Back to discover

Protein / target

Leucine-rich repeat serine/threonine-protein kinase 2

Encoded byLRRK2Q5S007Homo sapiensSwiss-Prot
Small-molecule tractable
Druggability
Structure with Ligand
1
Research papers

Protein at a glance

Biological role

Signaling receptor complex adaptor

Strongest disease association

Parkinson's Disease

Via encoding gene LRRK2 · Genetic evidence · score 0.80

Research activity

Emerging research

1 papers · latest 2013

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 overview

Serine/threonine-protein kinase which phosphorylates a broad range of proteins involved in multiple processes such as neuronal plasticity, innate immunity, autophagy, and vesicle trafficking.

View complete UniProt function annotation

Serine/threonine-protein kinase which phosphorylates a broad range of proteins involved in multiple processes such as neuronal plasticity, innate immunity, autophagy, and vesicle trafficking (PubMed:17114044, PubMed:20949042, PubMed:21850687, PubMed:22012985, PubMed:23395371, PubMed:24687852, PubMed:25201882, PubMed:26014385, PubMed:26824392, PubMed:27830463, PubMed:28720718, PubMed:29125462, PubMed:29127255, PubMed:29212815, PubMed:30398148, PubMed:30635421). Is a key regulator of RAB GTPases by regulating the GTP/GDP exchange and interaction partners of RABs through phosphorylation (PubMed:26824392, PubMed:28720718, PubMed:29125462, PubMed:29127255, PubMed:29212815, PubMed:30398148, PubMed:30635421). Phosphorylates RAB3A, RAB3B, RAB3C, RAB3D, RAB5A, RAB5B, RAB5C, RAB8A, RAB8B, RAB10, RAB12, RAB29, RAB35, and RAB43 (PubMed:23395371, PubMed:26824392, PubMed:28720718, PubMed:29125462, PubMed:29127255, PubMed:29212815, PubMed:30398148, PubMed:30635421, PubMed:38127736). Regulates the RAB3IP-catalyzed GDP/GTP exchange for RAB8A through the phosphorylation of 'Thr-72' on RAB8A (PubMed:26824392). Inhibits the interaction between RAB8A and GDI1 and/or GDI2 by phosphorylating 'Thr-72' on RAB8A (PubMed:26824392). Regulates primary ciliogenesis through phosphorylation of RAB8A and RAB10, which promotes SHH signaling in the brain (PubMed:29125462, PubMed:30398148). Together with RAB29, plays a role in the retrograde trafficking pathway for recycling proteins, such as mannose-6-phosphate receptor (M6PR), between lysosomes and the Golgi apparatus in a retromer-dependent manner (PubMed:23395371). Regulates neuronal process morphology in the intact central nervous system (CNS) (PubMed:17114044). Plays a role in synaptic vesicle trafficking (PubMed:24687852). Plays an important role in recruiting SEC16A to endoplasmic reticulum exit sites (ERES) and in regulating ER to Golgi vesicle-mediated transport and ERES organization (PubMed:25201882). Positively regulates autophagy through a calcium-dependent activation of the CaMKK/AMPK signaling pathway (PubMed:22012985). The process involves activation of nicotinic acid adenine dinucleotide phosphate (NAADP) receptors, increase in lysosomal pH, and calcium release from lysosomes (PubMed:22012985). Phosphorylates PRDX3 (PubMed:21850687). By phosphorylating APP on 'Thr-743', which promotes the production and the nuclear translocation of the APP intracellular domain (AICD), regulates dopaminergic neuron apoptosis (PubMed:28720718). Acts as a positive regulator of innate immunity by mediating phosphorylation of RIPK2 downstream of NOD1 and NOD2, thereby enhancing RIPK2 activation (PubMed:27830463). Independent of its kinase activity, inhibits the proteasomal degradation of MAPT, thus promoting MAPT oligomerization and secretion (PubMed:26014385). In addition, has GTPase activity via its Roc domain which regulates LRRK2 kinase activity (PubMed:18230735, PubMed:26824392, PubMed:28720718, PubMed:29125462, PubMed:29212815). Recruited by RAB29/RAB7L1 to overloaded lysosomes where it phosphorylates and stabilizes RAB8A and RAB10 which promote lysosomal content release and suppress lysosomal enlargement through the EHBP1 and EHBP1L1 effector proteins (PubMed:30209220, PubMed:38227290)

Subcellular location

Cytoplasmic vesiclePerikaryonGolgi apparatus membraneCell projection, axonCell projection, dendriteEndoplasmic reticulum membraneCytoplasmic vesicle, secretory vesicle, synaptic vesicle membraneEndosomeLysosomeMitochondrion outer membraneCytoplasm, cytoskeletonCytoplasmic vesicle, phagosome
Domains and Gene Ontology detail (160)

Domains & features

RocCORProtein kinase

Gene Ontology

  • Camphisome
  • Cautolysosome
  • Caxon
  • Ccaveola neck
  • Ccytoplasm
  • Ccytoplasmic side of mitochondrial outer membrane
  • Ccytoplasmic vesicle
  • Ccytoskeleton
  • Ccytosol
  • Cdendrite
  • Cdendrite cytoplasm
  • Cendoplasmic reticulum

2527 aa · 286 kDa

Biological roles

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

Excitatory neurotransmissionGOKinase signallingUniProt · GOMetabolic enzyme activityGOMotor controlGO
View supporting evidence

Excitatory neurotransmission

  • ·glutamatergic synapse
  • ·excitatory postsynaptic potential
  • ·negative regulation of excitatory postsynaptic potential
  • ·regulation of synaptic transmission, glutamatergic

Kinase signalling

  • ·Serine/threonine-protein kinase which phosphorylates a broad range of proteins involved…
  • ·GTP-dependent protein kinase activity
  • ·JUN kinase kinase kinase activity
  • ·kinase activity

Metabolic enzyme activity

  • ·GTP metabolic process
  • ·regulation of reactive oxygen species metabolic process

Motor control

  • ·locomotory exploration behavior
  • ·regulation of locomotion

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

Translational evidence

Open Targets 26

Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.

Strongest disease associations · via encoding gene LRRK2

Gene-level evidence surfaced through the gene LRRK2that encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.

Parkinson's Disease
0.86Well supported

Genetic evidence dominant · Open Targets 0.74

Genetic Diseases, Inborn
0.69Moderately supported

Genetic evidence dominant · Open Targets 0.42

Placental abruption
0.56Moderately supported

Genetic evidence dominant · Open Targets 0.34

Alzheimer's Disease
0.40Limited support

Pathway evidence dominant · Open Targets 0.37

Neurodegenerative Diseases
0.32Preliminary

Pathway evidence dominant · Open Targets 0.44 · no direct causal or clinical evidence

View evidence synthesis (5)
Parkinson's DiseaseWell supported
0.86
agreement 0.740.98
Genetic68%Pathway19%Literature13%Genetic literaturedup

Open Targets aggregate 0.74 · 3 independent evidence families · 1 not counted as duplicate

Genetic Diseases, InbornModerately supported
0.69
agreement 0.550.83
Genetic99%Literature1%

Open Targets aggregate 0.42 · 2 independent evidence families

Placental abruptionModerately supported
0.56
agreement 0.450.69
Genetic100%

Open Targets aggregate 0.34 · 1 independent evidence family

Alzheimer's DiseaseLimited support
0.40
agreement 0.280.52
Pathway49%Literature28%Genetic23%

Open Targets aggregate 0.37 · 3 independent evidence families

Neurodegenerative DiseasesPreliminary
0.32
agreement 0.140.50
Pathway84%Literature16%

Open Targets aggregate 0.44 · 2 independent evidence families · no direct causal or clinical evidence

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 per-type scores above show the calculation.

Show all associations
Parkinson's Disease0.74
Neurodegenerative Diseases0.44
Genetic Diseases, Inborn0.42
Alzheimer's Disease0.37
Placental abruption0.34
Multiple Sclerosis0.34

Tractability

Small moleculesEmerging

Feasibility evidence (structure with ligand and high-quality ligand) — no clinical-stage drug of this modality recorded.

AntibodiesEmerging

Feasibility evidence (uniprot loc high conf and go cc high conf) — no clinical-stage drug of this modality recorded.

Protein degradersEmerging

Feasibility evidence (literature and uniprot ubiquitination) — no clinical-stage drug of this modality recorded.

View underlying tractability evidence (10)
SM · Structure with LigandSM · High-Quality LigandSM · Druggable FamilyAB · UniProt loc high confAB · GO CC high confPR · LiteraturePR · UniProt UbiquitinationPR · Database UbiquitinationPR · Half-life DataPR · Small Molecule Binder

Raw Open Targets tractability assessment buckets, by modality.

Research activity

1 papers · to 2013

Papers linked directly to this protein. This is the protein's own literature — descriptor-derived papers are kept separate below.

Most cited

Dias V · Journal of Parkinson's disease · 2013

Recent

The role of oxidative stress in Parkinson's disease.

Dias V · Journal of Parkinson's disease · 2013

Europe PMC papers linked directly to this protein.