Related Experiment Video
Updated: Sep 3, 2026

Mapping the Cellular Distribution of an Optogenetic Protein Using a Light-Stimulation Grid
Published on: January 26, 2024
Soluble guanylate cyclase stimulators and activators: Chemistry, biology, and therapeutic advances
Zeping Zuo1, Haoran Yang1, Qipu Feng2
1Laboratory of Cardiac Structure and Function, Institute of Cardiovascular Diseases, Department of Cardiology, West China Hospital, Sichuan University, Chengdu, PR China.
Abstract:
The discovery of soluble guanylate cyclase (sGC) stimulators and activators has provided invaluable tools for elucidating nitric oxide (NO)-sGC signaling and has opened up novel therapeutic opportunities for cardiovascular diseases and beyond. In recent years, sGC modulators have garnered widespread attention as promising agents for diseases such as pulmonary hypertension, heart failure, chronic kidney disease, and diabetic retinopathy-with sGC stimulators and sGC activators emerging as key research focuses in this field. Although first-in-class sGC stimulators (e.g., riociguat, vericiguat) and activators (e.g., cinaciguat) have advanced into clinical use or development, most subsequent candidates continue to be refined to optimize efficacy, safety, and target selectivity. This review provides a comprehensive and systematic exploration of sGC stimulators and sGC activators in the context of disease therapy. Specifically, these small molecules are classified and elaborated based on their mechanisms of action, structural characteristics, and development trajectories; for each category, the binding modes, structural features, and pharmacological activities of representative compounds are analyzed in detail, while their inherent advantages and limitations are critically evaluated. Collectively, this review offers valuable insights and guidance for the future research and development of safer, more effective, and more precisely targeted sGC modulators.
More Related Videos
09:39Drug-induced Sensitization of Adenylyl Cyclase: Assay Streamlining and Miniaturization for Small Molecule and siRNA Screening Applications
Published on: January 27, 2014
07:41A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
Related Concept Videos
GPCRs Regulate Adenylyl Cylase Activity
Two...
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
GTPases and their Regulation
Large G-proteins, also known...
G Protein-coupled Receptors
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
G Protein-coupled Receptors
Activation and Inactivation of G Proteins