DGAT1

Diacylglycerol O-Acyltransferase 1

Score: 0.504 Price: $0.50 Low Druggability Status: active Wiki: DGAT1
🧠 Neurodegeneration
HYPOTHESES
1
PAPERS
29
KG EDGES
72
DEBATES
1

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:
9
Known Drugs:
1
Approved:
0
In Clinical Trials:
0
Drug Pipeline (1 compounds)
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 ✓
6VP06VYI6VZ18ESM8ETM+4 more
UniProt: Q3KQR6

🧬 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.

3D Protein Structure

PDB: Open in RCSB AlphaFold model

Interactive 3D viewer powered by RCSB PDB / Mol*. Use mouse to rotate, scroll to zoom.

Clinical Trials (2)

Relevant trials from ClinicalTrials.gov

Active
0
Completed
1
Total Enrollment
222
By Phase
PHASE2: 2
A Proof of Concept Study of Pradigastat in Patients With Functional Constipation Completed
PHASE2 NCT04620161 n=181
Functional Constipation
Interventions: Pradigastat Tablets 20mg, Pradigastat Tablets 40mg, Pradigastat Tablets 20mg matching Placeb
Sponsor: Anji Pharma | Started: 2020-09-22
Efficacy of LCQ908 on Cardiovascular Risk Terminated
PHASE2 NCT01474434 n=41
Coronary Artery Disease, Hypertriglyceridemia
Interventions: pradigastat (LCQ908), Placebo
Sponsor: Novartis Pharmaceuticals | Started: 2011-12

Linked Hypotheses (1)

Astrocyte-Specific DGAT1 Inhibition to Prevent Lipid Droplet-Induced Neuroinflammation0.515

Linked Experiments (0)

No linked experiments

Scoring Dimensions

Portfolio 0.59 (25%) Druggability 0.41 (20%) Evidence 0.50 (20%) Safety 0.50 (15%) Competitive 0.40 (10%) Connectivity 0.60 (10%) 0.504 composite

Knowledge Graph (20)

activates (4)

GBMDGAT1SOAT1DGAT1DGAT1APOA1DGAT1CD36

co discussed (13)

BMAL1DGAT1HK2DGAT1MIRO1DGAT1P2RY1DGAT1SOAT1DGAT1
▸ Show 8 more
KCNK2DGAT1TET2DGAT1PIEZO1DGAT1P2RX7DGAT1DGAT1C3CLOCKDGAT1PLIN2DGAT1DGAT1G3BP1

inhibits (1)

SOAT1DGAT1

interacts with (2)

DGAT1SOAT1SOAT1DGAT1

Debate History (1)

Should DGAT1 (Diacylglycerol O-Acyltransferase 1) be prioritized as a therapeuti2026-04-22