Chapter 2 Case Study

What TWO strategies could be used for the development of substrate-based inhibitors for HIV aspartyl protease? What could potential chemical structures be for suitable candidate molecules?

Each compound was tested for its ability to inhibit fatty acid synthase activity in both normal cells and breast cancer cells. ID50 values (the inhibitor concentration required to inhibit cell growth by 50%) are shown in the table. Which inhibitors are most effective? Compound Alkyl side chain (R) Breast cancer cellsID50 (µg/mL) Normal cellsID50 (µg/mL) A −−C13H27 3.9 10.6 B −−C11H23 4.8 29.0 C −−C8H17 5.0 21.3 D −−C6H13 8.4 12.4       Compound D Compound C Compound A Compound B

The NFPA Hazard Identification System in the label below signifies. (attached photo) a.Extreme Danger, Above 100 ⁰F Not Exceeding 200 ⁰F, Violent Chemical Change, Acid b.Extreme Danger, Above 100 ⁰F Not Exceeding 200 ⁰F, Unstable if Heated, Corrosive c.Extreme Danger, Above 200 ⁰F, Violent Chemical Change, Acid d. Extreme Danger, Above 100 ⁰F Not Exceeding 200 ⁰F, Violent Chemical Change, Corrosive e. none of the above

which NFPA label correctly describes diethyl ether (CH3CH2)2O

4) Paxlovid is treatment for COVID-19 that was recently approved for use because it can drastically reduce the risk for hospitalization and death when taken early in the infection. It is actually a package of two different antiviral drugs. One of those is Nirmatrelvir, which is a modified tripeptide protein mimetic designed to covalently bind to and inhibit the main protease (MPro) from the SARS-CoV-2 virus. This protease recognizes and hydrolyzes peptide bonds at specific points in their sequence, and it is essential for viral replication. a. Below is one of the sequences that Mpro recognizes and cleaves. It cleaves the peptide bond between the glutamine and the glycine. Draw out the structure of a peptide with this sequence, including the appropriate stereochemistry for biological amino acids and assuming the peptide is at physiological pH (pH = 7.4). SGVTFQGKF b. What would the net charge of the peptide be at physiological pH?. c. At what pH would the peptide be net neutral?

+ H₂N- Protein CPMV N

Imagine the main chain of a protein bends back on itself, so that two amino acid residues R, and R₂ come close to each other. In the table below are four possibilities for what R, and R₂ might be. In each case, decide whether a specific interaction could form between residues. If a specific interaction could form, give the name of the interaction. R₁ R₁₂ specific interaction? name of specific interaction X 5 O yes O valine phenylalanine 0 О по O yes threonine tyrosine 0 O no O yes lysine glutamate 0 O no O yes phenylalanine serine Π O no Explanation Check Vicoran Hill LLC. All Rights Reserved. Terms of Use Privacy Center

A4  Your enzyme is inhibited by one of the compounds depicted above. The inhibitor for your specific protein is indicated via the PDB protein code shown.On the basis of the enzyme’s structure, its substrate and mechanism of action, predict what type of enzyme inhibition ( i.e., competitive or non-competitive) may occur and justify why you think this is the case . (Up to 50 words) TYPE NOT WRITE.

According to the diagram 1.does y intercept and slope change in noncompetitive inhibitor？ 2. does y intercept and slope change in mix inhibitor？ 3. Not sure if I draw the graph correctly，please help to correct my graph and lable out y intercept and shows if slope increase or decrease for each graph.

Enzymes that are rather aggressive, and turned "off" by a protein segment until they are activated. е.

Et3 N DME/ Me Sich 50 LDA/DMELC H₂0

I don't get it at all my homework. I struggled with this question. Can you help me? Can you explain to me?

Explain why an irreversible inhibitor of an enzyme might be more toxic to humans than a reversible inhibitor.

What is NFPA 704?

Please explain why this anwser was wrong for question 1 and what the errors made were. If possible also please explain how you can get the correct anwser for this problem.

Why is melphalan a good cancer drug?