Protein / target

Amyloid-beta precursor protein

APPP05067Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
3
Approved medicines
23
Clinical trials
Small-molecule tractable
Druggability
Advanced Clinical

Protein at a glance

Biological role

Serine-type endopeptidase inhibitor activity

Primary system

Nervous system

Strongest disease association

Alzheimer disease type 1

Genetic evidence · score 0.95

Therapeutic maturity

Clinically validated target

3 approved medicines against this target

Druggability

Small molecule

Open Targets tractability · Advanced Clinical

Clinical development

3 approved · 10 in clinical development

23 linked trials

Derived from structured UniProt, Open Targets and literature data on this page.

Protein profile

UniProt 2026_02

Canonical identity and biological annotation from UniProt.

Function

Functions as a cell surface receptor and performs physiological functions on the surface of neurons relevant to neurite growth, neuronal adhesion and axonogenesis. Interaction between APP molecules on neighboring cells promotes synaptogenesis (PubMed:25122912). Involved in cell mobility and transcription regulation through protein-protein interactions. Can promote transcription activation through binding to APBB1-KAT5 and inhibits Notch signaling through interaction with Numb. Couples to apoptosis-inducing pathways such as those mediated by G(o) and JIP. Inhibits G(o) alpha ATPase activity (By similarity). Acts as a kinesin I membrane receptor, mediating the axonal transport of beta-secretase and presenilin 1 (By similarity). By acting as a kinesin I membrane receptor, plays a role in axonal anterograde transport of cargo towards synapses in axons (PubMed:17062754, PubMed:23011729). Involved in copper homeostasis/oxidative stress through copper ion reduction. In vitro, copper-metallated APP induces neuronal death directly or is potentiated through Cu(2+)-mediated low-density lipoprotein oxidation. Can regulate neurite outgrowth through binding to components of the extracellular matrix such as heparin and collagen I and IV. The splice isoforms that contain the BPTI domain possess protease inhibitor activity. Induces a AGER-dependent pathway that involves activation of p38 MAPK, resulting in internalization of amyloid-beta peptide and leading to mitochondrial dysfunction in cultured cortical neurons. Provides Cu(2+) ions for GPC1 which are required for release of nitric oxide (NO) and subsequent degradation of the heparan sulfate chains on GPC1

Subcellular location

Cell membraneMembranePerikaryonCell projection, growth coneMembrane, clathrin-coated pitEarly endosomeCytoplasmic vesicleEndoplasmic reticulumGolgi apparatusSecretedCell surfaceNucleusCytoplasm
Domains and Gene Ontology detail (128)

Domains & features

E1BPTI/Kunitz inhibitorE2

Gene Ontology

  • Camyloid-beta complex
  • Castrocyte projection
  • Caxon
  • Ccell surface
  • Cclathrin-coated pit
  • Ccytoplasm
  • Ccytosol
  • Cdendrite
  • Cdendritic shaft
  • Cdendritic spine
  • Cearly endosome
  • Cearly endosome membrane

770 aa · 87 kDa · 11 isoforms

Biological roles

Reactome v97

What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.

Synaptic signallingUniProt · GOTranscriptional regulationUniProt · GOCell adhesionUniProt · GOHaemostasisGO · ReactomeImmune signallingGOApoptosis & cell deathGO
View supporting evidence

Synaptic signalling

  • ·Functions as a cell surface receptor and performs physiological functions on the surface…
  • ·synapse
  • ·modulation of excitatory postsynaptic potential
  • ·positive regulation of synaptic transmission, cholinergic

Transcriptional regulation

  • ·Functions as a cell surface receptor and performs physiological functions on the surface…
  • ·negative regulation of gene expression
  • ·positive regulation of gene expression
  • ·positive regulation of transcription by RNA polymerase II

Cell adhesion

  • ·Functions as a cell surface receptor and performs physiological functions on the surface…
  • ·cell adhesion
  • ·extracellular matrix organization

Haemostasis

  • ·platelet alpha granule lumen
  • ·Platelet degranulation
  • ·Aggregated β-amyloid interacts with fibrinogen

Immune signalling

  • ·astrocyte activation involved in immune response
  • ·positive regulation of inflammatory response
  • ·positive regulation of interleukin-1 beta production
  • ·positive regulation of interleukin-6 production

Apoptosis & cell death

  • ·hippocampal neuron apoptotic process
  • ·regulation of neuron apoptotic process
View underlying pathways (20)

Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.

Interaction neighbourhood

STRING v12.0

Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.

SORL1APBB1APOEBACE1PSEN1TNFRSF…CLUPRNPNAE1APBA2APP

10 strongest partners — larger node and heavier line mean higher confidence

Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.

Drugs targeting this protein

2

Whether each drug engages this protein directly or through a complex, and how many other targets are recorded for it. Direct binders with few recorded targets are listed first.

lecanemab
Narrow target profileApprovedInhibitor

Amyloid-beta A4 protein inhibitor

Appears in clinical studies involving dementia, Cognitive impairment, Alzheimer disease, Alzheimer disease

Direct interaction with this protein · Only this protein recorded as a target

aducanumab
Narrow target profileApprovedBinding agent

Amyloid-beta A4 protein binding agent

Appears in clinical studies involving Alzheimer disease, dementia, Alzheimer disease, Alzheimer disease

Direct interaction with this protein · Only this protein recorded as a target

ChEMBL mechanism, action type and target identity. Open Targets clinical status and indications.

Translational evidence

Open Targets 26

Why this target matters therapeutically — disease associations, drugs in development, tractability and safety, from Open Targets.

Strongest genetic associations

Human genetic evidence — the most direct causal link between this target and a disease.

Alzheimer disease type 10.95

Genetic · overall 0.79

cerebral amyloid angiopathy, APP-related0.87

Genetic · overall 0.75

Alzheimer disease0.87

Genetic · overall 0.81

Hereditary cerebral hemorrhage with amyloidosis, Piedmont type0.78

Genetic literature · overall 0.64

Hereditary cerebral hemorrhage with amyloidosis, Dutch type0.78

Genetic literature · overall 0.64

Highest-confidence therapeutic associations

Diseases where a drug acting on this target has already reached clinical development.

dementia0.90

Clinical · overall 0.68

Highest overall evidence

Remaining associations by Open Targets' aggregated evidence score.

Hereditary cerebral hemorrhage with amyloidosis, Italian type0.64

Genetic literature

Hereditary cerebral hemorrhage with amyloidosis, Iowa type0.64

Genetic literature

Hereditary cerebral hemorrhage with amyloidosis, Arctic type0.64

Genetic literature

Hereditary cerebral hemorrhage with amyloidosis, Flemish type0.64

Genetic literature

Show all associations
Alzheimer disease0.81
Alzheimer disease type 10.79
cerebral amyloid angiopathy, APP-related0.75
dementia0.68
Hereditary cerebral hemorrhage with amyloidosis, Piedmont type0.64
Hereditary cerebral hemorrhage with amyloidosis, Dutch type0.64
Hereditary cerebral hemorrhage with amyloidosis, Italian type0.64
Hereditary cerebral hemorrhage with amyloidosis, Iowa type0.64
Hereditary cerebral hemorrhage with amyloidosis, Arctic type0.64
Hereditary cerebral hemorrhage with amyloidosis, Flemish type0.64

Open Targets ranks 2,010 associations for this target and we store the top 10 by aggregated score. The long tail is largely literature co-mention and RNA-expression evidence, not evidence that this target drives those diseases.

Known drugs · 13 total

LECANEMABApproval

dementia · Cognitive impairment · Alzheimer disease

TRAMIPROSATEPhase 3

Alzheimer disease · Alzheimer disease · glaucoma

DONANEMABApproval

Alzheimer disease · Cognitive impairment · dementia

GANTENERUMABPhase 3

Alzheimer disease · Alzheimer disease · Alzheimer disease

AMILOMOTIDEPhase 2 3

Alzheimer disease · Alzheimer disease

GSK933776Phase 2

age-related macular degeneration · atrophic macular degeneration · Alzheimer disease

ADUCANUMABApproval

Alzheimer disease · dementia · Alzheimer disease

BAPINEUZUMABPhase 3

Alzheimer disease · Alzheimer disease · Alzheimer disease

VALILTRAMIPROSATEPhase 3

Alzheimer disease · Alzheimer disease

CRENEZUMABPhase 3

Alzheimer disease · Alzheimer disease · Alzheimer disease

Tractability

SM · Advanced ClinicalSM · Structure with LigandSM · High-Quality LigandSM · High-Quality PocketSM · Druggable FamilyAB · Approved DrugAB · UniProt loc high confAB · GO CC high confAB · UniProt SigP or TMHMMPR · UniProt UbiquitinationPR · Database UbiquitinationPR · Small Molecule Binder

Clinical trials

23

Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein.

Show remaining trials (17)

ClinicalTrials.gov via the drug-target graph.

Forefront confidence

Synthesis

Our own weighting of the evidence behind each disease association. Human genetics and clinical evidence count for most; literature co-mention counts for little, because two entities sharing an abstract is not evidence that one drives the other.

Alzheimer diseaseWell supported
0.98
agreement 0.881.00
Genetic44%Clinical37%Pathway12%Literature8%

Open Targets aggregate 0.81 · 4 independent evidence families

Alzheimer disease type 1Well supported
0.96
agreement 0.841.00
Genetic82%Animal model15%Literature3%Genetic literaturedup

Open Targets aggregate 0.79 · 3 independent evidence families · 1 not counted as duplicate

cerebral amyloid angiopathy, APP-relatedWell supported
0.90
agreement 0.771.00
Genetic80%Animal model20%Genetic literaturedup

Open Targets aggregate 0.75 · 2 independent evidence families · 1 not counted as duplicate

dementiaWell supported
0.87
agreement 0.760.98
Clinical51%Genetic43%Literature6%Genetic literaturedup

Open Targets aggregate 0.68 · 3 independent evidence families · 1 not counted as duplicate

Hereditary cerebral hemorrhage with amyloidosis, Piedmont typeModerately supported
0.72
agreement 0.580.85
Genetic literature72%Animal model28%Geneticdup

Open Targets aggregate 0.64 · 2 independent evidence families · 1 not counted as duplicate

The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the underlying per-type scores are shown above so the calculation can be checked.

What's happening now

8

Recent activity around this target, drawn from one canonical event stream. Every item is reached through 2 drugs that target this protein, so each event is news about that drug rather than about the protein directly.

  1. Indication expanded2026-07-13

    Indication expansion: LECANEMAB-IRMB (BLA761375)

    fda · regulatory · fda · via lecanemab

  2. Manufacturing update2026-06-15
    Eisai snares government manufacturing grant as it brings Leqembi packaging to UK with $65M expansion

    Fierce Pharma · news · via lecanemab

  3. Regulatory approval2025-08-29

    Approval: LECANEMAB-IRMB (BLA761375)

    fda · regulatory · fda · via lecanemab

  4. Regulatory approval2025-04-15

    Approval: Leqembi (EMA)

    ema · regulatory · ema · via lecanemab

  5. New publication2024-08-23
    Recent advances in Alzheimer's disease: Mechanisms, clinical trials and new drug development strategies.

    Signal transduction and targeted therapy · 2024 · 640 citations · Europe PMC · via aducanumab

  6. New publication2023-01-01
    Lecanemab: Appropriate Use Recommendations.

    The journal of prevention of Alzheimer's disease · 2023 · 626 citations · Europe PMC · via lecanemab

  7. New publication2022-11-29
    Lecanemab in Early Alzheimer's Disease.

    The New England journal of medicine · 2023 · 3,691 citations · Europe PMC · via lecanemab

  8. New publication2022-01-01
    Two Randomized Phase 3 Studies of Aducanumab in Early Alzheimer's Disease.

    The journal of prevention of Alzheimer's disease · 2022 · 1,003 citations · Europe PMC · via aducanumab

Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.