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Related Concept Videos

Adrenergic Agonists: Chemistry and Structure-Activity Relationship01:16

Adrenergic Agonists: Chemistry and Structure-Activity Relationship

Adrenergic agonists' structure-activity relationship (SAR) determines their selectivity and efficacy. These agonists comprise a phenylethylamine moiety with an aromatic ring and an ethylamine side chain.
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of the aromatic...
Transducer Mechanism: Nuclear Receptors01:31

Transducer Mechanism: Nuclear Receptors

Nuclear receptors, or NRs, are unique transcription factors that regulate gene transcription and affect the cellular pathways involved in reproduction, development, or metabolism. Their ability to be stimulated by small lipophilic ligands and control vital cellular processes makes them ideal drug targets. Nearly 10-15% of currently prescribed drugs target these receptors.
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of cells.
Two...
Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists01:23

Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists

Prostacyclin receptor agonists are a class of therapeutic agents integral to managing pulmonary arterial hypertension (PAH). These drugs operate by mimicking the action of prostaglandin I2, or PGI2, a naturally occurring compound in the body.
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:29

Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

Indirect-acting cholinergic agonists are agents that interact with the acetylcholinesterase enzyme in the synaptic cleft, preventing the breakdown of acetylcholine into choline and acetate. Consequently, the concentration of acetylcholine in the synaptic cleft increases. These agonists can be classified into reversible and irreversible inhibitors based on their duration of action.
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:22

Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

Cholinergic agonists or cholinomimetics mimic the action of acetylcholine to stimulate the parasympathetic nervous system. They are categorized into direct-acting and indirect-acting agents. The direct-acting cholinergic drugs induce the parasympathetic response by directly binding to the muscarinic or nicotine receptors. In comparison, the indirect-acting cholinergic drugs prevent acetylcholine hydrolysis, indirectly contributing to the extended parasympathetic response.
The direct-acting...

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Structure-Guided Design and Development of Novel Cyclophilin A Inhibitors and Ganoderiol-F Derivatives: An In-Silico Approach
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Selective, potent PPARgamma agonists with cyclopentenone core structure.

M Paz Otero1, Efrén Pérez Santín, Fátima Rodríguez-Barrios

  • 1Departamento de Química Orgánica, Universidade de Vigo, 36310 Vigo, Spain.

Bioorganic & Medicinal Chemistry Letters
|March 12, 2009
PubMed
Summary

Researchers synthesized new PPARgamma ligand analogues. Analogues 18 and 20 selectively activated PPARgamma, while others showed altered subtype selectivity and PPARalpha affinity.

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Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers
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Structure-Guided Design and Development of Novel Cyclophilin A Inhibitors and Ganoderiol-F Derivatives: An In-Silico Approach
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Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers
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Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers

Published on: September 19, 2022

Area of Science:

  • Medicinal Chemistry
  • Molecular Pharmacology

Background:

  • Peroxisome proliferator-activated receptors (PPARs) are nuclear receptors regulating gene expression.
  • PPARgamma is a key target for metabolic and inflammatory diseases.
  • 15-deoxy-Delta(12,14)-PGJ(2) is a known PPARgamma ligand, but its analogues require further investigation.

Purpose of the Study:

  • To synthesize novel analogues of the PPARgamma ligand 15-deoxy-Delta(12,14)-PGJ(2).
  • To evaluate the subtype selectivity and binding affinity of these new compounds for PPARgamma and PPARalpha.

Main Methods:

  • Synthesis of cyclopentenone core structures via Piancatelli rearrangement.
  • Functionalization of the core structure to create diverse analogues.
  • Transient transactivation assays to assess PPAR subtype activity.

Main Results:

  • Analogues 18 and 20 demonstrated selective nanomolar agonism of PPARgamma.
  • Introduction of an alkynyl chain at the C3 position diminished PPARgamma selectivity.
  • The cis-configured derivative (23) exhibited increased affinity for PPARalpha.

Conclusions:

  • Novel PPARgamma ligand analogues were successfully synthesized.
  • Specific structural modifications can confer PPARgamma subtype selectivity.
  • Further research may lead to targeted therapeutics for PPAR-mediated conditions.