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Concepts of Genetics 11th Edition by William Klug,Michael Cummings,Charlotte Spencer,Michael Palladino
Edition 11ISBN: 9781292139456Concepts of Genetics 11th Edition by William Klug,Michael Cummings,Charlotte Spencer,Michael Palladino
Edition 11ISBN: 9781292139456 Exercise 39
Knowing the quaternary structure of proteins, specifically their surface properties, provides novel opportunities for enhancing the development of targeted drug therapies.
(a) Referring to Figure and the accompanying discussion, predict the class(es) of amino acids likely to reside on the surface of a protein within a cell.
(b) Assuming that Glu, Arg, and Asp exist in a functional site of a receptor molecule on the surface of a cell, provide an amino acid sequence that is likely to be effective in blocking that site.
(c) The androgen receptor associated with prostate cancer has recently been targeted using synthetic molecules known generally as peptidomimetics, many of which incorporate D-amino acid stereoisomers rather than the more naturally occurring L-amino acid stereoisomers. Why might D-amino acid stereoisomers be especially useful for inhibiting a functional site of the androgen receptor, or any deleterious functional site for that matter?
(d) Rational drug design is a relatively recent approach to the design of targeted therapeutic agents. Predict how knowledge of protein structure, especially surface properties, might be used in rational drug design as compared with the more classical "trial-and-error" approach.
Figure
Chemical structures and designations of the 20 amino acids encoded by living organisms, divided into four major categories. Each amino acid has two abbreviations in universal use; for example, alanine is designated either Ala or A.
(a) Referring to Figure and the accompanying discussion, predict the class(es) of amino acids likely to reside on the surface of a protein within a cell.
(b) Assuming that Glu, Arg, and Asp exist in a functional site of a receptor molecule on the surface of a cell, provide an amino acid sequence that is likely to be effective in blocking that site.
(c) The androgen receptor associated with prostate cancer has recently been targeted using synthetic molecules known generally as peptidomimetics, many of which incorporate D-amino acid stereoisomers rather than the more naturally occurring L-amino acid stereoisomers. Why might D-amino acid stereoisomers be especially useful for inhibiting a functional site of the androgen receptor, or any deleterious functional site for that matter?
(d) Rational drug design is a relatively recent approach to the design of targeted therapeutic agents. Predict how knowledge of protein structure, especially surface properties, might be used in rational drug design as compared with the more classical "trial-and-error" approach.
Figure
Chemical structures and designations of the 20 amino acids encoded by living organisms, divided into four major categories. Each amino acid has two abbreviations in universal use; for example, alanine is designated either Ala or A.Explanation
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The quaternary structure of a protein i...
Concepts of Genetics 11th Edition by William Klug,Michael Cummings,Charlotte Spencer,Michael Palladino
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