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Lysophosphatidic acid-1-receptor targeting agents for fibrosis
- Source :
- Expert Opinion on Investigational Drugs, Expert Opinion on Investigational Drugs, Taylor & Francis, 2011, 20 (5), pp.657-67. ⟨10.1517/13543784.2011.566864⟩, Expert Opinion on Investigational Drugs, 2011, 20 (5), pp.657-67. ⟨10.1517/13543784.2011.566864⟩
- Publication Year :
- 2011
- Publisher :
- HAL CCSD, 2011.
-
Abstract
- International audience; INTRODUCTION: The presence of fibrosis is associated with alterations in organ architecture and is responsible for the morbidity of diseases including pneumopathies, systemic sclerosis, liver cirrhosis, chronic cardiovascular diseases, progressive kidney diseases and diabetes. Although a growing number of pro-fibrotic molecules, mediators and other pathways have been reported, there are currently very few antifibrotic molecules being evaluated in clinical trials. AREAS COVERED: Current knowledge about the contribution of lysophosphatidic acid (LPA), a bioactive mediator acting via specific G-protein coupled receptors (LPAR), in the etiology of fibrosis. In a number of organs, fibrosis is associated with increased LPA production as well as with increased expression of some LPAR subtypes (mainly LPA1R). LPAR(-/-) knockout mice and treatment of animal models with specific antagonists clearly demonstrate the contribution of LPA1R subtype to the development of kidney, lung, vascular and dermal fibrosis. The involvement of LPA in liver fibrosis is also strongly suspected but still unproven. EXPERT OPINION: Experiments in animal models clearly demonstrate that LPA1R antagonists have interesting anti-fibrotic potencies. This reveals promising perspectives for the design of new therapeutic approaches to prevent fibrosis-associated diseases. Nevertheless, the number of efficient LPA1R antagonists currently available is still low, and none of them has been used in clinical trials so far.
- Subjects :
- Cirrhosis
MESH: Clinical Trials as Topic
receptor
Bioinformatics
MESH: Lysophospholipids
03 medical and health sciences
chemistry.chemical_compound
0302 clinical medicine
Mediator
Fibrosis
Diabetes mellitus
Lysophosphatidic acid
MESH: Molecular Targeted Therapy
medicine
MESH: Receptors, Lysophosphatidic Acid
Animals
Humans
Pharmacology (medical)
MESH: Animals
Molecular Targeted Therapy
Receptors, Lysophosphatidic Acid
Receptor
030304 developmental biology
Pharmacology
0303 health sciences
Kidney
Clinical Trials as Topic
MESH: Humans
business.industry
fibrosis
antagonist
General Medicine
medicine.disease
3. Good health
medicine.anatomical_structure
chemistry
030220 oncology & carcinogenesis
Immunology
Knockout mouse
MESH: Fibrosis
Lysophospholipids
business
lysophosphatidic acid
Subjects
Details
- Language :
- English
- ISSN :
- 13543784 and 17447658
- Database :
- OpenAIRE
- Journal :
- Expert Opinion on Investigational Drugs, Expert Opinion on Investigational Drugs, Taylor & Francis, 2011, 20 (5), pp.657-67. ⟨10.1517/13543784.2011.566864⟩, Expert Opinion on Investigational Drugs, 2011, 20 (5), pp.657-67. ⟨10.1517/13543784.2011.566864⟩
- Accession number :
- edsair.doi.dedup.....3a36554831b5204ccb8bd1ca3fbf2cb1