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Drug discovery toward antagonists of methyl-lysine binding proteins.

ABSTRACT: The recognition of methyl-lysine and -arginine residues on both histone and other proteins by specific "reader" elements is important for chromatin regulation, gene expression, and control of cell-cycle progression. Recently the crucial role of these reader proteins in cancer development and dedifferentiation has emerged, owing to the increased interest among the scientific community. The methyl-lysine and -arginine readers are a large and very diverse set of effector proteins and targeting them with small molecule probes in drug discovery will inevitably require a detailed understanding of their structural biology and mechanism of binding. In the following review, the critical elements of methyl-lysine and -arginine recognition will be summarized with respect to each protein family and initial results in assay development, probe design, and drug discovery will be highlighted.

SUBMITTER: Herold JM

PROVIDER: S-EPMC3229088 | biostudies-literature | 2011

REPOSITORIES: biostudies-literature

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Drug discovery toward antagonists of methyl-lysine binding proteins.

Herold J Martin JM Ingerman Lindsey A LA Gao Cen C Frye Stephen V SV

Current chemical genomics 20110822

The recognition of methyl-lysine and -arginine residues on both histone and other proteins by specific "reader" elements is important for chromatin regulation, gene expression, and control of cell-cycle progression. Recently the crucial role of these reader proteins in cancer development and dedifferentiation has emerged, owing to the increased interest among the scientific community. The methyl-lysine and -arginine readers are a large and very diverse set of effector proteins and targeting them ...[more]

PMID: 22145013

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