Search Results - "Rectenwald, Justin M"
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Design and Construction of a Focused DNA-Encoded Library for Multivalent Chromatin Reader Proteins
Published in Molecules (Basel, Switzerland) (22-02-2020)“…Chromatin structure and function, and consequently cellular phenotype, is regulated in part by a network of chromatin-modifying enzymes that place…”
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Discovery of hit compounds for methyl-lysine reader proteins from a target class DNA-encoded library
Published in SLAS discovery (01-12-2022)“…•Focused DNA-encoded libraries (DELs) are effective in target class hit discovery.•Reader domains of five methyl-lysine reader proteins screened using a…”
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Discovery of Potent Peptidomimetic Antagonists for Heterochromatin Protein 1 Family Proteins
Published in ACS omega (11-01-2022)“…The heterochromatin protein 1 (HP1) sub-family of CBX chromodomains are responsible for the recognition of histone H3 lysine 9 tri-methyl (H3K9me3)-marked…”
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Degradation of Polycomb Repressive Complex 2 with an EED-Targeted Bivalent Chemical Degrader
Published in Cell chemical biology (16-01-2020)“…Protein degradation via the use of bivalent chemical degraders provides an alternative strategy to block protein function and assess the biological roles of…”
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PROTAC Linkerology Leads to an Optimized Bivalent Chemical Degrader of Polycomb Repressive Complex 2 (PRC2) Components
Published in ACS chemical biology (17-03-2023)“…Bivalent chemical degraders, otherwise known as proteolysis-targeting chimeras (PROTACs), have proven to be an efficient strategy for targeting overexpressed…”
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Reprogramming CBX8-PRC1 function with a positive allosteric modulator
Published in Cell chemical biology (21-04-2022)“…Canonical targeting of Polycomb repressive complex 1 (PRC1) to repress developmental genes is mediated by cell-type-specific, paralogous chromobox (CBX)…”
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A Peptidomimetic Ligand Targeting the Chromodomain of MPP8 Reveals HRP2’s Association with the HUSH Complex
Published in ACS chemical biology (17-09-2021)“…The interpretation of histone post-translational modifications (PTMs), specifically lysine methylation, by specific classes of “reader” proteins marks an…”
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Characterization of a Radical Intermediate in Lipoyl Cofactor Biosynthesis
Published in Journal of the American Chemical Society (21-10-2015)“…Lipoyl synthase (LipA) catalyzes the final step in the biosynthesis of the lipoyl cofactor, the insertion of two sulfur atoms at C6 and C8 of an n-octanoyl…”
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A General TR-FRET Assay Platform for High-Throughput Screening and Characterizing Inhibitors of Methyl-Lysine Reader Proteins
Published in SLAS discovery (01-07-2019)“…Chromatin regulatory complexes localize to specific sites via recognition of posttranslational modifications (PTMs) on N-terminal tails of histone proteins…”
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Technology Development for Inhibitor Discovery of Chromatin Associated Proteins Linked to Lysine Methylation
Published 01-01-2020“…The identification of molecules that tightly bind to therapeutically relevant targets remains one of the biggest challenges in biomedical research. Continued…”
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Dissertation