First|in|class antifibrotic therapy targeting type 1 lysophosphatidic ...

First-in-class antifibrotic therapy targeting type 1 lysophosphatidic ...

Fibrosis is a normal process for repairing injured tissue. However, aberrant or hyperfibrotic responses result in serious pathologic conditions and ...

First-in-class antifibrotic therapy targeting type 1 lysophosphatidic ...

Fibrosis is a normal process for repairing injured tissue. However, aberrant or hyperfibrotic responses result in serious pathologic ...

A novel, orally active LPA1 receptor antagonist inhibits lung fibrosis ...

... first in class' molecules that treat IPF via blockade of LPA1 receptors. ... The type 1 lysophosphatidic acid receptor is a target for therapy in bone metastases.

Discovery of a Novel Orally Active, Selective LPA Receptor Type 1 ...

Lysophosphatidic acid receptor 1 (LPAR1) antagonists show promise as potentially novel antifibrotic treatments. In a human LPAR1 β-arrestin ...

Illustration of the mechanism of action of selective LPA 1 antagonists

First-in-class Antifibrotic Therapy Targeting Type 1 Lysophosphatidic Acid Receptor ... A new class of drugs antagonizing type 1 lysophosphatidic acid ...

The type 1 lysophosphatidic acid receptor is a target for therapy in ...

Platelet-derived lysophosphatidic acid (LPA) supports the progression of breast and ovarian cancer metastasis to bone.

Lysophosphatidic acid receptor 1 (LPA1) in pulmonary fibrosis fact ...

Idiopathic pulmonary fibrosis (IPF) is the most common type of progressive fibrosing ILD. ... Antifibrotic therapy for idiopathic pulmonary ...

LPA 1 antagonist BMS-986020 changes collagen dynamics and ...

Idiopathic pulmonary fibrosis (IPF) is a debilitating lung disease with limited treatment options. A phase 2 trial (NCT01766817) showed that ...

Lysophosphatidic acid receptor 1 inhibition: a potential treatment ...

This review discusses how novel pharmaceuticals target lysophosphatidic acid signalling in pulmonary fibrosis and summarises clinical trials of these ...

Differential activation mechanisms of lipid GPCRs by ... - Nature

The best studied lysophospholipids are lysophosphatidic acid (LPA) and sphingosine 1-phosphate (S1P). LPA receptor 1 (LPA1) was the first ...

Lysophosphatidic acid-1-receptor targeting agents for fibrosis

The Lysophosphatidic acid (LPA) receptor 1 (LPAR1) pathway has been considered a promising target for anti-fibrotic and anti-inflammatory therapy in adult and ...

LPA receptor signaling: pharmacology, physiology, and ...

... first lysophospholipid receptor, LPA1. This GPCR was previously ... The type 1 lysophosphatidic acid receptor is a target for therapy in bone metastases.

Phase 2 trial design of BMS-986278, a lysophosphatidic acid ...

Treatment with antifibrotic agents can slow, but not halt, disease progression, and treatment ... In a phase 2 trial with a first-generation LPA1 ...

Cellular and Molecular Control of Lipid Metabolism in Idiopathic ...

Studies are now under way on numerous targets for IPF treatment, including autotaxin (ATX) [1], a metabolic enzyme involved in the lysophosphatidic acid (LPA) ...

Translational engagement of lysophosphatidic acid receptor 1 in ...

Despite an increasing number of molecular targeted therapies in clinical testing, effective anti-fibrotic therapies are still not available.

Lysophosphatidic acid signaling through its receptor initiates ...

... target for anti-fibrotic therapies. The profibrotic interactions between ... type 1 diabetic nephropathy. Diabetes Care, 31 (2008), pp. 1177-1182.

LPA1 receptor antag News - LARVOL Sigma

In this first phase 2 study to evaluate antifibrotic treatment in parallel IPF and PPF cohorts, 60-mg admilparant slowed lung function decline and was safe ...

Role of lysophosphatidic acid and its receptors in health and disease

LPA4-mediated vascular network formation increases the efficacy of anti–PD-1 therapy against brain tumors. ... lysophosphatidic acid type 1 ...

Bristol Myers Squibb's Investigational LPA1 Antagonist Reduces the ...

... first-in-class, oral, lysophosphatidic acid receptor 1 (LPA 1 ) antagonist, in patients with idiopathic pulmonary fibrosis. The study showed ...

Destabilization of Lysophosphatidic Acid Receptor 1 Reduces ...

Further, we reveal that a deubiquitination enzyme USP11 stabilizes LPA1 by targeting and deubiquitinating LPA1. To investigate whether destabilization of LPA1 ...