Finding A Lead Flashcards

1
Q

What is the drug discovery process

A

Target identification - lead generations - active to hit - hit to lead - new lead optimisation projects - candidate drug

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2
Q

What is a lead compound

A

Compound that shows the desired pharmacological activity against a chosen target. Starting point for drug discovery process

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3
Q

Approaches for finding a lead compound

A

Natural product
Library screening
Evolution of excising drugs
Side effects of existing drugs

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4
Q

What are natural products

A

Rich source of biologically active compounds that contain an active compound

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5
Q

Example of demand for natural product

A

It takes 1 true to provide a months supply of taxol for one person. It is now being found in the leaves too

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6
Q

Medical folklore for finding a lead compound

A

Ancient people depended on local flora ad fauna and can give us clues to high plants might be worth studying ie willow tree for aspirin and opium poppy for morphine

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7
Q

Lead compounds from microorganisms

A

Bacteria and fungi have evolved t produce Antimicrobial properties. Most drugs are Antimicrobial bar a few.

Ie in a handful of soil there are thousands of bacteria fighting for the habitat and so have produced chemical defences

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8
Q

Lead compound sources from venoms and toxins

A

Venoms from plant and animals are potent and have specific interactions with macromolecule targets in the body

Ie Brazilian viper for captopril (ACE inhibitor)

Bright frogs don’t produce toxins its the ant they eat and the plants that the ants eat

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9
Q

What is a sensible staring point for a lead compound

A

The natural ligand of a target receptor

Adrenaline and noradrenaline were lead ompounds for the development of salbutamol `

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10
Q

What are existing libraries

A

Pharm companies dont throw out the compounds they make. Libraries are full of compounds for testing whenever a new target is studied. Companies also buy from ter libraries. Not the best way

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11
Q

What are me too and me better

A

Companies modify the structures of existing drugs to develop new drugs within the same market

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12
Q

Luck in finding new lead compound

A

Serendipity

Siendafil was originally designed a a vasodilator to treat angina and hypertension but showed more effective vasodilation in male genitals than the heart

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