Passage 1 (Questions 1-4) Human immunodeficiency virus 1 (HIV-1) protease inhibitors have been successful at lowering HIV-1 levels and blocking the onset of acquired immune deficiency syndrome (AIDS). However, because HIV-1 mutants are developing resistance to current protease inhibitors, new inhibitors such as Compound 1 (molar mass: 483.5 g-mol-¹) are being tested. N Compound 1 Compound 1 has been shown to inhibit HIV-1 protease with K₁ = 60.3 μM (Table 1). K; is the dissociation constant for the enzyme-bound inhibitor, which is either El or ESI, depending on the type of inhibitor. The peptide substrate for HIV-1 protease is IRKILFLDG. HIV-1 protease hydrolyzes only the peptide bond after leucine and before phenylalanine. Compound 1 (μm) 0 60.0 120 Table 1 Kinetic Parameters of HIV-1 Protease with and without Compound 1 N H Км Ксач Км K₁ (mM) (S¹) (mM-¹ s¹) (HM) 1.678 0.250 00.149 0.832 0.126 0.151 60.3 0.430 0.064 0.149 60.3 Note: HIV-1 protease follows Michaelis-Menten kinetics. N N= N A Lineweaver-Burk plot of V.¹ versus [S]-1, both without Compound 1 and with different concentrations of Compound 1, generates a set of parallel straight lines with positive slopes. Adapted from T. Sperka, J. Pitlik, P. Bagossi, and J. Tösner, Bioorganic & Medicinal Chemistry Letters. ©2005 Elsevier Inc. Question 2 If only [1] is increased, then [ESI] or [E] increases. This is an example of: O A. the Bose-Einstein Principle. OB. the Heisenberg Uncertainty Principle. O c. the Le Châtelier's Principle. OD. the Pauli Exclusion Principle. OA. 33.5 and 15.7 Question 3 Which structural change to Compound 1 would make it more water soluble? OB. 75 and 30.1 O C. 150 and 60.3 O A. Replacing benzene CH with N in the ring OB. Replacing C=0 with C=CH₂ OC. Replacing N-N-N with CH-CH=CH OD. Replacing NH with NCH3 O D. 300 and 120.6 Question 4 In μM-s¹ and μM, what should the approximate values of kcat/KM and K, be, respectively, when [1] = 180 μM?
Passage 1 (Questions 1-4) Human immunodeficiency virus 1 (HIV-1) protease inhibitors have been successful at lowering HIV-1 levels and blocking the onset of acquired immune deficiency syndrome (AIDS). However, because HIV-1 mutants are developing resistance to current protease inhibitors, new inhibitors such as Compound 1 (molar mass: 483.5 g-mol-¹) are being tested. N Compound 1 Compound 1 has been shown to inhibit HIV-1 protease with K₁ = 60.3 μM (Table 1). K; is the dissociation constant for the enzyme-bound inhibitor, which is either El or ESI, depending on the type of inhibitor. The peptide substrate for HIV-1 protease is IRKILFLDG. HIV-1 protease hydrolyzes only the peptide bond after leucine and before phenylalanine. Compound 1 (μm) 0 60.0 120 Table 1 Kinetic Parameters of HIV-1 Protease with and without Compound 1 N H Км Ксач Км K₁ (mM) (S¹) (mM-¹ s¹) (HM) 1.678 0.250 00.149 0.832 0.126 0.151 60.3 0.430 0.064 0.149 60.3 Note: HIV-1 protease follows Michaelis-Menten kinetics. N N= N A Lineweaver-Burk plot of V.¹ versus [S]-1, both without Compound 1 and with different concentrations of Compound 1, generates a set of parallel straight lines with positive slopes. Adapted from T. Sperka, J. Pitlik, P. Bagossi, and J. Tösner, Bioorganic & Medicinal Chemistry Letters. ©2005 Elsevier Inc. Question 2 If only [1] is increased, then [ESI] or [E] increases. This is an example of: O A. the Bose-Einstein Principle. OB. the Heisenberg Uncertainty Principle. O c. the Le Châtelier's Principle. OD. the Pauli Exclusion Principle. OA. 33.5 and 15.7 Question 3 Which structural change to Compound 1 would make it more water soluble? OB. 75 and 30.1 O C. 150 and 60.3 O A. Replacing benzene CH with N in the ring OB. Replacing C=0 with C=CH₂ OC. Replacing N-N-N with CH-CH=CH OD. Replacing NH with NCH3 O D. 300 and 120.6 Question 4 In μM-s¹ and μM, what should the approximate values of kcat/KM and K, be, respectively, when [1] = 180 μM?
Biology 2e
2nd Edition
ISBN:9781947172517
Author:Matthew Douglas, Jung Choi, Mary Ann Clark
Publisher:Matthew Douglas, Jung Choi, Mary Ann Clark
Chapter24: Fungi
Section: Chapter Questions
Problem 33CTQ: Historically, artisanal breads were produced by capturing wild yeasts from the air. Prior to the...
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