Pharmacology Assignment Targets and Receptors
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Added on 2020-05-08
Pharmacology Assignment Targets and Receptors
Added on 2020-05-08
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Targets and Receptors 1TARGETS AND RECEPTORS IN THE TREATMENT OF CONDITIONS OF THEENDOCRINE SYSTEM.by (Name)CourseTutorInstitutionLocationDate
Targets and Receptors 2IntroductionReceptors which are located on both the surface of the cell and also with it are the molecular targets through which drugs exert their effects in various diseases and health conditions. The term 'receptor' is used in a broader sense to refer to any recognition site for drug and drug-like compounds. They are defined as per their selectivity, saturability, functionality, and reversibility of ligand binding [ CITATIONWil06 \l 1033 ]. Defining a receptor in both physiological and pharmacological terms means that it bears precise interactions with ligands belonging to a particular pharmacological class. Thus, drug compounds used in the treatment of conditions of the endocrine system need to have a specific compound structure to be able to target the various receptors for the delivery of therapeutic effects. This paper is a discussion on the targets and receptors in the treatment of the various conditions of the endocrine system. This discussion is carried as per each individual condition or where feasible, class of conditions, outlining the drug compounds used and their targets.DiscussionThere are different classes of drugs adopted for the treatment of the various presentations of disorders of the endocrine system. It is, therefore, necessary to group and classify these disorders. There are four primary classes of disorders relevant to this discussion; disorders in glucose homeostasis. thyroid disorders, disorders in calcium homeostasis, and disorders of pituitary gland. a)Targets and receptors in the treatment of glucose homeostasis disordersConditions classified under glucose homeostasis disorders include diabetes, hypoglycemia, and glucagonoma.
Targets and Receptors 3The glucagon receptor (Gcgr)The glucagon receptor is a peptide hormone mainly expressed in the liver and kidney with other minor sources such as the heart, spleen, GI tract, pancreas, adipose tissue, thymus, adrenal glands, and cerebral cortex. This receptor is one of the members in the family B receptors classified under the G protein-coupled super-family of 7 transmembrane-spanning receptors [ CITATION FAu08 \l 1033 ]Glucagon is the primary hormone which opposes the action of insulin. It is the primary hormone secreted by pancreatic alpha cells whose primary role is the provision of sustainable supply of glucose to the vital organs during fasting periods. To achieve this, hepatic glucose production is stimulated by specific G-protein-coupled receptors (GPCRs) located mainly hepatocytes [ CITATION Chr111 \l 1033 ]. Patients presenting with type 2 diabetes mellitus, have elevated levels of glucagon which plays a key function in the development of hyperglycemia among thisgroup of patients. Evidence from a number of research studies shows that targeting the pancreatic alpha-cells and glucagon (its primary secretory product) can T2DM[ CITATION Chr111 \l 1033 ]. With such evidence, drugs developed in the management of T2DM either antagonise the glucagon receptor or suppress glucagon secretion.Glucagon receptor (GCGR) antagonism in the management of hyperglycaemia has been demonstrated using glucagon peptide antagonists, small molecular weight GCGR antagonists, GCGR antisense oligonucleotides, and anti-glucagon neutralising antibodies can treat diabetes [ CITATION Slo05 \l 1033 ]. The insulin receptor(IR)
Targets and Receptors 4This is a transmembrane receptor belonging to the class of tyrosine kinase receptors. Its activation is mediated by insulin, insulin-like growth factor 1 (IGF-1), and insulin-like growth factor 2 (IGF-2) [ CITATION War09 \l 1033 ]. This receptor regulates glucose homeostasis. Drugs targeting the insulin receptor increases the affinity of glucose transporter molecules on tissues that are insulin-responsive, and as a result increases the uptake of blood into such tissues [ CITATION Jér14 \l 1033 ].Glucagon-like peptide 1 receptor (GLP1R)This receptor is found in pancreatic beta cells and its activation leads to the stimulation of the adenylyl cyclase pathway which translates to increased insulin synthesis and its release [ CITATION Hol04 \l 1033 ]. This receptor has been a target in the development of the class of drugs known as GLP1R agonists used in the treatment of diabetes. GLP1R agonists potentiate the glucose-induced secretion of insulin from pancreatic beta cells, suppresses post-prandial glucagon release, promotes beta-cell neogenesis and also inhibits their apoptosis, delays stomach emptying, increases expression of insulin, elevates peripheral glucose disposal and promotes satiety [ CITATION Don12 \l 1033 ]. Free fatty acid receptorsFree fatty acids (FFAs) play a significant role in glycaemic regulation and the pathogenesis of T2DM [ CITATION Ber00 \l 1033 ]. GPCRs for FFAs form part of the body's nutrient sensing mechanism and are included in the pancreas, GI tract, leucocytes, adipose tissue and other parts of the CNS. This class of receptors are not restricted to the ‘lock and key’ theory but are rather considered to be diverse in the sense that their activation is mediated by a wide range of ligands [ CITATION Fre10 \l 1033 ]. Vangaveti and fellow authors further claim that agonists of FFAR1 and
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