Handout 1 - Drugs & Drug Targets
Handout 1 - Drugs & Drug Targets CH 405/505
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Popular in Chemistry
This 11 page One Day of Notes was uploaded by Evan Roberts on Friday January 23, 2015. The One Day of Notes belongs to CH 405/505 at University of Alabama - Tuscaloosa taught by Timothy Snowden in Spring2015. Since its upload, it has received 97 views. For similar materials see Medicinal Chemistry in Chemistry at University of Alabama - Tuscaloosa.
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Date Created: 01/23/15
Patrick An Introduction to Medicinal Chemistry 5e Chapter 01 DRUGS amp DRUG TARGETS AN OVERVIEW Contents 1 Introduction Med Chenl amp Drug Development Stages 2 Drug Targets 3 Intermolecular Bonding Forces 31 Electrostatic interactions ionic bonds 32 Iondipole interactions 33 Hydrogen bonds 34 Dipoledipole interactions 35 TE Stacking amp cation7t interactions 36 Induced dipole interactions 37 Van der Waals interactions 38 Hydrophobic interactions amp Desolvation penalties Next Topic Amino Acids and Protein Structure 11 What is a Drug FDA De nition of a Drug An active ingredient that is intended to furnish pharmacological activity or other direct effect in the diagnosis cure mitigation treatment or prevention of disease 39 Excludes foods vitamins cosmetics compounds believed to be safe prior to 1 95 8 and substances not claimed to offer health bene ts Three Requirements for New Drug Approval 1 SC 6 2 mine 7L disease mk ogc LHr reJoWr at n a ho Fefraci 0Q ib39lc39h i 12 Drug Development Facts On average it takes in 15 WW Average total cost from conception to shelf is e s 15 w tat01 6 500 million in discovery phases and 600 1000 million We g Cir CO H033 Only 1 in Only in 10 marketed drugs recoup development costs mood to get a new drug to market in early lead compounds reaches the market 13 Top Selling Drug Classes 2013 quarries Aobimwm algaears cam bereaio Ame c1 pubeMS Ere0W9 5 15 39 sewamps Haw yden 39 I90 W0 microbic nchdvcms Pathquot WHY 1 f Petites 116 2 Chan Q 3 5 Raw T hey recoup development costs and allow less pro table drug classes to be investigated 14 Key Drug Discovery amp Development Stages p of minutes Hits Lads r some cm136 COMQQ amt 39 E i i tquot 30m u Antiadj 3 a a 1 Screening in target or Ll 39 diseasebased assays f i Target ID and Validation Assay Development Marketed Dw5 La 1 Drug 394 r f r a r C akk ofhr m39 k m Batch Synthesis if if i i y 7 i FormulationsStability quotquot fi Human Efficacy Safety amp PK Clinical Trials f 8 year average 7 if 39 f 15 Drug Types Over 80 of drugs are either small organics or monoclonal antibodies Different Types of Drugs Synthetic small molecule Drugs Approved 2013 Natural product de rived small molecule Monoclonal antibody Other protein Polymer Pep de Oligonucleotide Oligosaccharide Inorganic Other Other 21 Drug Targets Lipids Cell membrane lipids Proteins i i Transport proteins cell membranes and intracellular Structural proteins Nucleic acids DNA RNA Carbohydrates Cell surface carbohydrates Antigens and recognition molecules Drug Target Classes and Therapeutic Areas 4 We se 8 Oxidanduclases 1 0 mquot quot A 5 514 mm Transporter Enzyme U Ion Chime Membrane Receptor Transcription Factor Santos et al unpub shed 2014 21 Drug Targets Drug Targets and Drugs i I Drug target Total small Blztjllfllel39il p uUC 39l otal Snmll 1 Bl 39tlml39apeutjgs Class 39 1 targets nmlecule Q drug target drugs molecules I drug targets H Protein 315 243 7 85 1 Pathogen f quot quot f 52 49 4 205 200 5 Protein A Father hITnlxan 7 Ts f biomolecules ipathogen 8 397 2 102 99 3 biomolecules Santos et al unpublished 2014 21 Drug Targets Privileged Target Families Rhodopsinlike GPCR Ion channels Nuclear receptors Protein kinases PDBe 35n6 PDBe 4kfm PDBe 3e00 PDBe 4foc 22 of drug targets 12 of drug targets 6 of drug targets 13 of drug targets 33 of small mol drugs 18 of small mol drugs 17 of small mol drugs 24 of small mol drugs