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Related Concept Videos

Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors01:28

Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors

Phosphodiesterase 5 (PDE5) inhibitors are potent enzymes that function to hydrolyze cyclic nucleotides to their corresponding 5' monophosphates. Their unique biochemical properties have been applied in treating Pulmonary Arterial Hypertension (PAH).
Among the PDE5 inhibitors, sildenafil (Revatio) stands out as a competitive and selective inhibitor. It operates by elevating cellular levels of cGMP and augmenting signaling through the cGMP-PKG pathway, promoting vasodilation. Upon oral...
Dipeptidyl Peptidase 4 Inhibitors01:23

Dipeptidyl Peptidase 4 Inhibitors

Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a significant...
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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...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Phosphodiester Linkages01:01

Phosphodiester Linkages

Overview
Phosphodiester bond forms when a phosphoric acid molecule (H3PO4) links with two hydroxyl groups (–OH) of two other molecules, forming two ester bonds. Two water molecules are released in this process. The phosphodiester bond is commonly found in nucleic acids (DNA and RNA) and plays a critical role in their structure and function.
Phosphodiester Bonds Link Nucleotides Together
DNA and RNA are polynucleotides or long chains of nucleotides that are linked together. A nucleotide is...
Phosphoinositides and PIPs01:42

Phosphoinositides and PIPs

Phosphoinositides are a group of phospholipids containing a glycerol backbone with two fatty acid chains and a phosphate attached to a myoinositol sugar ring. The inositol head group extends into the cytoplasm, where it is modified by adding phosphate groups to form phosphatidylinositol phosphates or PIPs.
Different phosphoinositides are synthesized and recruited on the cytosolic face of the plasma membrane. The localization of specific phosphoinositides concentrated in separate membrane...

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Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries
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Phosphodiesterase-5 inhibitors.

Barbara A Cockrill1, Aaron B Waxman

  • 1Pulmonary Vascular Disease Program, Brigham and Women's Hospital, Harvard Medical School, 75 Francis Street, Boston, MA, 02115, USA, bcockrill@partners.org.

Handbook of Experimental Pharmacology
|October 5, 2013
PubMed
Summary

Phosphodiesterase-5 (PDE-5) inhibitors enhance nitric oxide (NO) signaling, improving pulmonary hypertension treatment. These drugs target the cyclic guanylate monophosphate pathway, benefiting patients with pulmonary arterial hypertension (PAH).

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Area of Science:

  • Cardiovascular Medicine
  • Pharmacology
  • Pulmonary Circulation Physiology

Background:

  • Nitric oxide (NO) signaling is crucial for regulating vascular tone and remodeling in the pulmonary circulation.
  • The guanylate cyclase/cyclic guanylate monophosphate (cGMP) pathway is the primary mediator of NO signaling.
  • This pathway is vital for normal pulmonary vasculature regulation and a key therapeutic target for pulmonary hypertension (PH).

Purpose of the Study:

  • To discuss the mechanisms of NO signaling in the vasculature.
  • To describe the characteristics of approved phosphodiesterase-5 (PDE-5) inhibitors for PH treatment.
  • To review clinical data on the efficacy of PDE-5 inhibitors in patients with PH.

Main Methods:

  • Review of scientific literature on NO signaling and cGMP metabolism in the pulmonary vasculature.
  • Analysis of data from large randomized placebo-controlled trials of PDE-5 inhibitors in adult patients with pulmonary arterial hypertension (PAH).
  • Discussion of the role of PDE-5 in cGMP degradation and its impact on pulmonary vascular smooth muscle tone.

Main Results:

  • PDE-5 inhibitors demonstrate significant improvements in exercise capacity, hemodynamics, and quality of life in adult PAH patients.
  • Inhibition of PDE-5 impacts pulmonary vasculature smooth muscle tone by modulating cGMP levels.
  • Clinical trials confirm the therapeutic benefits of PDE-5 inhibitors for PAH management.

Conclusions:

  • PDE-5 inhibitors are effective therapeutic agents for pulmonary hypertension, particularly PAH.
  • Targeting the NO-cGMP pathway via PDE-5 inhibition offers a viable strategy for improving clinical outcomes in PH.
  • Further review of phosphodiesterase inhibitors in PH treatment is warranted.