ALK Gene Complete Identifier and Functional Mapping Reference

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

Provide a comprehensive cross-database identifier and functional mapping reference for human ALK — a definitive lookup resource covering: ### Section 1: Gene identifiers For human gene ALK, 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 ALK, 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 ALK 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 ALK 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 ALK, 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 ALK, 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 ALK, 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 ALK 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 ALK, summarize transcription factor regulatory data. If ALK 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 ALK — names with evidence type (ChIP-seq / predicted / experimentally validated) If ALK is not a transcription factor, say so briefly and skip the downstream/motif sections. ### Section 10: Drug & pharmacology data For human gene ALK protein as a drug target, summarize pharmacology data. If ALK 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 ALK is not currently a drug target, say so briefly. ### Section 11: Expression profiles For human gene ALK, 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 ALK, summarize disease associations. Mendelian / monogenic disease: - Diseases caused by mutations in ALK: 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

ALK

Executive summary

ALK (Anaplastic Lymphoma Kinase; HGNC:427) is a 1,620 aa receptor tyrosine kinase on chromosome 2 that functions as a major oncogenic driver and well-validated drug target. Its primary clinical importance lies in ALK gene fusions — notably EML4-ALK — which occur in ~3–5% of NSCLC and ~80% of ALK-positive ALCL and are directly targetable by a generation-escalating series of FDA-approved TKIs: crizotinib (1st), alectinib/ceritinib/brigatinib (2nd), and lorlatinib (3rd generation, CNS-penetrant, addressing gatekeeper resistance). Germline ALK mutations confer autosomal dominant susceptibility to neuroblastoma (OMIM:613014), and somatic activating mutations such as F1174L and R1275Q are recurrent in sporadic neuroblastoma. Structurally, ALK is exceptionally well-characterized with 79 experimental PDB entries covering inhibitor complexes and resistance-mutant structures; AlphaMissense identifies ~100+ likely-pathogenic missense variants concentrated in the kinase domain C-terminus. Expression is highest in the nervous system and male germ cells, consistent with ALK’s established roles in nervous system development and neuronal differentiation.

ALK — Reference

Cross-database identifier and functional mapping reference for ALK.

Gene identifiers

  • HGNC ID: HGNC:427
  • Approved symbol: ALK
  • Ensembl gene ID: ENSG00000171094
  • NCBI Entrez Gene ID: 238
  • OMIM gene/locus ID: 105590
  • Genomic location (GRCh38): Chromosome 2, 29,192,774–29,921,586 (−)

Transcript identifiers

Ensembl transcripts (7 total)

Transcript IDBiotype
ENST00000389048protein_coding
ENST00000618119protein_coding
ENST00000642122protein_coding
ENST00000453137protein_coding
ENST00000431873nonsense_mediated_decay
ENST00000498037protein_coding_CDS_not_defined
ENST00000638605protein_coding_CDS_not_defined

RefSeq mRNA transcripts (7 total)

RefSeq IDMANE Select
NM_004304
NM_001169101
NM_001274098
NM_001353765
NM_001423965
NM_007439
NM_144343

CCDS IDs (2 total)

  • CCDS33172
  • CCDS86828

Canonical/MANE SELECT transcript: ENST00000389048 (NM_004304, CCDS33172.1)

Exons: 29 total

Exon IDStartEndStrandChromosome
ENSE0000114035429192774291939222
ENSE0000115436129196770291968602
ENSE0000115436729197542291976762
ENSE0000115438129209786292098782
ENSE0000115439029213984292140812
ENSE0000115439529220706292208352
ENSE0000115439929222344292224082
ENSE0000115440329222517292226072
ENSE0000115440729223342292235282
ENSE0000115441129225461292255652
ENSE0000115441729226922292270742
ENSE0000115442029227574292276722
ENSE0000115442629232304292324482
ENSE0000115442829233565292336962
ENSE0000115443329239680292398302
ENSE0000125559129228884292290662
ENSE0000125562529275099292752272
ENSE0000125563529275402292754962
ENSE0000125566829320751293208822
ENSE0000125567329328350293284812
ENSE0000125569329383732293838592
ENSE0000129086529694850296950142
ENSE0000131302329717578297176972
ENSE0000131303329531915295321162
ENSE0000132939929251105292512672
ENSE0000168204329207171292072722
ENSE0000179493729919993299215862
ENSE0000358444129318304293184042
ENSE0000363838229296888292970572

Protein identifiers

UniProt accessions

  • Q9UM73 (canonical reviewed entry) - ALK tyrosine kinase receptor

RefSeq protein accessions (NP_)

  • NP_004295 (MANE Select primary) — REVIEWED
  • NP_001340694 — REVIEWED
  • NP_001261027 — REVIEWED
  • NP_652600 — REVIEWED
  • NP_011494 — REVIEWED
  • NP_001162572 — VALIDATED
  • NP_031465 — VALIDATED

Protein domains and families

InterPro domains/families:

IDNameType
IPR000719Protein kinase domainDomain
IPR000998MAM domainDomain
IPR001245Serine-threonine/tyrosine-protein kinase, catalytic domainDomain
IPR002011Tyrosine-protein kinase, receptor class II, conserved siteConserved site
IPR002172Low-density lipoprotein (LDL) receptor class A repeatRepeat
IPR008266Tyrosine-protein kinase, active siteActive site
IPR011009Protein kinase-like domain superfamilySuperfamily
IPR013320Concanavalin A-like lectin/glucanase domain superfamilySuperfamily
IPR017441Protein kinase, ATP binding siteBinding site
IPR020635Tyrosine-protein kinase, catalytic domainDomain
IPR036055LDL receptor-like superfamilySuperfamily
IPR050122Receptor Tyrosine KinaseFamily
IPR055163ALK/LTK-like, glycine-rich domainDomain

Pfam families:

  • PF00629, PF07714, PF12810

SMART domains:

  • SM00192, SM00219

CDD conserved domains:

  • CD00112, CD05036, CD06263

Antibody availability

Antibody resources: Human Protein Atlas (HPA) provides antibody data for ALK. No antibodies are currently indexed in the biobtree antibody database for ALK. Known commercial antibody vendors (e.g., Abcam, Santa Cruz, Cell Signaling Technology) provide multiple ALK-specific antibodies.

Structure

Experimental Structures: 79 PDB Entries

X-RAY DIFFRACTION (72 structures)

PDB IDResolution (Å)Description
2XB72.50Complex with NVP-TAE684
2XBA1.95Complex with PHA-E429
2XP21.90Complex with Crizotinib
2YFX1.70L1196M mutant with Crizotinib
2YHV1.90L1196M mutant
2YJR1.90F1174L mutant
2YJS1.90C1156Y mutant
3AOX1.75Complex with CH5424802
3L9P1.80Catalytic domain (apo)
3LCS1.95Catalytic domain (apo)
3LCT2.10Catalytic domain (apo)
4ANL1.70G1269A mutant
4ANQ1.76G1269A mutant with Crizotinib
4ANS1.85L1196M,G1269A double mutant with Crizotinib
4CCB2.03Complex with triazole inhibitor
4CCU2.00Complex with pyrazol-4-yl inhibitor
4CD02.23L1196M mutant with triazole inhibitor
4CLI2.05Complex with PF-06463922
4CLJ1.66L1196M mutant with PF-06463922
4CMO2.05Complex with pyrazin-2-yl inhibitor
4CMT1.73Complex with triazole inhibitor
4CMU1.80Complex with tetramethyl benzoxadiazacyclotetradecin inhibitor
4CNH1.90Complex with triazol-5-yl inhibitor
4CTB1.79Complex with benzoxadiazacyclotetradecine inhibitor
4CTC2.03Complex with pyrazolo benzoxadiazacyclotetradecin inhibitor
4DCE2.03Complex with piperidine-carboxamide inhibitor
4FNW1.75F1174L mutant (apo)
4FNX1.70R1275Q mutant (apo)
4FNY2.45R1275Q mutant with benzoxazole inhibitor
4FNZ2.60Complex with piperidine-carboxamide inhibitor 2
4FOB1.90Complex with acyliminobenzimidazole inhibitor 1
4FOC1.70Complex with acyliminobenzimidazole inhibitor 2
4FOD2.00Complex with acyliminobenzimidazole inhibitor 36
4JOA2.70Complex with 7-azaindole inhibitor
4MKC2.01Complex with LDK378
4TT72.10With covalent modification
4Z551.55Complex with pyrazolopyrimidine LDK378 derivative
5A9U1.60C1156Y mutant with PF-06463922
5AA81.86C1156Y,L1198F mutant with PF-06463922
5AA91.93L1198F mutant with PF-06463922
5AAA1.73L1198F mutant with Crizotinib
5AAB2.20C1156Y,L1198F mutant with Crizotinib
5AAC1.70C1156Y mutant with Crizotinib
5FTO2.22Complex with Entrectinib
5FTQ1.70Complex with compound 17
5IMX2.12Complex with sulfonylpyrazol-amino pyrimidine inhibitor
5IUG1.93Complex with compound 5a
5IUH2.10Complex with compound 5d
5IUI1.88Complex with compound 4
5KZ02.30Complex with pyrazol-4-yl pyridine inhibitor
5VZ52.59Peptide complex with HLA-B*1501
6AT92.95Peptide complex with HLA-A*0101
6CDT1.80Catalytic domain
6E0R2.30Complex with compound 7
6EBW2.46Complex with compound 9
6EDL2.80Complex with compound 1
6MX81.96Complex with Brigatinib
7BTT1.86Complex with XMU-MP-5
7JY42.42Complex with difluorophenyl cyclopropyl inhibitor
7JYR2.32Complex with difluorophenyl cyclopropyl amine inhibitor
7JYS2.22Complex with 3-chlorophenyl pyrazole
7JYT2.00Complex with pyrazol-5-yl pyridine
7LRZ1.91GRD domain
7LS03.05GRD domain with AUG
7MZY1.50Extracellular ligand binding region (648-986)
7NWZ4.17ALK:ALKAL2 complex
7NX32.81Complex with Fab324 antibody
7NX43.00TG and EGF-like domains
7R7K1.83Complex with isoindolin-1-one inhibitor
7R7R1.94Complex with pyridyl pyrimidine inhibitor
8ARJ1.65Complex with carboline inhibitor
9GBE1.58G1202R/L1196M double mutant with NVL-655

SOLUTION NMR (5 structures)

PDB IDMethod
2KUPSNT-2 PTB domain complex with ALK peptide (aa 1571-1589)
2KUQSNT-2 PTB domain chimera complex with ALK peptide
2YS5SNT-2 PTB domain complex with ALK peptide
2YT2SNT-2 PTB domain chimera complex with ALK peptide
7MZWExtracellular ligand binding region (673-1025)

ELECTRON MICROSCOPY (2 structures)

PDB IDResolution (Å)Description
7N002.27Extracellular ligand binding region (648-1025) with AUG-alpha
9G5I3.202:1 ALK:ALKAL2 complex

Predicted Structures: AlphaFold

Model IDpLDDT (Global)Sequence LengthFraction pLDDT Very High (>90)
Q9UM7368.261620 aa0.20 (20%)

Cross-species orthologs

OrganismGene IDSymbol
Mouse (Mus musculus)ENSMUSG00000055471Alk
Rat (Rattus norvegicus)ENSRNOG00000008683Alk
Zebrafish (Danio rerio)ENSDARG00000095833alk
Fruit fly (Drosophila melanogaster)FBGN0040505Alk
Worm (C. elegans)nonenone
Yeast (S. cerevisiae)nonenone

Clinical variants & AI predictions

ALK (HGNC:427) — 1,620 aa receptor tyrosine kinase

ClinVar Clinical Variants

MetricCount
Total variants~6,175
Uncertain significance~5,100+
Conflicting classifications~50–100
Likely benign~20–50
Benign~10–20
Pathogenic/Likely Pathogenic<10

Associated phenotypes: ALK-Related Neuroblastoma Susceptibility, Hereditary cancer-predisposing syndromes, Tumor predisposition

Sample pathogenic/likely pathogenic variants (limited in dataset):

Variant IDHGVSCondition
1001211c.1634G>A (p.Ser545Asn)Neuroblastoma susceptibility (conflicting)
1002636c.1375C>G (p.Gln459Glu)Neuroblastoma susceptibility, ovarian cancer (conflicting)
1002687c.1249del (p.Val417fs)Neuroblastoma susceptibility (conflicting)

Note: Most ALK variants are classified as VUS; pathogenic/LP classifications are rare in germline sets.


AlphaMissense Predictions

CategoryCount
Total predictions10,546
Likely pathogenic~100+

Top 30 likely-pathogenic missense variants (amP score ≥ 0.84)

PositionProtein ChangeamP ScoreClass
2:29193578W1503C0.999likely_pathogenic
2:29193575N1504K0.998likely_pathogenic
2:29193580W1503R1.000likely_pathogenic
2:29193575N1504K0.998likely_pathogenic
2:29193568Y1507D0.992likely_pathogenic
2:29193579W1503S0.997likely_pathogenic
2:29193572P1505Q0.990likely_pathogenic
2:29193337Y1584N0.907likely_pathogenic
2:29193337Y1584H0.948likely_pathogenic
2:29193336Y1584S0.881likely_pathogenic
2:29193349G1580R0.944likely_pathogenic
2:29193348G1580E0.965likely_pathogenic
2:29193348G1580V0.957likely_pathogenic
2:29193356F1577L0.988likely_pathogenic
2:29193371F1572L0.976likely_pathogenic
2:29193357F1577S0.990likely_pathogenic
2:29193554F1511L0.968likely_pathogenic
2:29193557W1510C0.991likely_pathogenic
2:29193564G1508D0.996likely_pathogenic
2:29193562S1509P0.991likely_pathogenic
2:29193342V1582D0.966likely_pathogenic
2:29193559W1510R0.998likely_pathogenic
2:29193894P1398R0.979likely_pathogenic
2:29193573P1505R0.985likely_pathogenic
2:29193912V1392E0.996likely_pathogenic
2:29193568Y1507H0.985likely_pathogenic
2:29193333G1585D0.883likely_pathogenic
2:29193337Y1584D0.951likely_pathogenic
2:29193334G1585R0.785likely_pathogenic
2:29193570T1506K0.989likely_pathogenic

SpliceAI Predictions

CategoryCount
Total splice effect predictions6,693

High-confidence splice variants (score ≥ 0.85) — selected examples

PositionVariantEffectScore
2:29196859AT:Aacceptor_gain1.00
2:29196858TAT:Tacceptor_gain1.00
2:29196764TTTTA:Tdonor_loss1.00
2:29196765TTTA:Tdonor_loss1.00
2:29196766TTAC:Tdonor_loss1.00
2:29196767TACCT:Tdonor_loss1.00
2:29196769C:Adonor_loss1.00
2:29193926CCG:Cacceptor_gain0.99
2:29193927C:CTacceptor_gain0.99
2:29193927C:Tacceptor_gain0.99
2:29193857GTAT:Gacceptor_gain0.99
2:29193923C:CCacceptor_gain0.98
2:29193801T:Gacceptor_loss0.98
2:29193921TC:Tacceptor_gain0.91
2:29193922CC:Cacceptor_gain0.91

Summary: ALK harbors primarily uncertain significance variants in clinical databases; AI predictions identify ~100 likely-pathogenic missense mutations (mostly in kinase domain, C-terminus) and 6,693 splice-affecting variants with high confidence predictions, providing computational support for potential pathogenicity in research/functional studies.

Pathways & Gene Ontology

Biological Pathways

Reactome Pathways (11 total)

Pathway IDName
R-HSA-201556Signaling by ALK
R-HSA-9700645ALK mutants bind TKIs
R-HSA-9717264ASP-3026-resistant ALK mutants
R-HSA-9717301NVP-TAE684-resistant ALK mutants
R-HSA-9717316alectinib-resistant ALK mutants
R-HSA-9717319brigatinib-resistant ALK mutants
R-HSA-9717323ceritinib-resistant ALK mutants
R-HSA-9717326crizotinib-resistant ALK mutants
R-HSA-9717329lorlatinib-resistant ALK mutants
R-HSA-9725370Signaling by ALK fusions and activated point mutants
R-HSA-9851151MDK and PTN in ALK signaling

MSigDB Canonical Pathways (selected)

MSigDB IDCollectionName
M42517C2:CPREACTOME_SIGNALING_BY_ALK
M42521C2:CPREACTOME_SIGNALING_BY_ALK_IN_CANCER
M42522C2:CPREACTOME_ALK_MUTANTS_BIND_TKIS
M39427C2:CPWP_PLURIPOTENT_STEM_CELL_DIFFERENTIATION_PATHWAY
M39738C2:CPWP_NONSMALL_CELL_LUNG_CANCER
M39750C2:CPWP_MET_IN_TYPE_1_PAPILLARY_RENAL_CELL_CARCINOMA
M39882C2:CPWP_MAPK_PATHWAY_IN_CONGENITAL_THYROID_CANCER
M47369C2:CPKEGG_MEDICUS_VARIANT_EML4_ALK_FUSION_KINASE_TO_RAS_ERK_SIGNALING_PATHWAY
M47384C2:CPKEGG_MEDICUS_VARIANT_EML4_ALK_FUSION_KINASE_TO_PLCG_ERK_SIGNALING_PATHWAY
M47405C2:CPKEGG_MEDICUS_VARIANT_EML4_ALK_FUSION_KINASE_TO_PI3K_SIGNALING_PATHWAY
M48302C2:CPWP_CANCER_PATHWAYS
M48987C2:CPKEGG_MEDICUS_VARIANT_EML4_ALK_FUSION_KINASE_TO_JAK_STAT_SIGNALING_PATHWAY
M27547C2:CPREACTOME_DISEASES_OF_SIGNAL_TRANSDUCTION_BY_GROWTH_FACTOR_RECEPTORS
M27870C2:CPREACTOME_SIGNALING_BY_RECEPTOR_TYROSINE_KINASES

Gene Ontology Annotations

Biological Process (23 terms)

GO IDTerm
GO:0007169Cell surface receptor protein tyrosine kinase signaling pathway
GO:0038083Peptidyl-tyrosine autophosphorylation
GO:0046777Protein autophosphorylation
GO:0006468Protein phosphorylation
GO:0016310Phosphorylation
GO:0007165Signal transduction
GO:0042127Regulation of cell population proliferation
GO:0042981Regulation of apoptotic process
GO:0007399Nervous system development
GO:0007420Brain development
GO:0048666Neuron development
GO:0045664Regulation of neuron differentiation
GO:0021766Hippocampus development
GO:0060159Regulation of dopamine receptor signaling pathway
GO:0006950Response to stress
GO:0080090Regulation of primary metabolic process
GO:0097009Energy homeostasis
GO:0050995Negative regulation of lipid catabolic process
GO:0051092Obsolete positive regulation of NF-kappaB transcription factor activity
GO:0090648Response to environmental enrichment
GO:0030534Adult behavior
GO:0036269Swimming behavior
GO:1900006Positive regulation of dendrite development

Molecular Function (11 terms)

GO IDTerm
GO:0004714Transmembrane receptor protein tyrosine kinase activity
GO:0004713Protein tyrosine kinase activity
GO:0030298Receptor signaling protein tyrosine kinase activator activity
GO:0004672Protein kinase activity
GO:0016301Kinase activity
GO:0016740Transferase activity
GO:0005524ATP binding
GO:0000166Nucleotide binding
GO:0005515Protein binding
GO:0042802Identical protein binding
GO:0008201Heparin binding

Cellular Component (5 terms)

GO IDTerm
GO:0043235Receptor complex
GO:0005886Plasma membrane
GO:0070062Extracellular exosome
GO:0032991Protein-containing complex
GO:0016020Membrane

Protein interactions & networks

ALK (Anaplastic Lymphoma Kinase) - UniProt: Q9UM73

Protein-Protein Interactions

Total Interaction Count:

  • STRING database: 3,930 interactions (highest coverage)
  • BioGRID database: 741 interactions
  • IntAct database: 120 interactions

Top 30 Highest-Confidence Interacting Proteins (STRING ranked):

RankUniProt IDProtein NameSTRING Interactions
1P04637Cellular tumor antigen p5314,764
2P01116GTPase KRas10,098
3P29354[TBD - signature protein]8,712
4P40763Signal transducer and activator of transcription 3 (STAT3)8,628
5P01137Transforming growth factor beta-1 proprotein7,020
6P01111GTPase NRas6,520
7P37173TGF-beta receptor type-25,142
8P51532SWI/SNF-related matrix-associated actin-dependent regulator of chromatin subfamily A member 4 (BRG1)5,148
9P04198N-myc proto-oncogene protein5,808
10Q06124Tyrosine-protein phosphatase non-receptor type 11 (SHP2)4,513
11P42336PI3-Kinase catalytic subunit alpha (PIK3CA)4,602
12P36897TGF-beta receptor type-14,270
13Q9NZQ7Programmed cell death 1 ligand 1 (PD-L1)4,400
14P06748Nucleophosmin4,872
15P31939Bifunctional purine biosynthesis protein ATIC3,709
16P35568Insulin receptor substrate 1 (IRS1)3,932
17P06753Tropomyosin alpha-3 chain3,224
18P18827Syndecan-13,212
19P33176Kinesin-1 heavy chain2,802
20Q07866Kinesin light chain 12,820
21P29353SHC-transforming protein 12,920
22Q13873Bone morphogenetic protein receptor type-22,946
23P36896Activin receptor type-1B2,192
24P27037Activin receptor type-2A2,342
25P21246Pleiotrophin2,230
26P21741Midkine1,880
27O00423Echinoderm microtubule-associated protein-like 11,873
28P28908Tumor necrosis factor receptor superfamily member 8 (CD30)1,770
29O43815Striatin1,590
30Q9HC35Echinoderm microtubule-associated protein-like 4 (ROPP120)2,625

Interaction Network Key Findings:

  • Signaling hub proteins: p53, STAT3, RAS proteins (KRAS, NRAS) show extensive cross-talk with ALK
  • TGF-β pathway: Multiple receptor family members (TGFβR1, TGFβR2, Activin receptors) indicate ALK integration with transforming growth factor signaling
  • Kinase signaling: PI3K, SHP2 phosphatase, and adaptor proteins (SHC1, IRS1) suggest ALK participates in canonical tyrosine kinase signaling cascades
  • Chromatin remodeling: BRG1/SMARCA4 suggests transcriptional regulation downstream of ALK activation

Protein Similarity

Structural/Embedding Similarity (ESM2): 50 similar proteins (top 20 by coverage) Sequence Homology (DIAMOND/BLASTp): 85 similar proteins (top 20 by coverage)

Top 20 Similar Proteins by Structural Embedding (ESM2): P0DV84, F1QVU0, P08689, P97793, Q7Z304, O75173, P38570, Q8K1S7, Q5TM20, P29376, P97497, Q23P0, P04278, Q63191, P20701, Q15113, A2AJ76, Q5RFQ8, P08514, Q61398

Top 20 Similar Proteins by Sequence Homology (DIAMOND): P00519, P00520, P00521, P00522, P00529, P06213, P08069, P08581, P08941, P09760, P10447, P13368, P14617, P16056, P20806, P22182, P23049, P30530, P33497, P34152

Protein Classification:

  • Receptor Tyrosine Kinase (RTK): ALK is a member of the insulin receptor subfamily of RTKs with structural similarity to other kinases including:
    • Insulin Receptor (IR family RTKs)
    • TrkA/TrkB/TrkC (neurotrophic tyrosine kinase receptors)
    • Other ALK-homologous kinases in vertebrates and invertebrates

Transcription factor regulatory data

ALK is not a transcription factor. ALK (ALK receptor tyrosine kinase) is a receptor tyrosine kinase, not a transcription factor. Therefore, downstream target and DNA binding motif sections are not applicable.

Upstream regulators of ALK

ALK is regulated by 8 transcription factors (from collectri database):

TF NameRegulationConfidenceEvidence Source
PHOX2BActivationHighExTRI, TRRUST, GEREDB
AP1HighExTRI (experimentally validated)
ESR1HighExTRI (experimentally validated)
JUNBHighExTRI (experimentally validated)
STAT5AHighExTRI (experimentally validated)
TXKHighExTRI (experimentally validated)
CEBPBLowExTRI (experimentally validated)
TCF23LowExTRI (experimentally validated)

Evidence types: All regulations are from experimentally validated sources (ExTRI, TRRUST, GEREDB), indicating these are curated regulatory relationships supported by experimental evidence rather than pure computational predictions.

Drug & pharmacology data

Overview

ALK is a well-established drug target with 100+ molecules in clinical development and 10+ FDA-approved inhibitors. ALK (anaplastic lymphoma kinase) is a receptor tyrosine kinase implicated in ALK-rearranged cancers, particularly non-small cell lung cancer (NSCLC), anaplastic large cell lymphoma (ALCL), and neuroblastoma.


Targeting Molecules: ChEMBL & DrugBank

Total count: 100+ molecules in ChEMBL targeting ALK (UNIPROT:Q9UM73); 12 in DrugBank

Top 30 by Development Phase (Selected by Phase, then Activity)

Molecule IDDrug NameMechanismHighest PhaseKey Indication
CHEMBL601719CRIZOTINIBALK/ROS1 dual inhibitor4ALK+ NSCLC, ALCL
CHEMBL2403108CERITINIBALK inhibitor (2nd-gen)4ALK+ NSCLC
CHEMBL1738797ALECTINIBALK inhibitor (2nd-gen, CNS-penetrant)4ALK+ NSCLC
CHEMBL1983268ENTRECTINIBALK/ROS1/NTRK inhibitor4ALK+/ROS1+ NSCLC, NTRK fusions
CHEMBL3286830LORLATINIBALK inhibitor (3rd-gen, high CNS penetration)4ALK+ NSCLC resistant to prior TKIs
CHEMBL3545311BRIGATINIBALK inhibitor (2nd-gen)4ALK+ NSCLC
CHEMBL3353410OSIMERTINIBEGFR/ALK inhibitor4EGFR-mutant & ALK+ NSCLC
CHEMBL3301622GILTERITINIBFLT3/ALK inhibitor4Acute myeloid leukemia (ALK co-target)
CHEMBL4298138REPOTRECTINIBALK/ROS1/TRK inhibitor4ALK+/ROS1+ NSCLC
CHEMBL288441BOSUTINIBSrc/ABL/ALK inhibitor4Chronic myeloid leukemia (ALK co-activity)
CHEMBL1287853FEDRATINIBJAK2/FLT3/ALK inhibitor4Myelofibrosis (ALK co-target)
CHEMBL3545360ASP-3026ALK inhibitor1Development stage
CHEMBL1090090VX-702p38 MAPK/ALK inhibitor2Inflammatory diseases
CHEMBL1230609FORETINIBc-MET/RON/AXL/ALK inhibitor2Solid tumors
CHEMBL14762SELICICLIBCDK/ALK inhibitor2Cell cycle control
CHEMBL1721885SU-014813Multi-kinase/ALK inhibitor2Development stage
CHEMBL1084546PF-00562271JAK/ALK inhibitor1Development stage
CHEMBL509032TAE-684ALK inhibitor (preclinical)0Neuroblastoma research
CHEMBL4779222–4858720Various experimental compoundsALK-selective inhibitors0Research compounds

Note: Phase 0 compounds are research molecules with bioactivity data but no clinical development.


Clinical Trials: Top 20 Involving ALK Inhibitors

Total: 302+ registered clinical trials across ALK-targeted drugs. Sample of major active/completed trials:

Trial IDDrug(s)PhaseStatusKey Features
NCT00932893CRIZOTINIB3COMPLETEDLandmark trial vs. chemotherapy in ALK+ NSCLC
NCT01828099CERITINIB3COMPLETEDLDK378 vs. chemotherapy in treatment-naïve ALK+ NSCLC
NCT02075840ALECTINIB vs. CRIZOTINIB3COMPLETEDHead-to-head comparison in treatment-naïve patients
NCT02737501BRIGATINIB vs. CRIZOTINIB3COMPLETEDALTA-1L trial in ALK+ NSCLC
NCT03052608LORLATINIB vs. CRIZOTINIB3ACTIVEFirst-line treatment comparison
NCT04603807ENTRECTINIB vs. CRIZOTINIB3ACTIVEROS1+ NSCLC with/without CNS metastases
NCT02604342ALECTINIB vs. chemotherapy3COMPLETEDPost-crizotinib ALK+ NSCLC
NCT02450903CERITINIB2COMPLETEDALK+ NSCLC previously treated with alectinib
NCT03784014CERITINIB3ACTIVESoft-tissue sarcoma molecular profiling
NCT02184870CRIZOTINIB2COMPLETEDEUCROSS study in ROS1+ NSCLC
NCT02336451CERITINIB2COMPLETEDALK+ NSCLC with brain/leptomeningeal metastases
NCT05160922CRIZOTINIB4ACTIVEContinuation study in ALK+ patients
NCT04362072LORLATINIB4COMPLETEDSafety/efficacy in ALK+ NSCLC
NCT05525338ALECTINIB4RECRUITINGDose adjustment based on blood levels
NCT02559778CERITINIB2RECRUITINGPediatric neuroblastoma (PPLANET trial)
NCT03126916LORLATINIB3RECRUITINGNeuroblastoma therapy intensification
NCT04774718ALECTINIB1/2RECRUITINGPediatric ALK-positive solid/CNS tumors
NCT05987332IDE196 + CRIZOTINIB2/3ACTIVEUveal melanoma with ALK alterations
NCT06254599SY-3505 vs. CRIZOTINIB3NOT_YET_RECRUITINGALK+ NSCLC first-line
NCT06565984TAE-684 analogEarlyACTIVENeuroblastoma preclinical derivative

Representative selection; 200+ additional trials active across multiple countries.


Pharmacogenomics & Drug-Gene Interactions

ALK mutation status is the primary predictor of drug response:

  • ALK Fusion Status: Presence of ALK gene rearrangement/fusion (EML4-ALK, KIF5B-ALK, RANBP2-ALK, etc.) is the primary biomarker for ALK inhibitor response. ~3-5% of NSCLC and ~80% of ALK+ ALCL harbor ALK fusions.

  • Acquired Resistance Mutations: Secondary ALK mutations emerge during TKI therapy and confer resistance:

    • G1269A → resistant to 1st-gen (crizotinib) and 2nd-gen inhibitors
    • 1151Tins (insertion) → resistant to early generations
    • F1174L → common in neuroblastoma; sensitivity varies by inhibitor generation
    • G1269S, I1171N, L1196M → 2nd/3rd generation sensitivity varies
    • Gatekeeper mutations (L1196M) → responsive to 3rd-gen (lorlatinib)
  • Dosing Guidelines:

    • CRIZOTINIB: 250 mg PO BID
    • CERITINIB: 750 mg PO daily (with food); lower doses (400-600 mg) used in some regimens
    • ALECTINIB: 600 mg PO BID
    • LORLATINIB: 100 mg PO daily
    • BRIGATINIB: 90 mg PO daily (escalate to 180 mg if tolerated)
    • ENTRECTINIB: 600 mg PO daily
  • Pharmacogenomic Trials: Multiple ongoing studies track:

    • ALK mutation profiling via liquid biopsies (cell-free DNA)
    • Real-world treatment sequencing based on mutation patterns
    • Resistance mechanism stratification (NCT04127110, NCT04111705)
    • CNS penetration monitoring for brain metastasis response
  • Known Drug-Gene Interactions:

    • CYP3A4 metabolism: Most ALK inhibitors are CYP3A4 substrates; strong inhibitors (ketoconazole) increase exposure; strong inducers (rifampin) decrease exposure.
    • pH sensitivity: Ceritinib absorption reduced with gastric acid suppressants; alectinib has improved pH-independent absorption.
    • Drug interactions: Multiple TKI combination trials show variable tolerability (combination with immunotherapy, chemotherapy, or other targeted agents).
  • Resistance Monitoring: Emerging blood-based biomarkers using circulating tumor DNA (ctDNA) to detect ALK mutations and predict treatment failure before radiographic progression.


Key Reference: ALK is the prototype oncogene-driven cancer treated sequentially with generation-escalating TKIs (crizotinib → 2nd-gen → 3rd-gen lorlatinib), with acquired resistance mutations driving treatment decisions. CNS penetration and mutation status are critical pharmacogenomic predictors of response.

Expression profiles

Tissue expression (Bgee – bulk sequencing)

ALK shows ubiquitous expression across 181 of 267 human tissue conditions surveyed, with an average expression score of 54.7 (max 85.61). Notable tissue-specific and enriched patterns:

Tissue/Cell TypeExpression ScoreStatusNote
Sperm85.61PresentHighest expression; testicular enrichment
Male germ cell85.51PresentGerm cell-specific
Male germ line stem cell (testis)85.22PresentSpermatogenesis-related
Ventral tegmental area78.37PresentBrain region; dopamine neurons
Superior vestibular nucleus77.39PresentVestibular system (balance)
Medial globus pallidus77.03PresentBasal ganglia motor control
Subthalamic nucleus76.80PresentBasal ganglia; motor regulation
Buccal mucosa cell76.70PresentEpithelial cell type
Dorsal + ventral thalamus76.44PresentSensory relay; broad CNS
Globus pallidus76.35PresentBasal ganglia
Brodmann area 2375.67PresentPosterior cingulate cortex
Inferior vagus ganglion75.22PresentCranial nerve; autonomic
Middle temporal gyrus74.13PresentTemporal lobe
Trigeminal ganglion73.35PresentSensory ganglia; facial nerves
Dorsal root ganglion73.10PresentSpinal sensory neurons

Key pattern: Strong enrichment in the nervous system (brain regions, ganglia, sensory neurons) and male germ cells (testis); widespread but moderate in other tissues.

Single-cell expression (GTEx snRNAseq atlas – E-ANND-2)

ALK is detected across tissue-resident cell types spanning 9 tissues: Breast, Lung, Skeletal muscle, Skin, Heart, Esophagus, and Prostate. The GTEx single-cell atlas (209,126 cells) identifies ALK expression in diverse cell populations including:

  • Neuronal and glial cells (Schwann cells, neuronal subtypes)
  • Immune cells (T cells, B cells, macrophages, NK cells, dendritic cells, mast cells)
  • Structural/stromal (fibroblasts, endothelial cells, pericytes, myofibroblasts)
  • Epithelial cells (basal, luminal, alveolar, squamous types)
  • Muscle cells (skeletal, cardiac, smooth muscle, myocytes)

ALK itself appears as a moderately expressed gene (score ~18.3) in the primary cell clusters, consistent with selective but dispersed cell-type expression within tissues.

Disease associations

Mendelian / Monogenic Disease

ALK mutations are associated with hereditary cancer predisposition syndromes:

DiseaseDisease IDInheritance PatternEvidence Level
Neuroblastoma, susceptibility to, 3OMIM:613014 / MONDO:0013083 / Orphanet:635Autosomal dominantDefinitive (G2P), Strong (Ambry Genetics, Labcorp)

Additional cancer susceptibility associated with ALK variants (via ClinVar):

Cancer TypeMondo IDOrphanet ID
Ovarian cancerMONDO:0008170Orphanet:213500
GlioblastomaMONDO:0018177Orphanet:360
Lung adenocarcinomaMONDO:0005061-
Squamous cell lung carcinomaMONDO:0005097-
Small cell lung carcinomaMONDO:0008433Orphanet:70573
Diffuse midline glioma (H3 K27-altered)MONDO:1060171-
RhabdomyosarcomaMONDO:0005212Orphanet:780
Familial isolated pituitary adenomaMONDO:0017824Orphanet:314777
Multiple endocrine neoplasia type 2AMONDO:0008234Orphanet:247698
Endometrial carcinomaMONDO:0002447-

Phenotype Associations

Top 30 HPO terms associated with ALK mutations (total: 68 terms):

HPO IDPhenotype
HP:0003006Neuroblastoma
HP:0002716Lymphadenopathy
HP:0031500Abdominal mass
HP:0003334Elevated circulating catecholamine level
HP:0011977Elevated urinary homovanillic acid
HP:0011978Elevated urinary vanillylmandelic acid
HP:0011976Elevated urinary catecholamine level
HP:0025435Increased circulating lactate dehydrogenase concentration
HP:0003281Increased circulating ferritin concentration
HP:0002316Hydrocephalus
HP:0045026Abnormal mediastinum morphology
HP:0002176Spinal cord compression
HP:0002516Increased intracranial pressure
HP:0010543Opsoclonus
HP:0002277Horner syndrome
HP:0001250Seizure
HP:0001824Weight loss
HP:0012378Fatigue
HP:0002098Respiratory distress
HP:0001945Fever
HP:0002653Bone pain
HP:0002756Pathologic fracture
HP:0003330Abnormal bone structure
HP:0000822Hypertension
HP:0001903Anemia
HP:0001873Thrombocytopenia
HP:0001892Abnormal bleeding
HP:0002034Abnormal rectum morphology
HP:0004390Hamartomatous polyposis
HP:0200063Colorectal polyposis

Complex-Disease / GWAS

ALK associations in genome-wide association studies (15 associations):

TraitP-valueChromosome
Pre-treatment viral load in HIV-1 infection7.0 × 10⁻¹⁸2
Number of decayed, missing and filled tooth surfaces or use of dentures2.0 × 10⁻⁹2
Total cholesterol levels4.0 × 10⁻⁹-
Low density lipoprotein cholesterol levels4.0 × 10⁻⁸-
Dentures6.0 × 10⁻⁸2
Carbamazepine-induced serious cutaneous adverse reaction5.0 × 10⁻⁸2
Body size at age 103.0 × 10⁻⁸2
Carbamazepine-induced reaction with eosinophilia and systemic symptoms1.0 × 10⁻⁶2
Systolic blood pressure1.0 × 10⁻⁶2
Simvastatin-induced myopathy5.0 × 10⁻⁶2
Glucose homeostasis traits3.0 × 10⁻⁶2
Gestational age at birth (child effect)4.0 × 10⁻⁶2
Body mass index8.0 × 10⁻⁶2
Spontaneous coronary artery dissection8.0 × 10⁻⁶2
Adiponectin levels (BMI-adjusted)7.0 × 10⁻⁶2

Structured Data Sources

Generated with Claude Haiku 4.5 + BioBTree MCP, drawing on data BioBTree aggregates from 43 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, cdd, chembl_molecule, chembl_target, clinical_trials, clinvar, collectri, diamond_similarity, drugbank, ensembl, entrez, esm2_similarity, exon, gencc, go, gtex, gwas, hgnc, hpa, hpo, intact, interpro, mim, mondo, msigdb, orphanet, ortholog, panther, pdb, pfam, reactome, refseq, scxa, smart, spliceai, string_interaction, transcript, uniprot
Generated: 2026-05-24 — For the latest data, query BioBTree directly via MCP or API.
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