PDGFRB

Platelet-derived growth factor receptor beta

Score: 0.629 Price: $0.63 Medium Druggability Status: active Wiki: PDGFRB

🧠 Neurodegeneration

HYPOTHESES

2

PAPERS

44

KG EDGES

326

DEBATES

1

3D Protein Structure

🧬 PDGFRB — PDB 3MJG Click to expand

Experimental structure from RCSB PDB | Powered by Mol*

Druggability & Clinical Context

Druggability

Medium

Score: 0.50

Clinical Stage

Approved

Target Class

Kinase

Safety

0.60

Druggability Analysis

Drug Development1.00

Structural Tractability0.70

Target Class0.85

Safety Profile0.60

Key Metrics

PDB Structures:

2

Known Drugs:

3

Approved:

3

In Clinical Trials:

0

Drug Pipeline (3 compounds)

3 Approved

Druggability Rationale: PDGFRB is highly druggable (0.90 score) as a receptor tyrosine kinase with an ATP-binding pocket amenable to small molecule inhibition, demonstrated by three FDA-approved kinase inhibitors (imatinib, dasatinib, sunitinib) already targeting this protein. High-resolution crystal structures (1.5 Å) and AlphaFold models provide excellent structural guidance for rational drug design and optimization.

Mechanism: Small molecule inhibitor of receptor tyrosine kinase activity

Drug Pipeline (3 compounds)

3 Approved

Known Drugs:

Imatinib (approved) — cancer

Dasatinib (approved) — cancer

Sunitinib (approved) — cancer

Structural Data:

PDB (2) ✓AlphaFold ✓Cryo-EM —

UniProt: E5RII0

🧬 3D Protein Structure

🧬 PDGFRB — PDB 3MJG Click to expand interactive 3D viewer

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

Selectivity & Safety Considerations

PDGFRB shares significant homology with PDGFRA and other receptor tyrosine kinases, presenting selectivity challenges; existing approved drugs show variable selectivity profiles, with dasatinib demonstrating broader kinase inhibition than imatinib. Achieving selective PDGFRB inhibition while minimizing off-target effects on related kinases remains a key optimization consideration.

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 (8)

Relevant trials from ClinicalTrials.gov

Active

0

Completed

8

Total Enrollment

967

By Phase

PHASE2: 7 · PHASE3: 1

Chronic Myelogenous Leukemia (CML) - Follow on: Study of BMS-354825 in Subjects With CML Completed

PHASE3 NCT00123474 n=724

Myeloid Leukemia, Chronic, Chronic-Phase

Interventions: dasatinib, dasatinib, dasatinib

Sponsor: Bristol-Myers Squibb | Started: 2005-07

Therapy of Early Chronic Phase CML With Gleevec Completed

PHASE2 NCT00048672 n=50

Leukemia, Myeloid, Chronic-Phase

Interventions: Gleevec

Sponsor: M.D. Anderson Cancer Center | Started: 2001-03

Imatinib Mesylate in Treating Patients With Liver Metastasis From a Gastrointestinal Stromal Tumor Completed

PHASE2 NCT00764595 n=5

Gastrointestinal Stromal Tumor, Metastatic Cancer

Interventions: imatinib mesylate

Sponsor: Translational Research Center for Medical Innovation, Kobe, | Started: 2008-10

Safety and Efficacy of Pegylated IFN-alpha 2B Added to Dasatinib in Newly Diagnosed Chronic Phase Myeloid Leukemia Completed

PHASE2 NCT01725204 n=40

Leukemia, Myeloid, Chronic-Phase

Interventions: Dasatinib + PegIFN

Sponsor: Norwegian University of Science and Technology | Started: 2012-09

Study Tests The Safety And Effectiveness Of SU011248 In Patients With Non-Small Cell Lung Cancer Having Brain Metastases Completed

PHASE2 NCT00372775 n=66

Non-Small Cell Lung Cancer

Interventions: Sunitinib

Sponsor: Pfizer | Started: 2007-03

Combination of Recombinant Human IL-21 (rIL-21) and Sunitinib in Stage IV Renal Cell Carcinoma Patients Completed

PHASE2 NCT00617253 n=9

Cancer, Renal Cell Carcinoma

Interventions: recombinant interleukin-21, sunitinib, recombinant interleukin-21

Sponsor: Novo Nordisk A/S | Started: 2007-07-12

Sunitinib Malate Before and After Surgery in Treating Patients With Previously Untreated Metastatic Kidney Cancer Completed

PHASE2 NCT01024205 n=43

Kidney Cancer

Interventions: sunitinib malate, laboratory biomarker analysis, adjuvant therapy

Sponsor: Barts and the London School of Medicine and Dentistry | Started: 2007-08

Sunitinib in Treating Patients With Kidney Cancer That Cannot Be Removed by Surgery Completed

PHASE2 NCT00459979 n=30

Kidney Cancer

Interventions: sunitinib malate, conventional surgery

Sponsor: Case Comprehensive Cancer Center | Started: 2007-03

Linked Hypotheses (4)

Pericyte Contractility Reset via Selective PDGFR-β Agonism0.684

Pericyte-First Sequential Biomarker Cascade — Soluble PDGFR-β as Sentinel Event in Pre-Symptomatic A0.662

Vascular mural cell degeneration precedes and exacerbates parenchymal pathology0.661

Elevated Circulating sPDGFRβ Reflects Early Pericyte Loss Preceding Neurodegeneration0.600

Linked Experiments (0)

No linked experiments

Scoring Dimensions

Knowledge Graph (20)

co discussed (18)

AQP1→PDGFRBKCNK2→PDGFRBGJA1→PDGFRBHCRTR2→PDGFRBLOXL1-4→PDGFRB

▸ Show 13 more

HCRTR1→PDGFRBAQP4→PDGFRBLOX→PDGFRBSDC1→PDGFRBFOXP3→PDGFRBTNFA→PDGFRBPPARGC1A→PDGFRBPRKAA1→PDGFRBNR3C1→PDGFRBDRD2→PDGFRBCHR2→PDGFRBCLOCK→PDGFRBCRH→PDGFRB

interacts with (2)

PDGFRB→ANGPT1ANGPT1→PDGFRB

Debate History (1)

Should PDGFRB (Platelet-derived growth factor receptor beta) be prioritized as a2026-04-21