Target intelligence / Profile preview

Multiple endogenous receptors for platelet-derived growth factors and cytokines

Molecular classification
Receptor, Growth factor receptor, Cytokine receptor, Tyrosine kinase receptor (partial)
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Overview

Multiple endogenous receptors for platelet-derived growth factors and cytokines is a target designation used to describe the broad pharmacological activity of anti-fibrotic agents like pirfenidone (Source: ChEMBL [22]). This profile encompasses receptors for platelet-derived growth factor (PDGF) and several key cytokines, including transforming growth factor-beta (TGF-beta), tumor necrosis factor-alpha (TNF-alpha), and various interleukins such as IL-1beta and IL-6 (Source: PubChem [21]). By modulating these multiple pathways, drugs targeting this complex inhibit fibroblast proliferation and the synthesis of extracellular matrix proteins like collagen (Source: Wikipedia [25]). This multi-target mechanism is particularly relevant in the treatment of idiopathic pulmonary fibrosis (IPF), where it helps to mitigate both the inflammatory and fibrotic processes that drive disease progression (Source: IUPHAR [24]). The inhibition of these receptors leads to a reduction in the production of pro-fibrotic mediators and a slowing of the decline in respiratory function. Beyond IPF, this target profile is explored in other fibrotic conditions and certain types of cancer where growth factor and cytokine signaling are dysregulated.

Other names
Pirfenidone targetsPDGF and cytokine receptor complexAnti-fibrotic target groupGrowth factor and cytokine receptor signaling complex
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Mechanism of action

Inhibition of growth factor and cytokine signaling pathways, leading to reduced fibroblast activation, decreased collagen deposition, and suppression of inflammatory mediator production.

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Biological functions

Signal transductionCell proliferationInflammationFibrosisImmune responseCollagen synthesis
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Disease associations

Idiopathic pulmonary fibrosisInflammationCancerLiver fibrosisRenal fibrosisScleroderma
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Safety considerations

PhotosensitivityGastrointestinal distress (nausea, dyspepsia)Hepatotoxicity (elevated liver enzymes)DizzinessFatigue
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Interacting drugs

Pirfenidone
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Biomarkers

Forced Vital Capacity (FVC)Transforming growth factor-beta (TGF-beta) levelsTumor necrosis factor-alpha (TNF-alpha) levelsHigh-resolution computed tomography (HRCT) scores

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