medicinal chem chapter 4 Flashcards
(30 cards)
What are the potential consequences of targeted drug design based on receptor structures?
Targeted drug design can lead to more effective treatments with reduced side effects and increased therapeutic specificity.
What is the significance of dimerization in receptor activation?
Dimerization is crucial for activation of receptors such as tyrosine kinase linked receptors, enabling their functional activity.
What is meant by induced fit in the context of receptor-messenger interactions?
Induced fit refers to the conformational change in the receptor that enhances binding interactions with the messenger.
Can you describe the process by which a receptor activates a membrane-bound enzyme?
The activated receptor binds to the enzyme or G-protein, inducing a conformational change that activates the enzymes catalytic site.
What types of chemical messengers are involved in neuronal communication?
Neurotransmitters and hormones are key chemical messengers in neuronal communication.
How do inflammatory mediators relate to receptor interactions?
Inflammatory mediators can initiate receptor activation, influencing immune responses and pain signaling in the body.
What is the mechanism of action for G-protein coupled receptors?
G-protein coupled receptors activate G-proteins upon ligand binding, leading to intracellular signaling cascades.
Why are receptors considered the most important drug targets in medicine?
Receptors are critical for drug action and are involved in various diseases, making them key targets for therapeutic intervention.
What is the general structure of G-protein coupled receptors?
G-protein coupled receptors are characterized by a single polypeptide chain that spans the membrane seven times, forming a helical structure.
Where are receptors predominantly located in the cell?
Receptors are mostly located in the cell membrane.
How do intracellular receptors regulate gene expression?
Intracellular receptors bind ligands, dimerize, and interact with DNA to regulate transcription and protein synthesis.
How do receptor types and subtypes influence drug selectivity?
Different receptor types and subtypes are distributed unevenly across tissues, impacting how drugs target specific physiological effects.
What defines the structure and function of receptors?
Receptors are proteins that act as cell communication letter boxes, located in cell membranes to receive and transmit messages from chemical messengers.
Which ailments are commonly associated with receptor dysfunction?
Receptor dysfunction is implicated in pain, depression, Parkinsons disease, psychosis, heart failure, and asthma.
How does the binding of a messenger to a receptor lead to signal transduction?
Binding causes an induced fit in the receptor, resulting in a change of shape that initiates signal transduction inside the cell.
How do intracellular receptors differ from membrane-bound receptors?
Intracellular receptors are located within the cell and often regulate gene transcription, while membrane-bound receptors typically transmit signals from outside the cell.
How do neurotransmitters differ from hormones in terms of their action?
Neurotransmitters act locally and are short-lived, while hormones travel longer distances in the bloodstream to their target cells.
How do different chemical messengers interact with receptors?
Each chemical messenger binds to specific receptors, switching them on without undergoing any reaction.
What are the various structural types of neurotransmitters?
Neurotransmitters can include amines, amino acids, ATP, prostaglandins, endorphins, and angiotensin.
What is the role of G-proteins in signal transduction?
G-proteins act as molecular switches that transmit signals from receptors to effector proteins within cells.
How are receptors named based on their activating neurotransmitters?
Receptors are named after the neurotransmitter that activates them, such as dopaminergic for dopamine-activated receptors.
What role do receptors play in cellular communication?
Receptors transmit messages into the cell leading to cellular effects.
What is the significance of receptor subtypes in medicinal chemistry?
Receptor subtypes allow for the design of selective drugs that target specific tissues with fewer side effects.
How does the flow of ions across a cell membrane affect cellular activity?
Ion flow can depolarize or hyperpolarize cell membranes, triggering subsequent biochemical responses.
