Small molecules are used as inhibitors of protein action - as drugs. They most often do thisby blocking the active site within the protein. Potential drugs can be screenedcomputationally to determine if they are strongly bound to the protein.Figure 1 shows a possible conformation of a candidate drug molecule, 4-bromo-2-carboxymethylamide-pyrrole (abbreviation: BCMAP) at the active site of a protein(abbreviation: PR). Figure 2 shows the full protein structure whilst figure 3 shows a knowninhibitor of the protein at the site, overlayed with another calculated conformer of BCMAP.(c) Outline how you would investigate whether BCMAP would be an effective inhibitorfor the protein in competition with the molecules that the protein normally targets,and any solvent.Figure 1. 4-bromo-2-carboxymethylamide-pyrrole (BCMAP) (C, N, O, and Br atoms in yellow, blue,red, and brown, respectively) in the active site of the protein structure. Figure 2. Cartoon (ribbon) structure of the entire protein with a known inhibitor in position, asdetermined experimentally. Cations and water molecules in the protein structure are omitted forclarity. The links labelled can be cleaved chemically.lle1122CleavableLinksLeul120Tyr1167Asn1168Val1174Prol110Figure 3. An overlay of a known inhibitor (from Figure 2) and an example conformer of BCMAP. Dashedlines indicate hydrogens bonds and electrostatic interactions. The isolated cyan atoms are sodiumcations and the isolated red atoms the determined positions of the oxygen in a water molecule.

Inhibitors are the molecules that slow down or completely block the protein activity of molecules,…

Answered: (c) Outline how you would investigate…

Biology: The Dynamic Science (MindTap Course List)

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ISBN:9781305389892

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Chapter4: Cells

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(c) Outline how you would investigate whether BCMAP would be an effective inhibitor for the protein in competition with the molecules that the protein normally targets, and any solvent.