Lecture #1 Flashcards
what is a ligand?
a molecule (biological or other) that interacts with another molecule
what is a xenobiotic?
a molecule that is not present naturally in the human body but is synthesized - able to interact with a protein
what does quality mean in terms of drug discovery?
means to populate the chemical space in terms of physical properties and to ensure the ideal pharmacokinetic profile
what is pharmacokinetics?
the fate of the molecule within the body
what is the objective of chemistry-driven drug discovery?
to design a molecule that is not only able to maximize the recognition of the binding site, but is also stable enough to survive a long time after the systemic administration and maximize its concentration at the site of action
what does modern refer to?
implies there was an evolution from the past
which is easier to do, create an effective drug or create a safe drug?
an effective drug
on average how long does it take to create a drug and go through all the steps?
more than 12-13 years
in 2017, what were the top 4 causes of death?
cardiovascular disease, cancer, respiratory disease, and diabetes
what is Parkinson’s disease?
a slow progressive disease of the CNS due to a reduction in the amount of dopamine in specific areas of the brain (substantial nigra)
what is Parkinson’s disease?
a slow progressive disease of the CNS due to a reduction in the amount of dopamine in specific areas of the brain (substantial nigra)
what does Parkinson’s effect?
the motor system at the early stage of the disease, and at the late stage there is a clear impact in terms of depletion → it is a degenerative process responsible for the loss of the cognitive process
what is a challenge when developing drugs for Parkinson’s?
the only drug at the moment has a tolerance mechanism occurring - there’s a need to increase the dose in order to maintain its effectiveness
what is a glioblastoma?
one of the mot devastating brain tumors - available drugs have minimal efficacy and the median survival time is 15 months
what is the main issue in terms of drug discovery when dealing with cancer?
the ability of chemotherapeutics to get across the blood brain barrier
