Small-Molecule Inhibitors of Protein-Protein Interactions by Marc J. Adler, Andrew G. Jamieson (auth.), Lyubomir

By Marc J. Adler, Andrew G. Jamieson (auth.), Lyubomir Vassilev, David Fry (eds.)

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In this quantity, the editors have accrued the an expert insights of a couple of leaders during this box - researchers who've accomplished luck in addressing the tricky challenge of inhibiting protein-protein interactions. those researchers describe their specific methods, and percentage reports, effects, recommendations, and critiques. The content material of the articles is wealthy, and when it comes to scope levels from generalized methods to express case experiences. there are numerous focal issues, together with methodologies and the molecules themselves. eventually, there are various classes to be taken clear of this assortment, and the editors desire that this photograph of the present cutting-edge in constructing protein-protein inhibitors not just can pay tribute to the previous successes, but in addition generates pleasure concerning the destiny strength of this field.

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Extra info for Small-Molecule Inhibitors of Protein-Protein Interactions

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1 Discovery of Ro26-4550 . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 2 Structural Characterization of Ro26-4550 and the Importance of Protein Dynamics . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 3 Ligand-Binding Potential and Surface Plasticity of IL-2 . . . . . . . . . . . . . . . 4 Medicinal Chemistry Optimization of IL-2 Antagonists: SP4206 . . . . .

5 Computational Methods . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 49 6 Conclusions . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 50 References . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 51 Abstract The IL-2:IL-2R protein–protein interaction is of central importance to both healthy and diseased immune responses, and is one of the earliest examples of successful small-molecule inhibitor discovery against this target class.

The X-ray structure of the IL-2:Ro26-4550 complex displays marked alterations in protein conformation from unliganded IL-2 (Arkin et al. 2003). This result contrasts with the determined protein co-structures described above, which show few differences in IL-2 upon binding receptor subunits. Where the free- and receptor-bound IL-2 Small-Molecule Inhibitors of IL-2/IL-2R: Lessons Learned and Applied 37 Table 1 Structure–activity relationships among IL-2 inhibitors. M. R. 06 N N O O Cl Cl N N O H H N NH2 NH Fig.

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