We have described five phosphodiesterase (PDE) isozymes that can be found in cardiac and vascular smooth muscle of animals and humans. Much of the evidence for the role that these isozymes have in the regulation of cellular processes has been generated through, or awaits, the identification of selective and potent PDE inhibitors. While selective inhibitors of the cGMP-inhibitable (cGi)-PDE isozyme have been approved for use in the acute treatment of heart failure, selective inhibitors of the cGMP-PDE have not been extensively explored as potential candidates for the treatment of cardiovascular diseases. More potent selective inhibitors of the cGMP-PDE isozyme are needed to determine whether these pharmacological potentiators of EDRF and ANP will be useful in the therapy of angina, hypertension or heart failure.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1007/978-3-642-72474-9_6 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Explanatory review on DDR inhibitors: their biological activity, synthetic route, and structure-activity relationship.
Mol Divers
January 2025
Integrated Drug Discovery Centre, Department of Pharmaceutical Chemistry, Acharya & BM Reddy College of Pharmacy, Bengaluru, 560107, Karnataka, India.
Discoidin domain receptors (DDR) are categorized under tyrosine kinase receptors (RTKs) and play a crucial role in various etiological conditions such as cancer, fibrosis, atherosclerosis, osteoarthritis, and inflammatory diseases. The structural domain rearrangement of DDR1 and DDR2 involved six domains of interest namely N-terminal DS, DS-like, intracellular juxtamembrane, transmembrane juxtamembrane, extracellular juxtamembrane intracellular kinase domain, and the tail portion contains small C-tail linkage. DDR has not been explored to a wide extent to be declared as a prime target for any particular pathological condition.
View Article and Find Full Text PDFBackground: Sodium-glucose co-transporter-2 (SGLT-2) inhibitors have been added to the mainstay of treatment for chronic heart failure. Recent studies suggest that empagliflozin may also reverse cardiac remodeling in heart failure by reducing N-terminal pro-B-type natriuretic peptide (NT-proBNP) levels. In our study, we wanted to show the decrease in NT-proBNP levels, which is an indicator of poor prognosis in heart failure, and to see if there was a decrease in the rate of renal progression in patients with HF after empagliflozin use.
View Article and Find Full Text PDFCostimulation blockade: the next generation.
Curr Opin Organ Transplant
January 2025
Division of Nephrology, Virginia Commonwealth University, Richmond, Virginia, USA.
Purpose Of The Review: Calcineurin inhibitors (CNIs) are central to immunosuppression in kidney transplantation (KT), improving short-term outcomes but falling short in enhancing long-term outcomes due to cardiovascular, metabolic, and renal complications. Belatacept, an FDA-approved costimulation blocker, offers a less toxic alternative to CNIs but is limited by its intravenous administration and reduced efficacy in high-immunological-risk patients.
Recent Findings: Emerging therapies target more specific pathways to improve efficacy and accessibility.
Structural and Mechanistic Insights into the Main Protease (Mpro) Dimer Interface Destabilization Inhibitor: Unveiling New Therapeutic Avenues against SARS-CoV-2.
Biochemistry
January 2025
Department of Biosciences and Bioengineering, Indian Institute of Technology, Roorkee, Uttarakhand 247667, India.
SARS-CoV-2 variant recurrence has emphasized the imperative prerequisite for effective antivirals. The main protease (Mpro) of SARS-CoV-2 is crucial for viral replication, making it one of the prime and promising antiviral targets. Mpro features several druggable sites, including active sites and allosteric sites near the dimerization interface, that regulate its catalytic activity.
View Article and Find Full Text PDFA study on the pharmacovigilance of various SGLT-2 inhibitors.
Front Med (Lausanne)
January 2025
The Second Clinical College of Guangzhou University of Chinese Medicine, Guangzhou, China.
Background: Sodium-glucose co-transporter two inhibitors (SGLT2is) are widely used in clinical practice due to their proven cardiovascular and renal benefits. However, various adverse drug reactions (ADRs) have been reported. This study aims to systematically update the ADRs associated with SGLT2is and identify the differences among various SGLT2is acovigilance of various SGLT-2 inhibitors.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!