Target intelligence / Profile preview

C-X-C motif chemokine receptor 2, Coagulation factor II thrombin receptor, Matrix metalloproteinase-1, Matrix metalloproteinase-2, Matrix metalloproteinase-3, Vascular cell adhesion molecule 1

Molecular classification
G protein-coupled receptor, Enzyme, Cell adhesion molecule, Metalloprotease
01

Overview

The target name provided is a composite list of six distinct proteins: C-X-C motif chemokine receptor 2 (CXCR2), Coagulation factor II thrombin receptor (F2R/PAR1), Matrix metalloproteinase-1 (MMP1), Matrix metalloproteinase-2 (MMP2), Matrix metalloproteinase-3 (MMP3), and Vascular cell adhesion molecule 1 (VCAM-1). CXCR2 is a G protein-coupled receptor (GPCR) primarily responsible for neutrophil chemotaxis and activation in response to IL-8 (Murphy & Tiffany, 1991 [1]). F2R, also known as Protease-activated receptor 1 (PAR1), is a GPCR that mediates the cellular effects of thrombin, playing a critical role in platelet aggregation and vascular signaling (Vu et al., 1991 [2]). MMP1, MMP2, and MMP3 are members of the matrix metalloproteinase family, which are zinc-dependent enzymes that degrade various components of the extracellular matrix, facilitating tissue remodeling and cell migration (Nagase et al., 2006 [3]). VCAM-1 is a cell surface sialoglycoprotein that mediates the adhesion of leukocytes to the vascular endothelium, a key step in the inflammatory response (Osborn et al., 1989 [4]). Collectively, these proteins are central to the pathophysiology of atherosclerosis, chronic inflammation, and tumor metastasis, where they coordinate leukocyte recruitment and matrix degradation (Libby, 2002 [5]). While individual drugs like Vorapaxar (targeting F2R) and Navarixin (targeting CXCR2) have been developed, this specific combination of proteins is typically analyzed as a panel of inflammatory markers rather than a single therapeutic target (StatPearls, 2023 [6]).

Other names
CXCR2F2RMMP1MMP2MMP3VCAM-1Protease-activated receptor 1 (PAR1)Interstitial collagenase72 kDa type IV collagenaseStromelysin-1Vascular cell adhesion protein 1CD106
02

Mechanism of action

This target set involves multiple mechanisms: antagonism of the CXCR2 and F2R (PAR1) G protein-coupled receptors to inhibit chemotaxis and thrombin signaling; inhibition of the proteolytic activity of MMP1, MMP2, and MMP3 to prevent extracellular matrix degradation; and the blockade of VCAM-1 to prevent leukocyte-endothelial adhesion.

03

Biological functions

InflammationCell adhesionExtracellular matrix degradationSignal transductionChemotaxisPlatelet activationLeukocyte recruitment
04

Disease associations

AtherosclerosisCancerInflammationRheumatoid arthritisCardiovascular diseaseChronic obstructive pulmonary disease (COPD)
05

Safety considerations

Increased risk of major bleeding (F2R inhibition)Neutropenia (CXCR2 inhibition)Musculoskeletal syndrome and joint stiffness (MMP inhibition)Impaired wound healingIncreased susceptibility to infections
06

Interacting drugs

Navarixin

6 more in the full profile.

07

Biomarkers

Soluble VCAM-1 (sVCAM-1)Serum MMP-2 levelsSerum MMP-9 levelsCXCR2 expression on neutrophilsC-reactive protein (CRP)

Beyond the preview

Go deeper on C-X-C motif chemokine receptor 2, Coagulation factor II thrombin receptor, Matrix metalloproteinase-1, Matrix metalloproteinase-2, Matrix metalloproteinase-3, Vascular cell adhesion molecule 1.

Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.

Drug pipeline

Full profile access

Explore the programs pursuing this target and their development progress.

  • Drug candidates
  • Developers
  • Development stage

Clinical trials

Full profile access

Follow the clinical studies evaluating therapies directed at this target.

  • Trial design
  • Status
  • Readouts

Competitive landscape

Full profile access

Compare approaches across drug candidates, modalities, and indications.

  • Programs
  • Modalities
  • Indications

Literature & evidence

Full profile access

Investigate the research and source evidence behind target biology and development.

  • Publications
  • Sources
  • Analysis

Patents

Full profile access

Explore patent activity around therapies and technologies addressing this target.

  • Patents
  • Assignees
  • Technologies

Research & analysis

Full profile access

Connect target biology, drug development, and emerging evidence in your research.

  • Biology
  • Development news
  • Analysis

Bring the full picture into focus.

See how Gosset can support your research on C-X-C motif chemokine receptor 2, Coagulation factor II thrombin receptor, Matrix metalloproteinase-1, Matrix metalloproteinase-2, Matrix metalloproteinase-3, Vascular cell adhesion molecule 1.

Explore the full profile

Gosset Free

Get started with Gosset.

Enter your work email and we’ll be in touch with next steps.

Work email preferred.

Book a call