Drug Discovery & Development

The first step in rational drug design is to ________

• identify the target molecule

• characterize the shape of the target molecule

• find a lead

• test the drug molecule

In rational drug design, you cannot design a new drug until _______

• you have tested a similar drug on animals

• you have tested a similar drug on people

• you have characterized the structure of the target molecule

• you have received clearance to do so from the FDA

The target molecules can be the following EXCEPT

• receptors

• enzymes

• free oxygen

• transcription factors

Which of these statements best describes a lead compound?

• A compound that contains the element lead

• A molecule that shows some activity or property of interest and serves as the starting point for the development of a drug

• A compound from the research laboratory that is chosen to go forward for preclinical and clinical trials

• The first compound of a structural class of compounds to reach the market.

Identify the kind of interactions that are typically involved in binding a drug to the binding site of a protein.

• predominantly van der Waals interactions

• predominantly hydrophobic interactions

• predominantly hydrogen bonds

• a combination of all of the above

Which of the following statements best describes an induced fit?

• the process by which a binding site alters shape such that it is ready to accept a drug

• the process by which a drug adopts the correct binding conformation before entering a binding site

• the process by which binding of a drug to a binding site alters the shape of the binding site

• the process by which a binding site alters the shape of the drug into the binding conformation before binding

Which of the following descriptions most accurately describes binding sites and binding regions?

• a binding site is part of a binding region

• a binding region is part of a binding site

• a binding region is the same as a binding site

• a binding region is on a drug whereas a binding site is on a macromolecular target

Which of the following statements best describes pharmacokinetics?

• the study of how drugs reach their target in the body and how the levels of a drug in the blood are affected by absorption, distribution, metabolism and excretion

• the study of how drugs can be designed using molecular modelling based on drug's pharmacophore.

• the study of how a drug interacts with its target binding site at the molecular level to produce a particular pharmacological effect.

• the study of which functional groups are important to a drug's activity, and the identification of a pharmacophore.

What is meant by ADME in pharmacokinetics?

• Affinity, dosage, marketing, efficacy

• Absorption, distribution, metabolism, excretion

• Agonism, dependence, mobility, efficiency

• Antagonism, deficiency, mean, efflux

Which of the following is one of the rules in Lipinski's rule of five?

• A molecular weight equal to 500

• No more than five hydrogen bond acceptor groups

• No more than 10 hydrogen bond donor groups

• A calculated logP value less than +5