By Mark E Bunnage; David E Thurston; David Fox
Annotation content material: Chemical Proteomics; Chemical Genetics; Chemical Biology of Post-Translational; transformations; Chemical Biology of Epigenetics; RNA Interference; Proteolysis concentrating on; himeric Molecules (PROTACS); Antibody-Drug Conjugates; Chemologics: New Therapeutics on the Interface of Chemistry and Biology; summary: This ebook highlights the recent frontiers in chemical biology and describes their influence and destiny capability in drug discovery. learn more...
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4). 45 Valuable small molecule tools may also be obtained by structure-guided ligand design. The interaction between the lysine 382-acetylated p53 and the bromodomain of the coactivator CBP is essential for p53-induced transcription of the cell cycle inhibitor p21 in response to DNA damage. 48 Thus, the structure of the bromodomain of CBP (in complex with a peptide mimic of lysine 382-acetylated p53) enabled the design of a focused small molecule library to target the CBP/p53 interaction: NMR spectroscopy was then used to identify specific small molecules that bound to the bromodomain of CBP.
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