L1 T 1/14

Lecture 1. General Chemistry Review

Lewis Structures, Molecular Geometry, Arrhenius Equation, Second Law

Text: Lewis Structures; Molecular Geometry; Chemical Kinetics; Acids & Bases, Chemical Thermodynamics

Handout: Lewis Structure Methodology

Wiki: Hybridization; Aromaticity; Arrhenius Equation; Second Law of Thermodynamics  

L2 R 1/16

PS 1 Due

Lecture 2. Intermolecular Forces (Noncovalent Interactions)

Coulomb’s Law, Electronegativity, Hydrogen Bonds, Van der Waals Forces, Dipole-Dipole & Ion-Dipole Interactions, Solvation, Hydrophobicity

Wiki: : Electronegativity; Intermolecular Forces; London Dispersion Forces; Hydrogen Bonds; Coulomb’s Law; Solvation; Hydrophobicity

Text: Electronegativity, Intermolecular Forces (Hydrogen Bonding, Van Der Waals Forces, Dipole-Dipole & Ion-Dipole Interactions

L3 T 1/21

PS2 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

Wiki: Partition Coefficient;

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 1/23

PS3 Due

Quiz 1

Lecture 4. Condensation and Hydrolysis Reactions

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

Handout: Condensation Reactions

L5 T 1/28

PS4 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

Wiki: Amino Acids; Chirality; Peptide Bond; Henderson-Hasselbalch Equation;

Link:  Amino Acid Structures at pH=7.4   Amino Acid Chart with pKa Table 

L6 R 1/30

PS5 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

Wiki: Protein Structure   Disulfide Bonds

Kimball's Biology Pages: Proteins; Polypeptides;

Kimball's Biology Pages: Protein Structure: Primary; Secondary; Tertiary; Quaternary

7 T 2/4

Quiz 4

7 R 2/6

PS6 Due

Lecture 8. 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: Michaelis-Menten Model of Enzyme-Catalyzed Reactions

Kimball's Biology Pages: Enzymes

Kimball's Biology Pages: Enzyme Kinetics

L8 T 2/11

PS7 Due

Lecture 9. Enzymes as Drug Targets

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

Wiki: Enzymes; Enzyme Inhibitors

C1 R 2/13

Compensatory Time for Review Paper Preparation

L9 T 2/18

Quiz 5

Lecture 10. Medical Approaches to Inflammation I

Cyclooxygenase Case Study

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

Wiki: NSAIDs; COX-2 Inhibitors

Reading: Molecular Basis of Inflammation

L10 R 2/20

PS8 Due

Lecture 11. 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

Wiki: Steroid ; Zinc Finger; Complex Ion ; d-Orbitals

L11 T 2/25

Quiz 6

Lecture 12. Receptors as Drug Targets I

Neurotransmitters & Hormones, Agonists, Antagonists, Partial Agonists, Inverse Agonists,

Treatment of Hormone-Dependent Breast Cancers

Wiki: Neurotransmitters; Hormones; Receptors; Antagonists; Agonists; Partial Agonists; Inverse Agonists;

Ligands; Tamoxifen; Aromatase Inhibitors;

L12 R 2/27

Lecture 13. Receptors as Drug Targets II

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

Wiki: Efficacy; Dose-Response Curve; EC50; IC50; Therapeutic Index;

Scribd: Sensitization and Desensitization;

T1 R 3/4

Midterm

Mid-Term Examination on Material from Lectures 1-13

A Few Practice Problems....

L13 T 3/6

Lecture 14. Nucleic Acids as Drug Targets

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

Wiki: Akylating Agents; Sulfur Mustard; Cisplatin;

L14 T 3/11

Lecture 15. 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,

Wiki: Ion Channels; Nernst Equation; Action Potential ; K+ Ion Channel Nobel Chemistry Lecture (Video)

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

L15 R 3/13

PS9 Due

Lecture 16. 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

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

Wiki: Neuron; Membrane Potential; Na+/K+-ATPase

McGraw-Hill: Sodium-Potassium-ATP Pump

L16 T 3/25

Lecture 17. 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

2012 Nobel Chemistry - Nobel Lecture Rob Lefkowitz   Nobel Lecture Brian Kobilka

Wiki: G-Protein Coupled Receptors (GPCRs);

L17 R 3/27

Quiz 7

Lecture 18. Cholinergics

Nervous System, Cholinergic System, Acetylcholine Structure & Receptor Binding, Cholinergic Antagonists, Acetylcholinesterase Inhibitors

L19 T 4/1

Lecture 19. Adrenergics

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

L20 T 4/3

Lecture 20. Psychoactive Drugs I: Stimulants and Tranquilizers

Handout:

L21 R 4/8

Lecture 21. Psychoactive Drugs II: Anti-Depressants

Handout:

L22 T 4/10

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

Handout

L23 R 4/15

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 4/17

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 R 4/22

Test 2 Concepts

R1 T 4/24

Paper Due

Review