PHR 911 Lecture 1: Drug Binding, Targets, and Cell Signaling

Flashcards cover key concepts from drug binding and targets, pharmacogenetics, drug interactions, routes of administration, signaling cascades, cell cycle regulation, and foundational pharmacology exam structure.

What forms when a drug binds to its biological target?

The drug-target complex, which leads to a pharmacological effect.

What must occur for a drug to produce a biological action in the body?

Formation of the drug-target complex is required for action.

What does pharmacogenetics study?

How genetic variation affects drug response, influencing which patients respond to which therapies.

What can drug-drug interactions cause in terms of drug metabolism and effect?

One drug can cause faster metabolism of another (lower therapeutic effect) or inhibit metabolism (longer exposure and potential toxicity).

What are some key components of giving the right drug to a patient?

Right concentration, right route, right time, and right individual.

Give an example of a non-oral route of drug administration mentioned in the notes.

IV (intravenous) administration is discussed alongside oral dosing.

What are the two main pieces of the course’s focus when studying pharmacology?

Drug molecules (organic chemistry and how they’re made) and the target (receptors and biology) that drugs act on.

Which textbook is referred to as the 'bible' for therapeutics in the course?

Goodman’s and Gilman’s Pharmacological Basis of Therapeutics.

How many blocks are in the course and what is the total point pool?

Four blocks totaling 400 points (4 x 100 points).

What are the grade thresholds for A, B, and C in this course?

A > 360 points, B > 320 points, C > 280 points.

What are the three parts of a signaling cascade?

Initiation (signal reception), propagation (downstream signaling), and termination (turning off the signal).

Where do most receptors reside and what is their job?

On the cell membrane; they bind ligands and trigger intracellular signaling.

What are the downstream signaling messengers after receptor activation?

Second messengers such as PIP2, DAG, IP3, and calcium.

Provide an example of a protein signaling molecule and a small molecule signaling molecule.

Protein signal: insulin; Small molecule signal: calcium (Ca2+).

What initiates a signaling cascade during wound healing in the example given?

Binding of a ligand to a receptor and subsequent kinase signaling that promotes cell proliferation to close the wound.

What is the role of kinases in signaling pathways?

Kinases add phosphate groups to proteins, propagating the ON signal; phosphatases remove them to turn signals off.

What are cyclin-dependent kinases (CDKs) and their role in the cell cycle?

Enzymes that drive cell cycle progression, regulated by cyclins.

What are cyclins and how do they regulate CDKs?

Regulatory partners of CDKs; they are produced and degraded to regulate progression through the cell cycle.

What is contact inhibition and how is it different in tumor cells?

Normal cells stop proliferating when they contact each other; tumor cells ignore this and keep growing.

How do bacterial cells replicate, in contrast to eukaryotic cells?

By binary fission, an asexual division process without a cyclin/CDK-regulated cell cycle.

What is a mitogen?

A signal that promotes progression through the cell cycle and DNA replication.

How long does a typical human epithelial cell take to divide?

Approximately 24 hours.

Where does signal initiation typically occur in receptor signaling?

At the cell membrane upon ligand binding to a receptor.

What happens when receptor tyrosine kinases are activated in the signaling cascade?

Receptor dimerizes or changes shape and triggers downstream kinase cascades.

What is the ultimate pharmacological goal discussed in the notes?

To use drugs to restore normal cellular function by forming the drug-target complex and modulating signaling.

What is the practical advice given about studying and using tutoring in this course?

Read regularly, take advantage of tutoring, and ask questions when unsure.