Elucidation of the active|type structure of the LPA receptor involved ...

Elucidation of the active-type structure of the LPA receptor involved ...

Publication details ... G protein-coupled receptors (GPCRs) exist on the membrane and change to their active conformation upon binding to agonists ...

Structure of the active Gi-coupled human lysophosphatidic acid ...

LPA1 is associated with various diseases such as cancer, inflammation, and neuropathic pain, and thus is a pathologically important receptor ...

Structural mechanisms of potent lysophosphatidic acid receptor 1 ...

In addition, our structure show that the ethyl group of CpY directly pushes W2716.48 to fix the active conformation. Endogenous LPA lacks these ...

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

LPA1 shares ∼50–60% amino acid sequence identity with LPA2 and LPA3. While no complete crystal structures have been reported for any LPA receptors to date, ...

Elucidating the binding mechanism of LPA species and analogs in ...

According to their amino acid sequence identity, LPA receptors may be divided into two subtypes. One subtype consists of members of the endothelial cell ...

development of agonists and antagonists for LPA and S1P receptors

Previous studies on lysophosphatidic acid (LPA) and sphingosine 1-phosphate (S1P) using various approaches have shown that both the ...

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

The LPA-induced vascular leakage model is a validated model of target involvement for the LPA-LPA1 receptor axis. Knockdown of the LPA1 receptor ...

Non-Edg family LPA receptors: the cutting edge of LPA research

In spite of its simple structure, LPA exserts various biological functions and is involved in processes such as cell growth, differentiation ...

LPA 4 receptor - IUPHAR/BPS Guide to PHARMACOLOGY

Lysophosphatidic acid receptors LPA4 and LPA6 differentially promote lymphocyte transmigration across high endothelial venules in lymph nodes. Species: Mouse.

LPA Receptors: Subtypes and Biological Actions - Scripps Research

Higher adiposity in Lpar1−/− compared to wild type ... receptor P2Y5 and its ligand LPA are involved in maintenance of human hair growth.

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

LPA1 shares ⵑ50–60% amino acid sequence identity with LPA2 and LPA3. While no com- plete crystal structures have been reported for any LPA receptors to date, ...

Lysophosphatidic acid (LPA) receptors of the EDG family are ...

We examined the structure–activity relationship of cloned lysophosphatidic acid (LPA) receptors (endothelial cell differentiation gene (EDG) ...

Lysophosphatidic Acid and Its Role in Reproduction

LPA induces proliferation and mitogenic signaling of prostate cancer cells, and a novel LPA receptor isoform has been recognized in healthy prostate tissues.

Novel Antagonist of the Type 2 Lysophosphatidic Acid Receptor ...

New potent and selective LPA2 antagonists could enable the validation of this receptor as a target for the treatment of SCI and might represent ...

Lysophospholipid (LPA) receptors | G protein-coupled receptors

for mice (Mouse Genome Informatics Database, MGI) to reflect species and receptor function of their corresponding proteins. The crystal structure of LPA1 [1-2, ...

Structural formulas of LPA, alkyl-LPA, cPA,and rosiglitazone. LPA is...

Alkyl-LPA is an alkyl-ether analog of LPA. Alkyl-LPA shows a higher potency than LPA at the intracellular LPA receptor PPARγ. cPA is a naturally occurring acyl ...

Lateral access mechanism of LPA receptor probed by molecular ...

This led to the proposal of the “lateral access model,” in which its lipophilic ligand directly enters the binding pocket through the gap structure at the ...

Autotaxin facilitates selective LPA receptor signaling - Cell Press

LPA1 accepts its LPA ligand from the extracellular space (water phase), whereas LPA6 is thought to receive LPA by lateral diffusion, following ...

Role of lysophosphatidic acid and its receptors in the kidney

The protein form of the LPA receptors (LPA1-6) are categorized as class A rhodopsin-like G protein-coupled receptors (GPCRs) and are divided into two primary ...

Lysophosphatidic Acid and Ion Channels as Molecular Mediators of ...

While some of the actions of LPA include modulation of signaling pathways associated to its specific receptors, other include a direct ...