Journal of Developing Drugs
Open Access

Novel Insights in G-Protein-Coupled Receptor of Signal Transduction Relevant to Recent Developments in Drug Action

Jessie Evan^{* *}Correspondence: Jessie Evan, Department of Physical Science, Yale University, New Heaven, USA, Email:

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Introduction

Molecular receptor and signal transduction pharmacology has developed significantly in the second half of the last century and especially in the last two decades, with many new and existing concepts and models of pharmacological action. Many exciting new drugs are working through the novel pharmacological mechanisms that are expected to be of clinical use in the very distant future. More than 40% of all drugs marketed exhibit activity through G-protein-coupled receptors, and with the current bio-informatics many new drug targets related to Gprotein- coupled receptors can be explored and their physical and medical significance explored. The physician should be prepared and prepared to understand the action of these drugs and the possible reasons for their therapeutic uses. G-Protein-Coupled Receptors (commonly abbreviated GPCRs) are a large family of seven-Tran membrane diffuse receptors, including adrenergic, dopaminergic, serotonergic, muscarinic acetylcholine and histaminergic receptor receptors. GPCRs can transmit a signal from a drug bound to an extracellular surface to an intracellular surface. This is achieved by changing the shape to activate Gproteins at the intracellular surface of the membrane. The signal is subsequently passed down through a series of intracellular processes by the G-protein. The receptor (GPCR), the transducer (G-protein), and the effector (e.g. adenyl cyclase, phospholipase C, Ca²⁺ channels, and K⁺ channels) are the three components of this signaling mechanism.

Description

Current GPCR function theories have had a significant impact on our knowledge of drug action and have opened up new options for drug discovery. G-proteins on the inner surface of the cell membrane can be activated by Tran’s membrane GPCRs to perform signal transduction triggered by GPCR binding. Gproteins consist of three subunits, α-, β and γ subunits (hence the heterotrimetric character of G proteins), where the β- and γ- subunits function as one unit. To understand potential future drugs such as RGS-modulating drugs discussed below and how they modulate G protein function and consequently signal transduction, it is important to understand more about the mechanism by which G-proteins work. In the inactive state, the α-subunit of the G-protein binds to GDP. The complex structure between the active receptor state and the G protein releases GDP from the α-subunit of the G protein, which allows the GTP molecule to bind. Regulators of G-protein Signaling (RGSs) are a family of proteins that can modulate (regulate) signal transduction through G-proteins. Due to their significant physical performance along with many other special features, they are important potential drug targets. Receptor function can be further regulated by receptor transport, thereby controlling the number of receptors available in the cell membrane. The body uses this mechanism to prevent the continuous stimulation of a specific receptor. GPCR smuggling is also believed to play an important role in drug abuse, for example opioids (morphine and related drugs) and hallucinogens (e.g. Lysergic Acid Diethylamide or LSD), where it is tolerated with common drug-seeking behavior.

Conclusion

Understanding molecular receptor and signal transduction pharmacology allows practitioners to improve their understanding and effectively implement current and future pharmacotherapy. It helps practitioners to understand and evaluate possible drug interactions, develop and improve treatment strategies, and improve the quality of life of their patients. The challenge for the next millennium in drug discovery and receptor pharmacology will be to utilize the complex pharmacological properties of drugs that act on GPCRs for therapeutic purposes. New research in the field of GPCRs in the near future will lead to novel therapies aimed at optimizing drug therapies.