Uses of Protein Structure in Molecular Medicine Flashcards Preview

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Flashcards in Uses of Protein Structure in Molecular Medicine Deck (12):
1

What are two methods to determine the three-dimensional structures of macromolecules?

X-ray crystallography and NMR spectroscopy

2

Allows us to see rpotein connectivity (which atoms are next to which)

2D NMR

3

Not used for de novo drug design

Structure

4

What is the purpose of structure elucidation in drug design?

Help to redesign drugs to improve affinity, specificity, pharmodynamics, and toxicity

5

The same forces that stabilize protein structure stabilize a ligands interaction with a

Protein

6

Usually, drugs fail not because of the binding to the protein, but because of the

Pharmokinetics of the drug

7

Removes an amino acid from GLP-1 and GIP, which inactivates the two metabolic hormones

DPP-4

8

Inactivation of GLP-1 and GIP leads to

Overeating, furthering metabolic syndrome

9

One attempt at treating type two diabetes was to

Inhibit DPP-4, thereby keeping GLP-1 and GIP active

10

Lowers prandial and fasting glucose

GLP-1

11

How did structural elucidation help in the attempt at synthesizing a nontoxic inhibitor of DPP-4?

Structural characterization of DPP-4 allowed for the inhibitors to be redesigned based on DPP-4's structure

12

Once two promising inhibitors were obtained, the important regions of these compounds were identified by knowing their structure. This then served as a scaffold for drug design to improve

Affinity, specificity, and pharmacokinetic properties

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