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Class Notes for Pharmaceutical Chemistry at University of Toronto St. George

PHC300Y1 Lecture 6: lecture 6_wells

PROTEIN-COUPLED RECEPTORS G protein raction Re eptor-G inte c MBcTnNISM oF SIcNRu.nvc Nature of the allosteric interactions guanyl between agonists and nucleotides Agonist O ll ' - siqruil 4raUsdueton JA ("'nrU ...

Pharmaceutical Chemistry
PHC230H1
Peter Wells
PHC300Y1 Lecture 5: 5.Molepharm G-protein.PDF

PROTEIN-COUPLED G RECEPTORS ?1 protetns u surh''rni-' artd A b ,J, alt n' , Wrr,i/0'tnhd'v- (a .- qO E D61 c<L;oSeHMr' t"rc'rnn3 -'fl^'L rS 4^AblWU.t - E.r1lrnrt c{ ' ucj"vW utw aI? pnoreN-CoUPLED pnor...

Pharmaceutical Chemistry
PHC230H1
Peter Wells
PHC300Y1 Lecture 4: 4.Molepharm G-rec.subtype.2.PDF

RECEPTORS PROTEIN-COUPLED G Receptors Pharmacological specificity receptors Subtypes of - *:*ffi;'"t"ncr 4o'ANTAGONISTS MUSCanNUC RaoToLegELLED /cHt N o (MeAtr Uethylatropine I'r- [3U] ) YV q cH3 ,lcHrcH2 CHe OH...

Pharmaceutical Chemistry
PHC230H1
Peter Wells
PHC300Y1 Lecture 2: 2.Molepharm basic pharm concepts.PDF

: BASIC PI{ARIVIACOLOGICAL CONCEPTS Dose, binding and response \ i . ; I t I I I I I I ! I tTHn Dose-RBspoNse CuRvn (2003) Matsui et al. J. Pharmacol. Exptl. Ther. 305,106-113. lo'ttdlvt{) 'r( LlttV.- - o1,l...

Pharmaceutical Chemistry
PHC230H1
Peter Wells
PHC300Y1 Lecture 3: 3.Molepharm G-rec.nature.structure.PDF

PROTEIN-COUPLED G RECEPTORS I ,, protein-mediated of Nature G systems Keceptors rrl , StructurePnOTEIN-CoUPLED G ReCgprORS (GPCRs) Protein-coupled receptors for approximately G account genome. 3.6% human of the (ne...

Pharmaceutical Chemistry
PHC230H1
Peter Wells
Lecture 8 Introduction to Model Organisms

Lecture 8 PHC320 Introduction to Model OrganismsModel organisms1Novel therapeutic Targets2Target ValidationChemical biologychemical geneticschemical probesInhibit gene function proteins with small moleculeTry to understand...

Pharmaceutical Chemistry
PHC320H1
Giaever
Lecture 7 Genetics and Technology Impact

Lecture 7 PHC320 Genetics and Technology ImpactCElegans to discover new small molecule toolsChemical Biology uses tools of chemistry to better understand biological processes overcome biological problemsDrug interferes wit...

Pharmaceutical Chemistry
PHC320H1
Giaever
Lecture 6 Failing Modern Drug Discovery

Lecture 6 PHC320 Failing Modern Drug DiscoveryFailing modern drug discovery invested in government and academic biotech and pharma60 approved drugsyear4045 reworked existing drugs1520 NCEsPreclinical science 35 years Very ...

Pharmaceutical Chemistry
PHC320H1
Giaever
Lecture 4 Clinical Trials

Lecture 4 PHC320 Clinical Trials Pharmacokinetics Pharmacodynamics and Drug metabolismConsiderations and potential biases in Lipinskis rulesPrePost 1997Criteria dependent onof Lipinski rules consideredPost 1983 most small ...

Pharmaceutical Chemistry
PHC320H1
Giaever
Lecture 3 Clinical Trials

Lecture 3 PHC320 Clinical TrialsTarget identificationHit GenerationLead GenerationEarly stage research and discoveryPreclinical AnimalsPhase 1 Safety Healthy HumansPhase 2 Efficacy Safety in PatientsPhase 3 Efficacy Safety...

Pharmaceutical Chemistry
PHC320H1
Giaever
Lecture 2 Biochemistry, Combinatorial Chemistry, Automation

Lecture 2 PHC320 Biochemistry Combinatorial Chemistry AutomationCellbased assay reverse disease based on general disease phenotypeTargetbased reverse disease based on molecular understandingMechanisms of action understood ...

Pharmaceutical Chemistry
PHC320H1
Giaever
Lecture 1 Historical Overview of Drug Discovery

Lecture 1 PHC320 Historical Overview of Drug DiscoveryDrugChemical substance affects processes of mindbodyUsed in diagnosis treatment prevention of diseaseSmall molecule synthetic or naturaloBiologicals antibody metabolite...

Pharmaceutical Chemistry
PHC320H1
Giaever
Historical Perspective: Targeted cancer therapies

Cells in multicellular organisms continuously signal each other and the environment This leads to proliferation differentiation and apoptosis In cancer there is a loss of balance in signalingProblem Humans go through a lar...

Pharmaceutical Chemistry
PHC320H1
Giaever
Targeting the EGFR: Iressa

The EGF ReceptorRTK family of cell surface receptorsIncludes epidermal growth factor receptor EGFRErb1Her1 and its relatives Receptors of EGFR subgroup essential for embryonic development and adult tissue homeostasis in ve...

Pharmaceutical Chemistry
PHC320H1
Giaever
Wnt and Hedgehog Signalling Pathways

Wnt signaling in development and diseaseNormal Roles multiple Wnt pathways regulate cell proliferation cell fates stem cell renewal and cell behavior in both embryos and adultsDiseases cancers bone density neurodegenerativ...

Pharmaceutical Chemistry
PHC320H1
Giaever
Inorganic Chemistry - Reference Guides

This Guide provides invaluable reference material to anyone who requires readily accessible information concerning the basic principles that underlie this complex science. The Guide carefully references the Periodic Table ...

Chemistry
CHEM 30100
All Professors
Permachart - Marketing Reference Guide: Iupac Nomenclature Of Inorganic Chemistry, Lithium Aluminium Hydride, Polyatomic Ion

p e r m a c h a rt s MT I n o r g a n i c C h e m i s t r y N o m e n c l a t u r e ...

Chemistry
CHEM 30100
All Professors
Permachart - Marketing Reference Guide: Locant, Parent Structure, Substituent

permacharts TM O r g a n icC h e m is t ryN o m e n c la t u r e Nam...

Chemistry
CHEM 22700
All Professors
Permachart - Marketing Reference Guide: Beta Particle, Beta Decay, Atomic Number

permacharts TM Periodic Table of the Elements ...

Chemistry
CHEM 11100
All Professors
Permachart - Marketing Reference Guide: Carnot Heat Engine, Carnot Cycle, Isentropic Process

permacha srtM PHYSICAL CHEMISTRY Basics Adiabatic process in which no heat is transferred into or out Internal energy The total kinetic and potent...

Chemistry
CHEM 11100
All Professors
Introductory Chemistry - Reference Guides

This Guide serves as a well organized and effective point of entry for anyone embarking upon the study of Chemistry. All fundamental terms are clearly organized in chart form, with illustrative graphics. More complex conce...

Chemistry
CHEM 11100
All Professors

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