Fragment-Based Drug Discovery: Difference between revisions

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Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

Arthur Cox, Justin Weekley, Jaime Prilusky

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 One tool used in rational drug design is structure-activity relationship (SAR) by nuclear magnetic resonance (NMR). This is a process "in which small organic molecules that bind to proximal subsites of a protein are identified, optimized, and linked together to produce high-affinity ligands."<ref>Shuker S. B., Hajduk P. J., Meadows R. P., Fesik S. W. Discovering High-Affinity Ligands for Proteins: SAR by NMR. Science; Nov 29, 1996; 274, 5292; ProQuest Central pg. 1531.</ref> Using this tool allows drug developers to create new drugs with minimal chemical synthesis, which then decreases the cost and time required to discover and develop new drugs.
-SAR by NMR is also useful for analyzing a drug target to obtain a better understanding of its function and activity as well as identifying similar targets. Bcl-2 and Bcl-w were discovered to play similar roles as anti-apoptotic proteins and were also found to be another target of
+SAR by NMR is also useful for analyzing a drug target to obtain a better understanding of its function and activity as well as identifying similar targets. For example, Bcl-2 and Bcl-w were proteins that were discovered to have structures very closely related to Bcl-xl as well as similar roles as anti-apoptotic proteins.
 === ABT-737 ===
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-Using this acylsulfonamide-based ligand as a template, or pharmacophore, other drugs can be designed to have similar effects. <scene name='Sandbox_reserved_394/Abt-737/1'>ABT-737</scene> has been shown to effectively inhibit the over-expression of this protein thereby inducing tumor regression and increasing chemo-sensitivity.
+Since proteins usually have multiple binding sites, exploring each site gives new insight on designing a ligand with the highest possible affinity. Upon analyzing cmpd 1,2,3,4, abt-737 waqs discovered <scene name='Sandbox_reserved_394/Abt-737/1'>ABT-737</scene> has been shown to effectively inhibit the over-expression of this protein thereby inducing tumor regression and increasing chemo-sensitivity.
 = References =
 {{Reflist}}