During an SAR effort to identify tyrosine kinase inhibitors, it was found that compound 2 was significantly more potent and selective than compound 1. To what might you attribute this improvement in activity and selectivity? Explain. ICS micromolar IC- 0.1 mcromelar
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- In Figure 4C, we see the inhibition of LRRK2 kinase activity by nanobody 1 (Nb1). Using the Lineweaver-Burke plot, estimate the Km of LRRK2 in the absence of Nb1. Show your work and provide your answer with the correct units.What is the relative inhibition of the kinase if the substrate concentration equals KS= 50mM and the concentration of the inhibitor equals KI =250mM?Functional and structural analysis indicates that Gleevec is an ATPcompetitive inhibitor of the Bcr-Abl kinase. In fact, many kinase inhibitors under investigation or currently marketed as drugs are ATP competitive. Can you suggest a potential drawback of drugs that utilize this particular mechanism of action?
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- Crystal structures exist for three neurokinin-1 (NK1) ligand complexes with the following pdb codes (6hll, 6hlo,6hlp). State which is the highest quality crystal structure indicating the criteria you used to evaluate this.Explain how can cAMP’s activation of a single molecule, cAMPdependent protein kinase, be common to the great variety of biochemical sequences and cell responses initiated by cAMP-generating first messengers?Assuming you have an agonist, a competitive antagonist, and an easy assay for measuring binding of the agonist, describe a simple experiment that would allow you to determine specific binding, nonspecific binding, and total binding of the agonist at a SINGLE concentration.
- If instead of using 3.5 µM myoglobin (receptor) you used half of this (that is, 1.75 µM myoglobin), what would be that value of the Kd, that you calculated ( how would it change)? Please explain so I can solve on my own :) (How does changing concentration of the receptor in a ligand-receptor binding experiment affect the dissociation constant?)From experiments in which cells expressing normal myosin II heavy chain were altered to either lack (mhckA-) or overexpress (MHCKA ++) a myosin heavy chain kinase (MHCKA). For answering this question recall the earlier the variants on the myosin II heavy chain, in which three key threonines, normally subject to reversible phosphorylation, were altered in various ways: 3X Ser = Serines in place of Threonines 3X Ala = Alanines in place of Threonines 3X Asp = Aspartate in place of Threonines MHCKA is present at normal levels. Which of the two mutants (mhcp- or MHCP++) would be most likely to have a defect in cytokinesis?To maximize the activity of an α4β2 nicotinic Achtylchcholine Receptor (nAChR), how many agonist binding sitea should be occupied?