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Protein / target

Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha

Encoded byFNTAP49354Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
1
Approved medicines
Open Targets target-level
View by indication →
26
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

CAAX-protein geranylgeranyltransferase

Strongest disease association

Neurodegenerative Diseases

Via encoding gene FNTA · Pathway evidence · score 0.54

Therapeutic position

Established drug target

Small molecules

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

Essential subunit of both the farnesyltransferase and the geranylgeranyltransferase complex.

View complete UniProt function annotation

Essential subunit of both the farnesyltransferase and the geranylgeranyltransferase complex. Contributes to the transfer of a farnesyl or geranylgeranyl moiety from farnesyl or geranylgeranyl diphosphate to a cysteine at the fourth position from the C-terminus of several proteins having the C-terminal sequence Cys-aliphatic-aliphatic-X. May positively regulate neuromuscular junction development downstream of MUSK via its function in RAC1 prenylation and activation

Domains and Gene Ontology detail (24)

Gene Ontology

  • CCAAX-protein geranylgeranyltransferase complex
  • Ccytoplasm
  • Ccytosol
  • Cmicrotubule associated complex
  • Cplasma membrane
  • Cprotein farnesyltransferase complex
  • Facetyltransferase activator activity
  • Falpha-tubulin binding
  • FCAAX-protein geranylgeranyltransferase activity
  • Fenzyme binding
  • Fmicrotubule binding
  • Fmolecular adaptor activity

379 aa · 44 kDa · 3 isoforms

Biological roles

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

Ion channel gatingGOMetabolic enzyme activityGO
View supporting evidence

Ion channel gating

  • ·skeletal muscle acetylcholine-gated channel clustering

Metabolic enzyme activity

  • ·CAAX-protein geranylgeranyltransferase activity
  • ·protein farnesyltransferase activity
  • ·protein geranylgeranyltransferase activity
  • ·Rab geranylgeranyltransferase activity

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

Approved medicines with mapped indications

1 medicine · 2 areas

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.

Laminopathies1 medicine
Progeria1 medicine

Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.

Drugs targeting this protein

1

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.

lonafarnib
ApprovedInhibitor

Protein farnesyltransferase inhibitor

Indicated for Laminopathies, Progeria

Acts on a complex — shared with FNTB · 1 of 2 recorded protein targets — narrow recorded profile

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

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 FNTA

Gene-level evidence surfaced through the gene FNTA that 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.

Leukemia, Myeloid, Acute
0.41Limited support

Clinical evidence dominant · Open Targets 0.33

Neurodegenerative Diseases
0.35Preliminary

Pathway evidence dominant · Open Targets 0.54 · no direct causal or clinical evidence

View evidence synthesis (2)
Leukemia, Myeloid, AcuteLimited support
0.41
agreement 0.250.56
Clinical99%Literature1%

Open Targets aggregate 0.33 · 2 independent evidence families

Neurodegenerative DiseasesPreliminary
0.35
agreement 0.130.58
Pathway100%

Open Targets aggregate 0.54 · 1 independent evidence family · no direct causal or clinical evidence

This ranking differs from Open Targets' own: re-weighting moves genetically-evidenced diseases above more heavily co-mentioned ones. 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
Neurodegenerative Diseases0.54
Leukemia, Myeloid, Acute0.33

Drug development

2 compounds recorded · 1 approved · 1 in clinical development

Open Targets' development universe — every compound recorded against the target at any stage, not all approved medicines. Distinct from the 1 drug that targets this protein in Forefront's canonical graph (1 with a mapped approved indication, shown above): these count different sets and are not a subset relation.

View all recorded compounds (2)
TIPIFARNIBPhase 3
LONAFARNIBApproval

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 moleculesStrong

Approved Drug and Structure with Ligand support this modality.

AntibodiesEmerging

Feasibility evidence (go cc med conf) — no clinical-stage drug of this modality recorded.

Protein degradersEmerging

Feasibility evidence (database ubiquitination and half-life data) — no clinical-stage drug of this modality recorded.

View underlying tractability evidence (9)
SM · Approved DrugSM · Structure with LigandSM · High-Quality LigandSM · Med-Quality PocketSM · Druggable FamilyAB · GO CC med confPR · Database UbiquitinationPR · Half-life DataPR · Small Molecule Binder

Raw Open Targets tractability assessment buckets, by modality.

Clinical trials

26

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 (22)

COMPLETED · via lonafarnib · NCT02511431

COMPLETED · via lonafarnib · NCT01495585

TERMINATED · via lonafarnib · NCT00773474

ClinicalTrials.gov via the drug-target graph.

What's happening now

2

Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for a drug that targets 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.

  1. Regulatory approval2022-07-18

    Approval: Zokinvy (EMA)

    ema · regulatory · ema · via lonafarnib

  2. New publication2013-06-28
    Neurologic features of Hutchinson-Gilford progeria syndrome after lonafarnib treatment.

    Neurology · 2013 · 38 citations · Europe PMC · via lonafarnib

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.