Dugga 2 - chapter 12 Flashcards
What is an orphan receptor?
In geonomics and proteomics when a possible target protein/receptor has been found but no lead compound have been developed to interact with this protein, then the receptor is an orphan receptor.
What is a multi-target directed ligand?
Single drug that targets many in a controlled manner
In vivo tests are done on?
Single cells, cell tissue or enzymes.
In vitro tests are done on?
Animals or bacteria.
What is transgenic animals?
Animals with altered genome ex has a human gene.
What is High throughput screenings (HIT)?
Robotic in vitro tests. They are fast, 1000 tests per day.
Con is possible false positives/negatives
promiscuous inhibitors
Agents that inhibit a range of different target proteins.
Screening natural products
Complex structures, can be hard to synthesis
What is pharmacognosy?
The study of medicines derived from natural sources
Plants is a rich source of lead compunds, name three.
- Cocain
- Paclitaxel (Taxol) from yew three
- Glantamine from Daffodils
What are some strategies deriving drugs form allready excisting drugs?
- Me too drugs
- Me better drugs
- Selective optimization of side activities ex viagra
- Medical folklore
- Screening synthetic compound libraries
Natural ligand or modulator
Often used by turing a agonist into an atagonist
Fragment-based lead discovery
Design a lead compound instead of discovering one. Linking of fragments = identification if a single fragment that binds to part of the binding sitem then finding larger and larger molecules containing the important fragments. (click chemistry)
