DGAT1

Diacylglycerol O-Acyltransferase 1

Score: 0.583 Price: $0.58 Low Druggability Status: active Wiki: DGAT1

🧠 Neurodegeneration

HYPOTHESES

PAPERS

KG EDGES

DEBATES

3D Protein Structure

🧬 DGAT1 — PDB 6VP0 Click to expand

Experimental structure from RCSB PDB | Powered by Mol*

Druggability & Clinical Context

Druggability

Low

Score: 0.41

Clinical Stage

Phase III

Target Class

Enzyme

Safety

0.50

Druggability Analysis

Drug Development0.45

Structural Tractability0.70

Target Class0.85

Safety Profile0.50

Key Metrics

PDB Structures:

Known Drugs:

Approved:

In Clinical Trials:

Drug Pipeline (1 compounds)

Therapeutic Areas:

Metabolic Disease Oncology Rare Disease

Druggability Rationale: DGAT1 represents a high-potential druggable target with structural tractability, evidenced by multiple PDB structures and an AlphaFold prediction, suggesting amenability to small molecule inhibition. The existing clinical trial of Pradigastat indicates proof-of-concept for pharmacological modulation, though its specific neurodegeneration applications remain underexplored. Structural resolution at 3.0Å provides sufficient molecular detail for rational drug design strategies targeting triglyceride metabolism in neurological contexts.

Mechanism: Small molecule inhibitor of triglyceride synthesis enzyme

Drug Pipeline (1 compounds)

Known Drugs:

Pradigastat (clinical_trial) — obesity/metabolic disorders

Structural Data:

PDB (9) ✓AlphaFold ✓Cryo-EM ✓

6VP0 6VYI 6VZ1 8ESM 8ETM+4 more

UniProt: Q3KQR6

Binding Pocket Analysis:

Catalytic residues, substrate-binding cleft

🧬 3D Protein Structure

🧬 DGAT1 — PDB 6VP0 Click to expand interactive 3D viewer

Experimental structure from RCSB PDB | Powered by Mol* | Rotate: click+drag | Zoom: scroll

Selectivity & Safety Considerations

Selectivity within the enzyme family is important to avoid mechanism-based toxicity. Isoform-selective inhibitors generally have superior therapeutic windows.