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Protein / target

Caspase-1

Encoded byCASP1P29466Homo sapiensSwiss-Prot
Clinical-stage
Therapeutic maturity
3
Clinical candidates
1
Clinical trials
Small-molecule tractable
Druggability
Advanced Clinical

Protein at a glance

Biological role

Cysteine-type endopeptidase

Strongest disease association

Severe Acute Respiratory Syndrome

Via encoding gene CASP1 · Pathway evidence · score 0.37

Therapeutic position

Clinically advancing target

Small molecules

Research activity

Emerging research

2 papers · latest 2024

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

Thiol protease involved in a variety of inflammatory processes by proteolytically cleaving other proteins, such as the precursors of the inflammatory cytokines interleukin-1 beta (IL1B) and interleukin 18 (IL18) as well as the pyroptosis inducer Gasdermin-D (GSDMD), into active mature peptides.

View complete UniProt function annotation

Thiol protease involved in a variety of inflammatory processes by proteolytically cleaving other proteins, such as the precursors of the inflammatory cytokines interleukin-1 beta (IL1B) and interleukin 18 (IL18) as well as the pyroptosis inducer Gasdermin-D (GSDMD), into active mature peptides (PubMed:15326478, PubMed:15498465, PubMed:1574116, PubMed:26375003, PubMed:32051255, PubMed:37993714, PubMed:7876192, PubMed:9334240). Plays a key role in cell immunity as an inflammatory response initiator: once activated through formation of an inflammasome complex, it initiates a pro-inflammatory response through the cleavage of the two inflammatory cytokines IL1B and IL18, releasing the mature cytokines which are involved in a variety of inflammatory processes (PubMed:15326478, PubMed:15498465, PubMed:1574116, PubMed:32051255, PubMed:7876192). Cleaves a tetrapeptide after an Asp residue at position P1 (PubMed:15498465, PubMed:1574116, PubMed:7876192). Also initiates pyroptosis, a programmed lytic cell death pathway, through cleavage of GSDMD (PubMed:26375003). In contrast to cleavage of interleukin IL1B, recognition and cleavage of GSDMD is not strictly dependent on the consensus cleavage site but depends on an exosite interface on CASP1 that recognizes and binds the Gasdermin-D, C-terminal (GSDMD-CT) part (PubMed:32051255, PubMed:32109412, PubMed:32553275). Cleaves and activates CASP7 in response to bacterial infection, promoting plasma membrane repair (PubMed:22464733). Upon inflammasome activation, during DNA virus infection but not RNA virus challenge, controls antiviral immunity through the cleavage of CGAS, rendering it inactive (PubMed:28314590). In apoptotic cells, cleaves SPHK2 which is released from cells and remains enzymatically active extracellularly (PubMed:20197547)

Subcellular location

CytoplasmCell membrane
Domains and Gene Ontology detail (44)

Domains & features

CARD

Gene Ontology

  • CAIM2 inflammasome complex
  • Ccytoplasm
  • Ccytosol
  • CIPAF inflammasome complex
  • Cmicrotubule
  • CNLRP1 inflammasome complex
  • CNLRP3 inflammasome complex
  • Cnucleolus
  • Cplasma membrane
  • Cprotease inhibitor complex
  • Cprotein-containing complex
  • FCARD domain binding

404 aa · 45 kDa · 5 isoforms

Biological roles

Reactome v97

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

Immune signallingUniProt · GO · ReactomeProteolysisUniProt · GOApoptosis & cell deathGO · Reactome
View supporting evidence

Immune signalling

  • ·Thiol protease involved in a variety of inflammatory processes by proteolytically cleavi…
  • ·cytokine binding
  • ·cytokine precursor processing
  • ·positive regulation of inflammatory response

Proteolysis

  • ·Thiol protease involved in a variety of inflammatory processes by proteolytically cleavi…
  • ·protease inhibitor complex
  • ·cysteine-type endopeptidase activity
  • ·endopeptidase activity

Apoptosis & cell death

  • ·cysteine-type endopeptidase activator activity involved in apoptotic process
  • ·apoptotic process
  • ·positive regulation of apoptotic process
  • ·TP53 Regulates Transcription of Caspase Activators and Caspases
View underlying pathways (11)

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.

PYCARDMEFVAIM2NLRC4NLRP3IL1BCASP8GSDMDNLRP6NLRP1CASP1

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

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.

belnacasan
Narrow target profilePhase 2Inhibitor

Caspase-1 inhibitor

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

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 CASP1

Gene-level evidence surfaced through the gene CASP1 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.

Severe Acute Respiratory Syndrome
0.25Preliminary

Pathway evidence dominant · Open Targets 0.37 · no direct causal or clinical evidence

COVID-19
0.21Preliminary

Literature evidence dominant · Open Targets 0.11

Infections
0.14Preliminary

Literature evidence dominant · Open Targets 0.12 · no direct causal or clinical evidence

Neoplasms
0.14Preliminary

Literature evidence dominant · Open Targets 0.11 · no direct causal or clinical evidence

Major depressive disorder
0.13Preliminary

Literature evidence dominant · Open Targets 0.11 · no direct causal or clinical evidence

View evidence synthesis (5)
Severe Acute Respiratory SyndromePreliminary
0.25
agreement 0.070.42
Pathway98%Literature2%

Open Targets aggregate 0.37 · 2 independent evidence families · no direct causal or clinical evidence

COVID-19Preliminary
0.21
agreement 0.050.36
Literature53%Clinical47%

Open Targets aggregate 0.11 · 2 independent evidence families

InfectionsPreliminary
0.14
agreement 0.000.42
Literature100%

Open Targets aggregate 0.12 · 1 independent evidence family · no direct causal or clinical evidence

NeoplasmsPreliminary
0.14
agreement 0.000.41
Literature100%

Open Targets aggregate 0.11 · 1 independent evidence family · no direct causal or clinical evidence

Major depressive disorderPreliminary
0.13
agreement 0.000.40
Literature100%

Open Targets aggregate 0.11 · 1 independent evidence family · 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
Severe Acute Respiratory Syndrome0.37
Infections0.12
Neoplasms0.11
COVID-190.11
Major depressive disorder0.11
Carcinoma, Hepatocellular0.11
Diabetes Mellitus, Type 20.10

Drug development

3 compounds recorded · 3 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: these count different sets and are not a subset relation.

View all recorded compounds (3)
BELNACASANPhase 2
EMRICASANPhase 2
NIVOCASANPhase 2

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

Advanced Clinical and Structure with Ligand support this modality.

AntibodiesEmerging

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

Protein degradersEmerging

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

View underlying tractability evidence (11)
SM · Advanced ClinicalSM · Structure with LigandSM · High-Quality LigandSM · Med-Quality PocketSM · Druggable FamilyAB · UniProt loc high confAB · GO CC med confPR · UniProt UbiquitinationPR · Database UbiquitinationPR · Half-life DataPR · Small Molecule Binder

Raw Open Targets tractability assessment buckets, by modality.

Safety-related annotations

regulation of catalytic activityToxCast

Terms indexed against this target in Open Targets' safety data, with their datasource. These are annotations, not causal claims: the direction of effect (whether activation or inhibition is implicated), species and evidence strength are not captured here, so an entry does not mean that modulating this target is known to cause that condition.

Clinical trials

1

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.

ClinicalTrials.gov via the drug-target graph.

What's happening now

1

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. New publication2019-10-25
    Pharmacological Inhibitors of the NLRP3 Inflammasome.

    Frontiers in immunology · 2019 · 518 citations · Europe PMC · via belnacasan

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.

Research activity

2 papers · to 2024

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

Most cited

Recent

Europe PMC papers linked directly to this protein.