"G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors (GPLR), form a large group of evolutionarily related proteins that are cell surface receptors that detect molecules outside the cell and activate cellular responses."
Introduction to relevant targets and receptors like enzymes, ion channels, G-protein coupled receptors (GPCRs), and nuclear receptors.
Introduction to Medicinal Chemistry: This provides fundamental knowledge about the principles and concepts of medicinal chemistry, including drug design, molecular targets, and mechanism of action.
Receptor Theory: This is the study of the interaction between drug molecules and their target receptors, including types of receptors, receptor binding, and signal transduction pathways.
Pharmacodynamics: The study of the relationship between drug concentration and its effects on the body, including dose-response curves and drug efficacy.
Pharmacokinetics: The study of drug absorption, distribution, metabolism, and excretion, including pharmacogenetics and drug interactions.
Drug Design and Optimization: The process of designing and optimizing drug molecules to improve their efficacy, safety, and selectivity.
Enzymes as Drug Targets: An overview of enzymes, enzyme inhibition, and its role in drug design.
GPCR (G-protein coupled receptor) targeting: The study of the largest family of receptors in the human body and their role in disease and drug discovery.
Ion channels targeting: An overview of ion channels, their structure, and their role in disease and drug discovery.
Nuclear receptor targeting: An overview of nuclear receptors, their role in gene regulation, and their implications in drug discovery.
ADMET (Absorption, Distribution, Metabolism, Excretion, and Toxicity): The study of the characteristics of drugs that determine their efficacy, safety, and pharmacokinetic profile.
Drug Development Process: The process of developing new drugs, including drug discovery, pre-clinical testing, clinical trials, and regulatory approval.
Design and Conduct of Clinical Trials: Study design, patient selection, ethical issues, and statistical analysis in clinical trials.
In vitro and in vivo Models: The use of models in drug discovery and development, including cell cultures, animal models, and human clinical trials.
Precision Medicine and Personalized Medicine: The application of genomic, proteomic, and other data to individualize medical treatments.
Modern Techniques in Drug Discovery: An overview of advanced techniques such as high-throughput screening, biologics, and computational drug design.
Enzymes: Proteins that catalyze biochemical reactions in the body by converting one molecule into another. Drugs that target enzymes can inhibit or enhance their activity depending on the therapeutic need.
G protein-coupled receptors (GPCRs): Membrane proteins that activate second messenger signaling pathways inside the cell upon binding with signal molecules such as hormones and neurotransmitters.
Ion channels: Membrane proteins that control the flow of ions into and out of cells. Drugs that target ion channels can modulate cellular excitability in nerve and muscle cells.
Nuclear receptors: Intracellular proteins that function as transcription factors to regulate gene expression in response to specific ligands such as hormones and vitamins.
Transporters: Membrane proteins that facilitate the transfer of molecules across cell membranes. Drugs that target transporters can modulate the uptake, distribution, and elimination of endogenous and exogenous substances in the body.
Kinases: Enzymes that transfer phosphate groups from ATP to proteins to regulate their activity. Drugs that target kinases can selectively inhibit abnormal signaling pathways that are associated with cancer and other diseases.
Ribosomes: Cellular particles composed of RNA and proteins that are responsible for protein synthesis. Interacting with ribosomes could prevent protein synthesis and cell division as seen in antibiotics.
"They pass through the cell membrane seven times in the form of six loops (three extracellular loops interacting with ligand molecules, three intracellular loops interacting with G proteins, an N-terminal extracellular region, and a C-terminal intracellular region)."
"The ligands that bind and activate these receptors include light-sensitive compounds, odors, pheromones, hormones, and neurotransmitters, and vary in size from small molecules to peptides to large proteins."
"The two principal signal transduction pathways involving G protein-coupled receptors are the cAMP signal pathway and the phosphatidylinositol signal pathway."
"When a ligand binds to the GPCR, it causes a conformational change in the GPCR, which allows it to act as a guanine nucleotide exchange factor (GEF). The GPCR can then activate an associated G protein by exchanging the GDP bound to the G protein for a GTP."
"GPCRs are targets for about 50% of drugs currently on the market, mainly due to their involvement in signaling pathways related to many diseases i.e. mental, metabolic including endocrinological disorders, immunological including viral infections, cardiovascular, inflammatory, senses disorders, and cancer."
"G protein-coupled receptors are found only in eukaryotes, including yeast and choanoflagellates."
"G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors (GPLR), form a large group of evolutionarily related proteins."
"They pass through the cell membrane seven times in the form of six loops (three extracellular loops interacting with ligand molecules, three intracellular loops interacting with G proteins...)."
"The global sales volume for these drugs is estimated to be 180 billion US dollars as of 2018."
"Approximately 34% of all Food and Drug Administration (FDA) approved drugs target 108 members of this family."
"They are all activated by agonists, although a spontaneous auto-activation of an empty receptor has also been observed."
"The long ago discovered association between GPCRs and many endogenous and exogenous substances, resulting in e.g. analgesia, is another dynamically developing field of the pharmaceutical research."
"...signaling pathways related to many diseases i.e. mental, metabolic including endocrinological disorders, immunological including viral infections, cardiovascular, inflammatory, senses disorders, and cancer."
"GPCRs are targets for about 50% of drugs currently on the market... associated with signaling pathways related to many diseases...cancer."
"The G protein's α subunit, together with the bound GTP, can then dissociate from the β and γ subunits..."
"The ligands that bind and activate these receptors include light-sensitive compounds..."
"They pass through the cell membrane seven times in the form of six loops..."
"Ligands can bind either to the extracellular N-terminus and loops (e.g. glutamate receptors) or to the binding site within transmembrane helices..."
"G protein-coupled receptors are found only in eukaryotes, including yeast, and choanoflagellates."