Flashcards in Uses of Protein Structure in Molecular Medicine Deck (12):
What are two methods to determine the three-dimensional structures of macromolecules?
X-ray crystallography and NMR spectroscopy
Allows us to see rpotein connectivity (which atoms are next to which)
Not used for de novo drug design
What is the purpose of structure elucidation in drug design?
Help to redesign drugs to improve affinity, specificity, pharmodynamics, and toxicity
The same forces that stabilize protein structure stabilize a ligands interaction with a
Usually, drugs fail not because of the binding to the protein, but because of the
Pharmokinetics of the drug
Removes an amino acid from GLP-1 and GIP, which inactivates the two metabolic hormones
Inactivation of GLP-1 and GIP leads to
Overeating, furthering metabolic syndrome
One attempt at treating type two diabetes was to
Inhibit DPP-4, thereby keeping GLP-1 and GIP active
Lowers prandial and fasting glucose
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