Protein / target
Voltage-dependent R-type calcium channel subunit alpha-1E
Protein at a glance
Biological role
Voltage-gated monoatomic cation channel
Strongest disease association
Genetic developmental and epileptic encephalopathy
Therapeutic position
Established drug target
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function overview
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells.
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Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells (PubMed:30343943). They are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1E gives rise to R-type calcium currents. R-type calcium channels belong to the 'high-voltage activated' (HVA) group and are blocked by nickel. They are however insensitive to dihydropyridines (DHP). Calcium channels containing alpha-1E subunit could be involved in the modulation of firing patterns of neurons which is important for information processing
Subcellular location
Domains and Gene Ontology detail (11)Hide
Domains & features
Gene Ontology
- Cneuronal cell body
- Cplasma membrane
- Csynapse
- Cvoltage-gated calcium channel complex
- Fcalcium ion binding
- Fhigh voltage-gated calcium channel activity
- Fvoltage-gated calcium channel activity
- Fvoltage-gated monoatomic cation channel activity
- Pcalcium ion import across plasma membrane
- Pchemical synaptic transmission
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
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Synaptic signalling
- ·synapse
- ·chemical synaptic transmission
- ·Presynaptic depolarization and calcium channel opening
Ion channel gating
- ·voltage-gated monoatomic cation channel activity
Cell migration
- ·Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitab…
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Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.
Interaction neighbourhood
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.
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.
Approved medicines with mapped indications
Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.
7 medicines meet Open Targets' target-level approved-medicine definition; the 2 shown here are those on this page with a canonical approved disease indication in the graph. Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.
Drugs targeting this protein
How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.
Voltage-gated calcium channel modulator
Indicated for Epilepsy, Neuralgia, Postherpetic, Restless Legs Syndrome, Seizures
Voltage-gated calcium channel modulator
Indicated for Anxiety Disorders, Epilepsy, Fibromyalgia, Neuralgia
ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.
Translational evidence
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 CACNA1E
Gene-level evidence surfaced through the gene CACNA1Ethat 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.
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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.
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Drug development
10 compounds recorded · 7 approved · 2 in clinical development · 1 earlier-stage
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Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.
Tractability
Small molecules — Strong
Antibodies — Emerging
Protein degraders — Emerging
View underlying tractability evidence (9)Hide
Raw Open Targets tractability assessment buckets, by modality.
Clinical trials
Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.
View all trials (26)Hide
ClinicalTrials.gov via the drug-target graph.
What's happening now
Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for 2 drugs that target this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.
- Label change
Label change: GABAPENTIN (ANDA217995)
- Label change
Label change: GABAPENTIN (ANDA203934)
- Label change
Label change: PREGABALIN (ANDA211687)
- Regulatory approval
Approval: GABAPENTIN (ANDA203611)
- Regulatory approval
Approval: PREGABALIN (ANDA219593)
- Safety communication
Drug Safety Update: Pregabalin (Lyrica): findings of safety study on risks during pregnancy
- Safety communication
Drug Safety Update: Pregabalin (Lyrica): reports of severe respiratory depression
- Safety communication
Drug Safety Update: Gabapentin (Neurontin): risk of severe respiratory depression
- New publicationPrevention and management of chemotherapy-induced peripheral neuropathy in survivors of adult cancers: American Society of Clinical Oncology clinical practice guideline.
- New publicationA proof-of-concept randomized controlled study of gabapentin: effects on cannabis use, withdrawal and executive function deficits in cannabis-dependent adults.
- New publicationCerebrospinal fluid neurotransmitter changes during the perioperative period in patients undergoing total knee replacement: a randomized trial.
- New publicationAn enhanced bunionectomy model as a potential tool for early decision-making in the development of new analgesics.
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.