GMS6504 Exam 2 Questions And Answers With Real Tests
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GMS6504
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GMS6504
GMS6504 Exam 2 Questions And Answers With Real Tests
What are the 4 things that make something a good drug? ANS 1. Lipinski's Rule of 5
2. Chemical reactivity: good or bad?
3. Some chemically or biologically reactive functional groups to recognize
4. Choosing a target
What is Lipinski's ...
GMS6504 Exam 2 Questions And Answers With Real
Tests
What are the 4 things that make something a good drug? ANS 1. Lipinski's Rule of 5
2. Chemical reactivity: good or bad?
3. Some chemically or biologically reactive functional groups to recognize
4. Choosing a target
What is Lipinski's Rule of 5? ANS 1.Molecular mass greater than 500 Da
2.High lipophilicity (expressed as LogP greater than 5)
3.More than 5 hydrogen bond donors
4.More than 10 hydrogen bond acceptors
Partition Coefficient Definition ANS P = Coct/Cwater
How big are the differences in the partition coefficient? ANS very large scale, Log10(P)
What are the Improvements on the Lipinski Parameters (5) ANS 1. Partition coefficient log P in -
0.4 to +5.6 range
2. Molar refractivity from 40 to 130
3. Molecular weight from 160 to 500
4. Number of atoms from 20 to 70 (includes H-bond donors [e.g.;OHs and NHs] and H-bond
acceptors [e.g.; Ns and Os])
5. Polar surface area no greater than 140 Å2
What are 2 things that make chemical reactivity a good thing? ANS 1.Modification of Proteins
and/or Nucleic Acids (Bad if unanticipated and non-selective, but can be good if selective)
2. Labile in Biological Systems *Esters *Amide Bonds *Disulfide Bonds
, What are some chemically reactive functional groups? ANS Sulfonyl Halides - most halides (R
and X groups)
Aldehydes
Ketones
Epoxides - carcinogens
What is the name of the carrier linked to drugs to increase their availability? ANS Promoiety
What are some of the most common (biologically labile) functional groups utilized in prodrug
design? ANS Esters
Amides
Carbonates
What are the most commonly employed prodrugs? ANS Esters
What makes a good drug target? ANS Enzymes- Kinases, Phosphatases, Histone Deacetylases,
Misc. Metabolic Enzymes (Generally Cell Permeable Small Molecule Drugs)
Cell Surface Receptors- G-Protein Coupled Receptors, Receptor Tyrosine Kinases, Cytokine
Receptors. These can be:
- Cell Permeable Small Molecule Drugs that inhibit cytoplasmic enzyme domain
- Monoclonal Antibodies that target the extracellular domain
- Ligand binding site antagonists/inverse agonists
What are some challenges to Pharmacological Intervention? ANS "Undruggable" targets
(transcription factors, scaffolding proteins, protein-protein interactions involving large, flat protein-
protein interfaces)
Restoring the function of a gene lost by mutation/deletion
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