Date post: | 04-Jun-2015 |
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THE QUEST FOR THE CURE
THE DRUG DISCOVERY CRISIS
Are we running out of drugs??
HOW DO DRUGS WORK
DIAZEPAM
PROZAC
IBUPROFEN
OMEPRAZOL
Most drugs (their active principle) are small molecules
ATORVASTATIN
DRUGS OF ABUSE
Morphine
Heroine (Bayer, 1874)
Cocaine
Cannabinol (THC)
The active principle is also a small moleculeAddiction as a side effect makes them not useful
HOW DO DRUGS WORKDrugs work by binding to specific proteins (enzymes) and modifying their activity
The selectivity of a drug in provided by the 3D structure of the target protein
Besides the large number of drugs available, only 2% of the human proteins are known to targeted by the drugs
Antibiotics and antivirals are drugs that inhibit bacterial and viral proteins, while leave ours untouched
Protein
HOW NEW DRUGS ARE DISCOVERED
In the past:
• by identifying the active ingredient from traditional remedies (plant extracts…etc. )
• by serendipitous discovery (e.g. penicillin, benzodiazepines)
Nowadays:
• Large scale testing of chemical collections • Rational design
HOW NEW DRUGS ARE DISCOVERED
Development of an assay for the desired activity
Screening thousand of compounds
Preclinical & clinical studies
Rational design based on :• Structure of the target.• Modification of known drugs
Target candidate
Basic Science
STAGES IN THE DRUG DISCOVERY PROCESS
Food and Drug Administration (FDA) in the United States (or comparable agency in other countries)
Lombardino & Lowe. Nature Reviews Drug Discovery (2004) 3, 853-862
The development of a new drug can take several decades and billion dollars invested
Target selection
THE DRUG DISCOVERY CRISIS
Are we running out of drugs??
• The better understanding of human biology will offer new candidates to find drugs(We must support basic research!!!)
• New technologies for the rational design of drugsare in development. They will reduce costs and will provide new medicines.
• There is little knowledge yet about how drugs interact.
• Gene therapy methods will join the “small molecule”toolbox once their safety is assured.
The future