L1 T 8/23

Lecture 1. General Chemistry Review

Electronegativity, Electron Configuration, Lewis Structures, Molecular Geometry, Hybridization, Double Bonds, Aromatic Structure, Kinetic Energy Molecular Distribution, and Vapor Pressure

L2 R 8/25

Lewis Due

UQ1

Lecture 2. Intermolecular Forces (Noncovalent Interactions)

Ionic Interactions, Hydrogen Bonds, Van der Waals Interactions, Dipole-Dipole and Ion-Dipole Interactions, Repulsive Interactions, Water Solvation, and Hydrophobic Interactions

Text Assignment: MedChem – 1.3 (Intermolecular Bonding Forces); Atkins – 5.1-5.5 (Intermolecular Forces)

L3 T 8/30

PS1 Due

Lecture 3. Solubility and Lipids

Thermodynamics of Liquid-Liquid Solubility, Octanol-Water Distribution Equilibrium Constants [Partition Coefficients (P)], Phospholipid Components and Structure, Cell Membrane Structure and Properties

Text Assignment: Atkins – 8.9 (The Like-Dissolves-Like Rule); MedChem – 18.2.1 (Hydrophobicity), 1.2.1 (Cell Structure)

Link: UCSF Membrane Tutorial (Great resource!!)

Reading: The Components and Properties of Cell Membranes

Link: Kimball's Biology Pages: Fats (Unsaturated Fats, Trans and Omega Fatty Acids, Phospholipids

L4 R 9/1

PS2 Due

Quiz1

Lecture 4. Condensation and Hydrolysis Reactions

Alcohols and Carboxylic Acids, Triglyceride Formation, Polyphosphate and Phospholipid Formation

Handout: Condensation Reactions

L5 T 9/6

PS3 Due

Quiz 2

Lecture 5. Amino Acids

Structure, Chirality, Side Chain Polarity, Peptide Bond,Peptide Condensation and Hydrolysis, Henderson-Hasselbalch Equation, Charge and pH, Solubility and pH

Text Assignment: MedChem – Chapter 2 and Appendix 1

L6 R 9/8

PS4 Due

Quiz 3

Lecture 6. Protein Structure

Primary Structure, Disulfide Bonds, Secondary Structure - Alpha Helices and Beta Sheets, Tertiary/Quaternary Structures and Associated Noncovalent Interactions, Prions, PostTranslational Protein Modifications

Text Assignment: MedChem – Chapter 2

L7 T 9/13

Quiz 4

Lecture 7. Enzymes: Structure and Function

Enzyme Catalysis, Mechanism of Action, Active Site, Substrate Binding, Catalytic Roles, Michaelis-Menton Kinetics, Lineweaver-Burk Plots, Km and Vmax Determination, Turnover Numbers, Km and Substrate-Enzyme Affinity

Text Assignment: MedChem – Chapter 3 (Enzymes: Structure and Function)

Text Assignment: Kimball's Biology Pages: Enzymes

Text Assignment: Kimball's Biology Pages: Enzyme Kinetics

L8 R 9/15

PS5 Due

Lecture 8. Enzymes as Drug Targets

Active Site Inhibitors, Allosteric Inhibition, Competitive / Uncompetitive / Non-Competitive Inhibitors, Suicidal Substrates

Text Assignment: MedChem – Chapter 7 (Enzymes as Drug Targets)

L9 T 9/20

PS6 Due

Quiz 5

Lecture 9. Medical Approaches to Inflammation I

Cyclooxygenase Case Study

Reading: Protein Function – Section III Cyclooxygenase (COX): An Example of How Enzymes Function

Reading: Molecular Basis of Inflammation

L10 R 9/22

PS7 Due

Lecture 10. Medical Approaches to Inflammation II

Steroids - Structure, Intracellular Receptors, Anti-Inflammatory MOA

Reading: Molecular Basis of Inflammation

Reading: Protein Function – Section II Nuclear Receptors: An Example of How Proteins Function

Reading: Kimball's Biology Pages: Steroid Hormone Receptors and their Response Elements

L11 T 9/27

Lecture 11. Receptors as Drug Targets I

Neurotransmitters & Hormones, Agonists, Antagonists, Partial Agonists, Inverse Agonists, Treatment of Hormone-Dependent Breast Cancers

Text Assignment: MedChem – Chapter 8, Sections 8.1-8.5

L12 R 9/29

Lecture 12. Receptors as Drug Targets II

Desensitization & Sensitization; Tolerance & Dependence; Receptor Types & Subtypes; Affinity, Efficacy, & Potency; Ligand-Receptor Dissociation Equilibria, EC50, IC 50, Scatchard Plots

Text Assignment: MedChem – Chapter 8, Sections 8.6-8.9

L13 T 10/4

Quiz 6

Lecture 13. Nucleic Acids as Drug Targets

Structure of DNA, Central Dogma, Intercalating Drugs, Alkylating & Metallating Agents, Cisplatin, 5-FU

Text Assignment: MedChem – Chapter 6, Section 6.1 (Structure of DNA)

Text Assignment: MedChem – Appendix 2 (The Standard Genetic Code)

Text Assignment: MedChem – Chapter 9, Sections 9.1, 9.3 (Intercalating Drugs, Alkylating & Metallating Agents)

Text Assignment: MedChem – Chapter 21, Section 21.2.3 (Alkylating & Metallating Agents)

L14 R 10/6

Lecture 14. Receptor Structure and Signal Transduction I – Overview of Ion Channel Receptors

Ion Concentration Gradients, Ion Channel Structure and Mechanisms of Action, Ligand-Gated and Voltage-Gated Ion Channels, Cell Membrane Potentials, Nernst Equation and Membrane Equilibrium Potentials, Ion Movements and Resulting Inhibitory/Excitatory Potential Changes,

Text Assignment: MedChem – Chapter 4, Section 4.6 (Ion Channel Receptors)

Text Assignment: MedChem – Appendix 4 (The Action of Nerves)

UCSF Reading: “Diffusion and Transport Across Membranes” Section on Ion Channels (pages 80-86)

T1 T 10/11

Midterm

Mid-Term Examination on Material from Lectures 1-13

A Few Practice Problems....

L15 R 10/13

Lecture 15. Receptor Structure and Signal Transduction II – Thermodynamics of Ion Channels

Sodium-Potassium-ATP Pump Mechanism, Cell Membrane Potentials, Nernst Equation and Membrane Equilibrium Potentials, Free Energy Changes of Ion Movement across Voltage and Concentration Gradients, Ion Movements and Resulting Inhibitory/Excitatory Potential Changes

Text Assignment: MedChem – Chapter 4, Section 4.6 (Ion Channel Receptors), Appendix 4 (The Action of Nerves)

UCSF Reading: “Diffusion and Transport Across Membranes” Section on ATP-Driven Ion Pumps (pages 73-77)

Wiki: 1. Resting Potential,  2. Na+/K+-ATPase

L16 R 10/20

PS8 Due

Lecture 16. Receptor Structure and Signal Transduction III – G-Protein Coupled Receptors (GPCRs)

G-Protein Coupled Receptor Structure, Evolutionary Tree of GPCRs, GPCR Signaling Mechanism of Action

Text Assignment: MedChem – Section 4.7 (G-Protein Coupled Receptors)

Text Assignment: MedChem – Section 5.1 (Signal Transduction Pathways for G-Protein Coupled Receptors)

Text Assignment: MedChem – Section 5.2 (Signal Transduction Involving G-Proteins and Adenylate Cyclase)

L17 T 10/25

Quiz 7

Lecture 17. Cholinergics I

Nervous System, Cholinergic System, Acetylcholine Structure & Receptor Binding

Text Assignment: MedChem – Chapter 19 and Appendix 4 (The action of nerves)

L18 R 10/27

Lecture 18. Cholinergics II

Cholinergic Antagonists, Acetylcholinesterase Inhibitors

Text Assignment: MedChem – Chapter 19 and Appendix 4 (The Action of Nerves)

L19 T 11/1

Lecture 19. Adrenergics

Geometry of Adrenergic Receptors, Main Types of Norepinephrine Receptors, Interaction of Adrenergic Receptors with Neurotransmitters, MOA of Activated Receptors

Text Assignment: MedChem – Chapter 20

 C1 R 11/3

Compensatory Time for Review Paper Preparation


L20 T 11/8

Lecture 20. Psychoactive Drugs I: Stimulants and Tranquilizers

Handout:

L21 R 11/10

Lecture 21. Psychoactive Drugs II: Anti-Depressants

Handout:

L22 T 11/15

Lecture 22. Psychoactive Drugs III: Anti-Psychotics and Hallucinogens

Handout


L23 T 11/17

Lecture 23. Psychoactive Drugs IV: Cannabinoids, Opium & Opioid Analgesics

Cannabinoids, Source and History of Opiates, Structure of Opioids and Opioid Receptors, Endogenous Opioids, Side Effects of Opiates

Text Assignment: MedChem – Chapter 21

L24 T 11/22

Lecture 24. Chemistry of Local & General Anesthetics

MOA for Local Anesthetics, pKa Relevance, History of Cocaine Use by Humans, MOA for General Anesthetics, Molecular Structures of Widely Used General Anesthetics

Handout: Local and General Anesthetics

T2 T 11/29

Test 2 Concepts

R1 R 12/1

Rev Paper Due

Review