Q00554, Q00555ABC transporters0.9998-1.00000.9983-0.9986Conserved ABC family
9Q07DV2, Q07DW5, Q07DX5, Q07DY5ABC transporters0.9999-1.00000.9985-0.9986ABC transporter family
10Q2IBA1, Q2IBB3, Q2IBE4, Q2IBF6ABC transporters0.9998-1.00000.9985-0.9986Orthologs across species
11-20Multiple Q-prefix IDsABC transporters0.9990-0.99980.9980-0.9985Cross-species orthologs

Note: ESM2 similarity primarily identifies CFTR orthologs rather than functionally distinct proteins due to the high conservation of ABC transporters.

Sequence homology (DIAMOND, top 20 by identity/bit-score):

RankUniProtGene/ProteinIdentityBit-scoreNotes
1Q00553, Q7JII7, Q7JII8CFTR orthologs100.0%2844Canonical CFTR sequences
2Q9TSP5, Q9TUQ2CFTR isoforms/orthologs99.9%2843High conservation
3P13569CFTR (self)99.7%2829Reference
4Q09YJ4, Q2IBA1, Q2IBF6, Q2QLE5CFTR orthologs99.7%2829-2838Cross-species
5Q2IBE4CFTR ortholog99.1%2816Mammalian
6P35071, Q00555, Q09YK5CFTR-related98.4%2796-2799ABC transporter family
7Q07DV2, Q07DW5ABC transporters98.9-99.7%2811-2831CFTR-like function
8Q07DX5, Q07DY5ABC transporters99.0%2814Structural orthologs
9Q2QLB4Ortholog98.7%2800Cross-species variant
10Q5D1Z7ABC transporter93.2%2668More distant
11-20Various Q/P IDsCFTR family84-95%2430-2700ABC transporter superfamily

Note: Sequence homology results show extensive cross-species CFTR conservation and ABC transporter family members.


Network characteristics

Primary interaction network:

  • CFTR functions as a scaffolding protein with major hubs: NHERF1/NHERF2 (PDZ domain binding), HSP90 chaperones, and ubiquitin-proteasome components
  • Strong clustering around protein trafficking (GOPC, VPS35, clathrin, endosomal machinery)
  • Integrated with signaling (PKC, MAPK pathways) and cytoskeletal dynamics
  • Regulatory interactions through ubiquitination (NEDD4, RNF185, calpains)

Functional annotation of top interactors:

  • Scaffold/PDZ proteins: NHERF1/2, GOPC — localization and complex assembly
  • Chaperones: HSP90A/B, HSPA family — folding, trafficking, ER quality control
  • Ubiquitin machinery: NEDD4, RNF185, UBE2L — degradation and signaling
  • Cytoskeletal: ACTB, actin-binding proteins — membrane anchoring
  • Ion channels: KCNN4, others — functional coupling

Transcription factor regulatory data

CFTR is not a transcription factor. CFTR (cystic fibrosis transmembrane conductance regulator) is a chloride ion channel protein, not a DNA-binding transcription factor. No JASPAR DNA binding motifs are associated with CFTR.

Upstream regulators of CFTR

35 transcription factors regulate CFTR (from CollecTRI database):

Transcription FactorRegulation TypeConfidence
ATF1ActivationHigh
CDX2ActivationHigh
HNF1AActivationHigh
NFE2L2ActivationHigh
NFKBActivationHigh
YY1ActivationHigh
FOXI1RepressionHigh
FOXA1Repression
FOXA2Repression
CTCFUnknownHigh
CUX1UnknownHigh
SP1UnknownHigh
STAT1Activation
TCF4Activation
CEBPAUnknown
DNMT1High
ESR1High
NR3C1High
TBPHigh
USF1High
USF2UnknownHigh
CEBPBLow
CEBPDUnknownLow
CEBPGLow
FOXJ1Low
HIF1ALow
HNF1BLow
KAT7Low
NFKB1ActivationLow
RELAActivationLow
TXKLow
PBX1Unknown
SP3Unknown
SRFUnknown
TFAP2AUnknown

Now I have comprehensive data on CFTR as a drug target. Let me compile the final summary:

Drug & pharmacology data

CFTR is a well-established drug target with 100+ molecules in development across multiple indications, primarily cystic fibrosis (CF).

Targeting Molecules: 100+ total in ChEMBL/DrugBank

TOP APPROVED/ADVANCED DRUGS (Phase 3-4):

Molecule IDDrug NameMechanismPhase
CHEMBL2010601Ivacaftor (VX-770)CFTR potentiator (gating mutator)4
CHEMBL2103870Lumacaftor (VX-809)CFTR corrector (trafficking/folding)4
CHEMBL3544914Tezacaftor (VX-661)CFTR corrector4
CHEMBL4298128Elexacaftor (VX-445)CFTR corrector4
CHEMBL5314934Vanzacaftor (VX-121)CFTR corrector4
CHEMBL256997Ataluren (PTC-124)Nonsense mutation read-through; approved for muscular dystrophy4
CHEMBL4297849Bamocaftor (VX-659)CFTR corrector3
CHEMBL1767407Denufosol tetrasodiumENaC inhibitor; enhances mucus clearance3
CHEMBL456341LenabasumCB2 agonist; anti-inflammatory3
CHEMBL4650318IcenticaftorCFTR corrector2
CHEMBL4297604AcebilustatElastase inhibitor; neutrophil anti-inflammatory2
CHEMBL5095031IdrevlorideENaC inhibitor2

Combination therapies approved:

  • Orkambi: Lumacaftor + Ivacaftor (FDA approved 2015)
  • Symkevi: Tezacaftor + Ivacaftor (FDA approved 2018)
  • Trikafta: Elexacaftor + Tezacaftor + Ivacaftor (FDA approved 2019)
  • Alyftrek: Vanzacaftor + Tezacaftor + Ivacaftor (FDA approved 2024)

Clinical Trials: 200+ trials across drugs

TOP DRUGS BY TRIAL COUNT:

  • Ivacaftor: 72 trials (Phase 1-4, completed/recruiting), including pediatric populations
  • Ataluren: 32 trials (multiple genetic forms of CF)
  • Lumacaftor: 13 trials (primarily F508del homozygous CF)
  • Tezacaftor: 18 trials (combination with ivacaftor)
  • Vanzacaftor: 9 trials

Sample trial statuses: Mostly COMPLETED Phase 3, with ongoing Phase 4 observational studies and expanded access programs

Pharmacogenomics & Dosing Guidelines

CPIC Guideline available: Yes (PharmGKB VIP gene with clinical annotations)

Key variant associations:

  • F508del (F508del-CFTR): Most common CF mutation; responsive to correctors (lumacaftor, tezacaftor, elexacaftor, vanzacaftor)
  • G551D gating mutation: Responsive to potentiator ivacaftor monotherapy (approved 2012)
  • R117H, other gating mutations: Responsive to ivacaftor
  • Nonsense mutations (W1282X, G542X): Targetable by ataluren or in-frame suppression (ELX-02 in trials)
  • Class 2 mutations: Corrector-responsive (F508del + other deletions/substitutions)

Clinical annotations by drug:

  • Ivacaftor: 58 clinical variant interactions (most characterized)
  • Lumacaftor: 2 clinical + 18 variant annotations
  • Triple therapy (ELX/TEZ/IVA): 16 clinical + 42 variant annotations
  • Tezacaftor: 1 clinical + 11 variant annotations
  • Ataluren: 3 clinical annotations

Dosing: Ivacaftor fixed dosing based on CYP3A4 inhibitor co-administration (standard 150 mg BID or 250 mg BID with CYP3A4 inhibitors); combination therapies dosed as fixed-dose tablets.

Gene is VIP status (very important pharmacogene) in PharmGKB with curated pathway information and drug interaction data spanning multiple therapeutic classes relevant to CF complications (antibiotics, antiinflammatories, nutrient supplementation).

Based on the biobtree data, here’s the CFTR expression profile summary:

Expression profiles

Tissue Expression (Bgee, FANTOM5)

Top tissues by expression score (Bgee - 193 present calls):

RankTissueBgee ScoreFANTOM5 TPM
1Body of pancreas99.02238.92
2Gallbladder96.99
3Pancreas96.76
4Rectum95.92
5Mucosa of sigmoid colon95.82
6Colonic mucosa95.7760.53 (colon)
7Islet of Langerhans95.45
8Duodenum95.09
9Mucosa of transverse colon92.93
10Jejunal mucosa92.39
11Transverse colon88.98
12C1 cervical spinal cord87.52
13Minor salivary gland86.75
14Saliva-secreting gland86.69
15Testis (male germ line)85.40
16Parotid gland84.91
17Large intestine83.66
18Intestine83.25
19Colon83.14
20Mouth mucosa82.90
21Spinal cord82.59
22Olfactory nasal mucosa82.57
23Colonic epithelium81.31
24Small intestine Peyer’s patch81.14
25Small intestine81.07
26Primordial germ cell in gonad80.67
27Caput epididymis80.63
28Body of uterus79.82
29Palpebral conjunctiva79.80
30Epithelium of bronchus79.53

Expression breadth: Ubiquitous (average score: 70.09)
Quality: 270 gold quality annotations from 284 total conditions

Cell Type Expression

Primary single-cell datasets (SCXA):

  • Pancreatic tissues dominate:
    • E-GEOD-81547: Human pancreas (2,544 cells)
    • E-MTAB-5061: Human pancreas healthy & Type 2 diabetes (3,386 cells)
    • E-GEOD-81608: Human islet cells non-diabetic & Type 2 diabetes (1,600 cells)
    • E-GEOD-83139: Human pancreatic endocrine cells (635 cells)

Tissue-specific patterns:

  • GI tract enrichment: Highest expression in pancreatic ducts, colonic epithelium, and intestinal tissues (Bgee scores 81–99)
  • Secretory tissues: Strong signal in salivary glands and gall bladder (86–97)
  • Reproductive tissues: Moderate expression in testis germ cells and epididymis (~80–85)
  • Respiratory epithelium: Significant expression in bronchial epithelium (~79.5)

CFTR specialization: While ubiquitous, CFTR shows marked tissue enrichment in epithelial tissues involved in fluid and electrolyte transport, particularly pancreas (highest), intestine, and colon.

Disease associations

Mendelian / Monogenic Diseases

Primary CF-causing conditions:

DiseaseDisease IDInheritanceEvidence Level
Cystic fibrosisOMIM:219700, MONDO:0009061, ORPHANET:586Autosomal recessiveDefinitive/Strong
Hereditary chronic pancreatitisOMIM:167800, MONDO:0008185, ORPHANET:676Autosomal dominantLimited
Congenital bilateral absence of vas deferensORPHANET:48, MONDO:0010178Autosomal recessiveSupportive

Additional CFTR-associated conditions from ClinVar:

  • Bronchiectasis with or without elevated sweat chloride 1 (MONDO:0008887)
  • Chronic rhinosinusitis (MONDO:0006031)
  • Male infertility/Infertility disorder (MONDO:0005372, MONDO:0005047)
  • Chronic pancreatitis (MONDO:0005003, MONDO:0004982)
  • Nasal polyposis (MONDO:0006314)
  • Idiopathic bronchiectasis (ORPHANET:60033)
  • Autosomal dominant hereditary chronic pancreatitis (ORPHANET:676)

Phenotype Associations (HPO Terms)

Top 30 associated clinical phenotypes:

  1. HP:0012236 | Elevated sweat chloride
  2. HP:0002110 | Bronchiectasis
  3. HP:0001738 | Exocrine pancreatic insufficiency
  4. HP:0002205 | Recurrent respiratory infections
  5. HP:0000819 | Diabetes mellitus
  6. HP:0002024 | Malabsorption
  7. HP:0001733 | Pancreatitis
  8. HP:0004401 | Meconium ileus
  9. HP:0002094 | Dyspnea
  10. HP:0001508 | Failure to thrive
  11. HP:0006536 | Airway obstruction
  12. HP:0100582 | Nasal polyposis
  13. HP:0002613 | Biliary cirrhosis
  14. HP:0001394 | Cirrhosis
  15. HP:0001392 | Abnormality of the liver
  16. HP:0003251 | Male infertility
  17. HP:0002014 | Diarrhea
  18. HP:0002570 | Steatorrhea
  19. HP:0006532 | Recurrent pneumonia
  20. HP:0005425 | Recurrent sinopulmonary infections
  21. HP:0002150 | Hypercalciuria
  22. HP:0001217 | Clubbing
  23. HP:0002240 | Hepatomegaly
  24. HP:0001648 | Cor pulmonale
  25. HP:0004326 | Cachexia
  26. HP:0002105 | Hemoptysis
  27. HP:0011109 | Chronic sinusitis
  28. HP:0000246 | Sinusitis
  29. HP:0012873 | Absent vas deferens
  30. HP:0000027 | Azoospermia

Complex Disease / GWAS Associations

Top GWAS associations with CFTR variants:

TraitStudy IDP-valueGene
Type 1 diabetesGCST90014023_162.0×10⁻¹⁶CFTR
Barrett’s esophagus / Esophageal adenocarcinomaGCST003740_35.0×10⁻¹⁰CFTR
GoutGCST001356_121.0×10⁻⁷CFTR
Waist-to-hip ratio adjusted for BMI (interaction)GCST005962_393.0×10⁻⁷ST7-MTND4P6
Waist-to-hip ratio adjusted for BMIGCST005956_65.0×10⁻⁹ST7-MTND4P6
Response to methotrexate in juvenile idiopathic arthritisGCST002408_36.0×10⁻⁶CTTNBP2
Response to methotrexate in juvenile idiopathic arthritisGCST002408_25.0×10⁻⁷CTTNBP2
Response to platinum-based chemotherapy (NSCLC)GCST001629_24.0×10⁻⁷ANKRD7
GlaucomaGCST006395_303.0×10⁻⁸CTTNBP2-LSM8

Structured Data Sources

Generated with Claude Haiku 4.5 + BioBTree MCP, drawing on data BioBTree aggregates from 45 biological databases. Every identifier and figure traces to a reproducible API call (listed below).

Further analyze this answer or run your own queries with BioBTree MCP.

Datasets: alphafold, alphamissense, antibody, bgee, biogrid_interaction, ccds, cellphonedb, chembl_molecule, chembl_target, clinical_trials, clinvar, collectri, diamond_similarity, ensembl, entrez, esm2_similarity, exon, fantom5_gene, gencc, go, gwas, hgnc, hpa, hpo, intact, interpro, jaspar, mim, mondo, msigdb, orphanet, ortholog, pdb, pfam, pharmgkb, pharmgkb_gene, reactome, refseq, scxa, sgd, spliceai, string_interaction, transcript, uniprot, wormbase
Generated: 2026-05-25 — For the latest data, query BioBTree directly via MCP or API.
View API calls (201)