Publication

A SPECIFIC TEMPLATE-ASSEMBLED PEPTIDIC AGONIST FOR THE ANGIOTENSIN-II RECEPTOR SUBTYPE-2 (AT2) AND ITS EFFECT ON INFERIOR OLIVARY NEURONS

1995
Journal Articles

Abstract

We synthesized a molecule composed of two angiotensin II 4-8 pentapeptide fragments attached to a carrier molecule (TA), according to the template-assembled synthetic proteins concept. This molecule was investigated for receptor binding on angiotensin type-1 and type-2 receptors (AT1 and AT2) and its biological activity was determined by iontophoretic experiments on neurones of the inferior olive (ION) that express only AT2 receptors, TA binds exclusively to the AT2 receptor and mediates an agonistic angiotensin-II effect on the ION. TA is the first agonist available to study the direct stimulation of AT2 receptors.

Official source

https://infoscience.epfl.ch/entities/publication/f29892b1-76fa-47b1-9674-17027f70ea24

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1995
Journal Articles

Abstract

Official source

https://infoscience.epfl.ch/entities/publication/f29892b1-76fa-47b1-9674-17027f70ea24

About this result

Related concepts (32)

Agonist

An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. From the Greek αγωνιστής (agōnistēs), contestant; champion; rival < αγων (agōn), contest, combat; exertion, struggle < αγω (agō), I lead, lead towards, conduct; drive Receptors can be activated by either endogenous agonists (such as hormones and neurotransmitters) or exogenous agonists (such as drugs), resulting in a biological response.

Receptor (biochemistry)

In biochemistry and pharmacology, receptors are chemical structures, composed of protein, that receive and transduce signals that may be integrated into biological systems. These signals are typically chemical messengers which bind to a receptor and produce physiological responses such as change in the electrical activity of a cell. For example, GABA, an inhibitory neurotransmitter inhibits electrical activity of neurons by binding to GABA_A receptors.

Inverse agonist

In pharmacology, an inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist. A neutral antagonist has no activity in the absence of an agonist or inverse agonist but can block the activity of either; they are in fact sometimes called blockers (examples include alpha blockers, beta blockers, and calcium channel blockers). Inverse agonists have opposite actions to those of agonists but the effects of both of these can be blocked by antagonists.

Related publications (3)

A SPECIFIC TEMPLATE-ASSEMBLED PEPTIDIC AGONIST FOR THE ANGIOTENSIN-II RECEPTOR SUBTYPE-2 (AT2) AND ITS EFFECT ON INFERIOR OLIVARY NEURONS

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Brain Stimulation and its Role in Neurological Diseases

Peptide ligands stabilized by small molecules

Study of ligand-receptor interactions by fluorescence correlation spectroscopy with different fluorophores: Evidence that the homopentameric 5-hydroxytryptamine type 3(As) receptor binds only one ligand