drug designing and enzymology
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Drug designing and
Enzymology
Submitted by :Mahnoor Khawaja
Submitted to: Dr. Amber
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Introduction
• Drugs act by binding to a receptor and
modifies its function.
• Lead compounds are best candidates for this
purposes .
Enzymes Proteins Neurotransmitters
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Lead compound
target validation
high-throughput screening
lead optimization
preclinical drug
development
clinical drug development
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SARs and QSARs
SARs
• Relationship between chemical or 3D of a molecule and its biological activity
• Can help to insert new chemical groups into the biomedical compound and test the results.
• Uses X-rays and NMR techniques.
QSARs
• Gives idea that there is simple mathematical relationship between biological activity of drug and physiology chemical properties.
• Calculate dosage
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Pharmacokinetics
Pharmacokinetics, described as what the body does to a drug,refers to the movement of drug into, through, and out of thebody—the time course of its absorption bioavailability distributionmetabolism and excretion.
‘make many compounds and see what they do’
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Formulation of HIV1 protease
HIV-1 protease is a retropepsin, that is essential for the life-
cycle of HIV.
HIV protease inhibitors, decreases in plasma HIV level, effect replication
infection rate of additional cells
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Mechanism
Binding to the active site
Mimic the tetrahedral
intermediate of its substrate
Become stuck
Produces immature proteins
Work with reverse transcriptase , to
lower the intensity.