LOX

Lysyl oxidase

Score: 0.593 Price: $0.59 Low Druggability Status: active Wiki: LOX
🧠 Neurodegeneration
HYPOTHESES
11
PAPERS
26
KG EDGES
774
DEBATES
1

3D Protein Structure

🧬 LOX — PDB 5SOR Click to expand

Experimental structure from RCSB PDB | Powered by Mol*

Druggability & Clinical Context

Druggability
Low
Score: 0.43
Clinical Stage
Phase II
Target Class
Enzyme
Safety
0.50
Druggability Analysis
Drug Development0.30
Structural Tractability0.70
Target Class0.85
Safety Profile0.50
Key Metrics
PDB Structures:
3
Known Drugs:
1
Approved:
0
In Clinical Trials:
0
Drug Pipeline (1 compounds)
Druggability Rationale: LOX (lysyl oxidase) represents a moderately promising neurodegeneration drug target with medium druggability, primarily due to its critical role in extracellular matrix remodeling and crosslinking. The availability of structural data and existing small molecule inhibition strategies like simtuzumab suggest potential therapeutic approaches, though significant additional validation would be required to establish neurodegeneration-specific efficacy. Structural insights from PDB entries and AlphaFold predictions provide a foundation for rational drug design targeting its enzymatic active site.
Mechanism: Small molecule inhibition of lysyl oxidase enzymatic activity
Drug Pipeline (1 compounds)
Known Drugs:
Simtuzumab (Clinical) — Fibrotic diseases
Structural Data:
PDB (3) ✓AlphaFold ✓Cryo-EM —
4G324G334RPE
UniProt: B7ZAJ4

🧬 3D Protein Structure

🧬 LOX — PDB 5SOR Click to expand interactive 3D viewer

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

Selectivity & Safety Considerations

LOX shares structural homology with the copper-dependent amine oxidase family (LOX-like proteins: LOXL1-4), presenting significant isoform selectivity challenges for small molecule inhibitors. Off-target inhibition of monoamine oxidases (MAO-A/B) and other oxidative enzymes must be carefully monitored, particularly in CNS applications where neurochemical balance is critical.

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 (6)

Relevant trials from ClinicalTrials.gov

Active
0
Completed
3
Total Enrollment
1,074
By Phase
PHASE2: 6
Pilot Study of Simtuzumab in the Treatment of Liver Fibrosis Completed
PHASE2 NCT01452308 n=20
Liver Fibrosis
Interventions: Simtuzumab
Sponsor: Gilead Sciences | Started: 2011-11
Safety, Tolerability, and Efficacy of GS-4997 Alone or in Combination With Simtuzumab (SIM) in Adults With Nonalcoholic Completed
PHASE2 NCT02466516 n=72
Non-Alcoholic Steatohepatitis (NASH)
Interventions: SEL, SIM
Sponsor: Gilead Sciences | Started: 2015-06-08
Simtuzumab (GS-6624) in the Prevention of Progression of Liver Fibrosis in Adults With Primary Sclerosing Cholangitis (P Completed
PHASE2 NCT01672853 n=235
Primary Sclerosing Cholangitis (PSC)
Interventions: Simtuzumab, Placebo
Sponsor: Gilead Sciences | Started: 2013-03-04
Efficacy and Safety of Simtuzumab (SIM) With FOLFIRI as Second Line Treatment in Colorectal Adenocarcinoma Terminated
PHASE2 NCT01479465 n=266
Colorectal Cancer
Interventions: Simtuzumab, Placebo to match SIM, Leucovorin
Sponsor: Gilead Sciences | Started: 2011-12
Safety and Efficacy of Simtuzumab (SIM, GS-6624) in Adults With Advanced Liver Fibrosis But Not Cirrhosis Secondary to N Terminated
PHASE2 NCT01672866 n=222
Liver Fibrosis Due to NASH
Interventions: Placebo, SIM
Sponsor: Gilead Sciences | Started: 2012-12-05
Simtuzumab (SIM, GS-6624) in the Treatment of Cirrhosis Due to NASH Terminated
PHASE2 NCT01672879 n=259
Liver Fibrosis Due to NASH
Interventions: Placebo, SIM
Sponsor: Gilead Sciences | Started: 2012-10-29

Linked Hypotheses (0)

No linked hypotheses

Linked Experiments (0)

No linked experiments

Scoring Dimensions

Portfolio 0.63 (25%) Druggability 0.43 (20%) Evidence 0.72 (20%) Safety 0.50 (15%) Competitive 0.40 (10%) Connectivity 0.90 (10%) 0.593 composite

Knowledge Graph (20)

associated with (1)

LOXneurodegeneration

co discussed (9)

AQP1LOXKCNK2LOXGJA1LOXHCRTR2LOXLOXL1-4LOX
▸ Show 4 more
HCRTR1LOXAQP4LOXLOXSDC1LOXPDGFRB

inhibits (2)

P2RY12LOXMTORLOX

interacts with (8)

LOXLOXL1-4LOXL1-4LOXACTBLOXAPOA1LOXULK1LOX
▸ Show 3 more
ATG5LOXEIF4EBP1LOXLC3LOX

Debate History (1)

Should LOX (Lysyl oxidase) be prioritized as a therapeutic target for neurodegen2026-04-21