Given the active site and reaction mechanism, identify the mechanism of irreversible inhibition for the inhibitor provided below. Active Site HN Affinity-based inhibitor Mechanism-based inhibitor Transition state analog Non-specific inhibitor Uncompetitive Inhibitor Reaction Mechanism مو 8+ HN ܘܟܘ O d. -EtOH HN Inhibitor OH HN. Br
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- Given the active site and reaction mechanism below, what is the mechanism of irreversible inhibition of the inhibitor provided? NH* Active Site *H₂N. HN NH₂ +H₂N HN H₂N NH₂* Non-specific inhibition Uncompetitive Inhbitor Transition State Analog i Affinity-based inhibition Mechanism-Based Inhibition Reaction Mechanism *H₂N. NH HN- HN [*] H₂N NH₂ 2+Mn Mn²+ i +H₂N. H₂N i H₂N NH₂ HO Inhibitor *H₂N. B OH r View site informatiA schematic representation of the enzyme IspD complexed to inhibitor 3, and a series of inhibitors 3-5 are shown below. Ala202 lle240 mwww NH NH Val263 ОН www HN N- lle177 HN 'N' CI 3 X = N 4 X = C-CN 5 X = C-COO IC50 274 µM IC50 140 nM IC50 35 nM NH2 HN Val266 N -N O-H---- N HN %3D Arg157 HN wwww lle265 Explain why structure 4 is a more potent inhibitor (lower IC50 value) than inhibitor 3 and why structure 5 is a much weaker inhibitor (higher IC50 value) than 3 and 4.Why does the apparent KM decrease in the presence ofan uncompetitive inhibitor?
- Under what conditions, a higher rate in the presence of the inhibitor observed? (how could the effect of inhibitor be compensated) explainMatch the different names for inhibition mechanisms (1-5) with a description of their properties 7a-7d: 1. competitive inhibitor. 2. allosteric inhibitor also known as non-competitive inhibitor. 3. un-competitive inhibitor. 4. affinity label also known as active site directed covalent (irreversible) enzyme inhibitor. 5. Kcat inhibitor, also known as a mechanism-based covalent (irreversible) enzyme inhibitor. 4a. An enzyme inhibitor in which a substrate or competitive inhibitor is modified so that it contains a chemically reactive electrophile which can bind to and subsequently react with the enzyme active site: 4b. An enzyme inhibitor that contains latent reactive group that upon binding followed by catalytic turnover at the enzyme active site produces a reactive electrophile that reacts covalently with the enzyme: 4c. A reversible inhibitor that competes with the substrate for binding to the enzyme active site: 4d. A reversible inhibitor that can bind independently of substrate to its…Calculate KI' of the inhibitor from the information given. All information may not be needed to calculate. K'm = (29Ki+1.45x10^-10)/Ki Vmax = 11.7 µMs-1 Kcat = 130 s^-1 Vo = 3.0 μMs-1 S = 10 μM Et = 0.09 µM Inhibitor Concentration = 5x10^-12
- Define the term minimum inhibitory concentration and their uses.Which of these heterocyclic drugs is likely to be the least soluble in water? Use the Fsp³ parameter to decide. OH Tramadol Chemical Formula: C16H25NO2 YOUR OW Pantoprazole Torasemide Chemical Formula: C16H15F2N3O4S Chemical Formula: C16H20N4O3S Temazepam -OH Chemical Formula: C16H13CIN₂O2 Tioconazole Chemical Formula: C16H13C3N₂OS A. Tramadol B. Pantoprazole C. Torasemide D. Temazepam E. ToconazoleGiven the active site and reaction mechanism below, what is the mechanism of irreversible inhibition of the inhibitor provided? Active Site Reaction Mechanism Inhibitor `NH2. н Он SH OH- OH OH HO- NH „NH OH OH OH -Mg²+ Uncompetitive Affinity-based Transition state analog Non-specific Mechanism-based
- Briefly describe the effects of a linear noncompetitive inhibitors on the kinetic parameters Km and Vmax. breifly discuss the reasons behind the effect of this type of inhibition on the kinetic parametersDiscuss why fluoroacetate can be called a mechanism-based inhibitor. what is a mechanism based inhibitor?A series of novel phenadoxone derivatives without mu2 receptor activity (mu2 activity is responsible for physical dependence) proposed to be developed as analgesics is shown below. Addition of which heterocyclic substituent R to phenadoxone is LIKELY to cause the MOST binding of the corresponding derivative to plasma proteins? Use the additivity of approximate estimates of logP to answer this question. phenadoxone derivatives A. Azetidine B. Thiophene C. Oxetane D. Furan E. Pyrrole ترف لي تي في R= -NH