HIV-1 Protease Inhibitors Overview
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Questions and Answers

What is the dissociation constant (Ki) for Compound 1 when inhibiting HIV-1 protease?

  • 60.0 μM
  • 60.3 μM (correct)
  • 1.678 mM
  • 0.149 mM

    • How does the presence of Compound 1 affect the KM value of HIV-1 protease?

  • Increases KM value
  • Decreases KM value (correct)
  • Remains the same
  • KM value varies with concentration

    • What conclusion can be drawn from the parallel straight lines in a Lineweaver–Burk plot with Compound 1?

  • The enzyme undergoes activation.
  • The inhibitor is competitive. (correct)
  • The enzyme is non-competitive.
  • The substrate is saturated.

    • What is the maximum turnover number (kcat) for HIV-1 protease when 60 μM of Compound 1 is present?

    <p>0.126 s−1</p> Signup and view all the answers

    What is the quantity of Compound 1 needed to achieve a concentration equal to its Ki in a 100.00 mL solution?

    <p>2.92 mg</p> Signup and view all the answers

    Which parameter indicates how effectively an enzyme converts substrate into product per unit time?

    <p>kcat</p> Signup and view all the answers

    What effect does a decrease in kcat/KM have on an enzyme's efficiency?

    <p>Decreases efficiency</p> Signup and view all the answers

    Which peptide bond does HIV-1 protease hydrolyze in the peptide substrate IRKILFLDG?

    <p>After L and before F</p> Signup and view all the answers

    What is the quantity of Compound 1 that must be provided to prepare 100.00 mL of solution with a concentration equal to Ki?

    <p>2.92 mg</p> Signup and view all the answers

    What is the molar mass of Compound 1?

    <p>483.5 g mol−1</p> Signup and view all the answers

    What is the dissociation constant (Ki) of Compound 1?

    <p>60.3 μM</p> Signup and view all the answers

    HIV-1 protease hydrolyzes the peptide bond after leucine and before phenylalanine.

    <p>True</p> Signup and view all the answers

    Match the following kinetic parameters with their values for HIV-1 protease without Compound 1:

    <p>KM = 1.678 mM kcat = 0.250 s−1 kcat/KM = 0.149 mM−1 s−1 Ki = —</p> Signup and view all the answers

    What is the peptide substrate for HIV-1 protease?

    <p>IRKILFLDG</p> Signup and view all the answers

    Study Notes

    HIV-1 Protease Inhibitors

    • HIV-1 protease inhibitors are used to treat HIV-1 infections and prevent the onset of AIDS.
    • HIV-1 protease inhibitors work by blocking the activity of HIV-1 protease, an enzyme that is essential for the replication of the virus.
    • HIV-1 mutants can develop resistance to protease inhibitors, necessitating the development of new inhibitors.
    • Compound 1 is a new HIV-1 protease inhibitor being tested.
    • Compound 1 has a Ki value of 60.3 μM, which indicates its binding affinity to HIV-1 protease.
    • Ki is the dissociation constant for the enzyme-bound inhibitor, which can be EI or ESI depending on the type of inhibitor.
    • HIV-1 protease cleaves the peptide bond after leucine and before phenylalanine in the peptide substrate IRKILFLDG.
    • The study investigates the kinetics of HIV-1 protease with and without Compound 1.
    • Michaelis-Menten kinetics is followed by HIV-1 protease.
    • A Lineweaver-Burk plot of Vo-1 versus [S]-1 (without Compound 1) and at different Compound 1 concentrations produces parallel straight lines with positive slopes, signifying competitive inhibition.

    Preparation of Compound 1 Solution

    • To prepare 100 mL of a solution with a concentration equal to Ki (60.3 μM), 2.92 mg of Compound 1 is required.
    • The calculation involves converting 60.3 μM to μmol, then to mol, and finally multiplying by the molar mass of Compound 1 (483.5 g/mol) to obtain the mass in grams (0.00292 g).

    HIV-1 Protease Inhibitors

    • HIV-1 protease inhibitors are effective in reducing HIV-1 levels and delaying AIDS onset
    • HIV-1 mutants are developing resistance to existing protease inhibitors
    • Compound 1 is a new protease inhibitor being tested

    Compound 1

    • Compound 1 has a molecular weight of 483.5 g/mol
    • Compound 1 inhibits HIV-1 protease with a Ki of 60.3 μM
    • Ki is the dissociation constant for the enzyme-bound inhibitor
    • The peptide substrate for HIV-1 protease is IRKILFLDG
    • HIV-1 protease hydrolyzes the peptide bond after leucine and before phenylalanine

    Kinetic Parameters

    • The data was analyzed using Michaelis-Menten kinetics
    • A Lineweaver-Burk plot was used to determine the kinetic parameters
    • The plot showed parallel straight lines with positive slopes
    • This pattern suggests that Compound 1 is a competitive inhibitor

    Calculating the Amount of Compound 1 Needed

    • To prepare 100.00 mL of solution with a concentration equal to Ki (60.3 μM), 2.92 mg of Compound 1 is required
    • You can calculate this using the Molarity equation: M = mol of solute/ L
    • Convert 100 ml to L (100 ml / 1000 mL/L = 0.1 L)
    • Plug the values into the equation ( 60.3 μmol / 0.1 L)
    • Convert μmol to mol and then multiply by the molecular weight (483.5 g/mol) to get the mass in grams

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    MCAT Review: HIV-1 Protease Inhibitors PDF

    Description

    This quiz explores HIV-1 protease inhibitors and their role in treating HIV-1 infections. It covers the mechanism of action, resistance development, and the kinetics involved in the new inhibitor Compound 1. Test your understanding of protease inhibition and enzyme kinetics.

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