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A phenotypic screen with Trypanosoma brucei for discovering small molecules that target the SLiM?binding pocket of proliferating cell nuclear antigen orthologs

Chemical Biology and Drug Design

Abstract Proliferating cell nuclear antigen (PCNA) is a homo-trimeric protein complex that clamps around DNA to tether DNA polymerases to the template during replication and serves as a hub for many other interacting proteins. The assay design is to discover bioactive small molecules that restore proliferation in T. brucei

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A Cross-Functional Mindset in DMPK

Drug Hunter

researching DNA photoproducts related to skin cancer. Her interest in research landed her a job at Genentech, where she focused on ADCs—and learned other skills critical to her career. It could have been some residual DNA, or maybe a protein, but they knew it was something big due to the 24 kDa change in mass of the ADC.

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Unlocking Undruggable Targets: Shifting Paradigms in Modern Drug Discovery

DrugBank

Researchers would sift through natural extracts , hoping to stumble upon a compound that exhibited beneficial effects. In fact, it's one of the most exciting areas in drug research today. With billions in funding and innovative research, we're starting to see strategies that can tackle these tough targets.

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The Future of Drug Discovery: Tackling the Undruggable with New Biotechnologies

DrugBank

These multifunctional small molecules are like tiny spies, hijacking the body’s natural protein degradation system to remove unwanted proteins. Multifunctional Small Molecules and Peptides Beyond PROTACs, there are other exciting tools in the new drug discovery toolbox.

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Antibody-drug conjugates payloads: then, now and next

Drug Target Review

The research community pressed on, turning to novel compounds that were substantially more potent than those used in the first generation. 2 In response, DNA-damaging agents that could target the entire cell cycle received renewed attention as ADC payloads.

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DNA Barcodes Could Streamline Search for New Drugs to Combat Cancer

NIH Director's Blog: Drug Discovery

A little more than a decade ago, researchers began adapting a familiar commercial concept to genomics: the barcode. Instead of the black, printed stripes of the Universal Product Codes (UPCs) that we see on everything from package deliveries to clothing tags, they used short, unique snippets of DNA to label cells.

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From Impossible to Inevitable: Transforming Undruggable Targets

DrugBank

In the dynamic world of drug discovery, the notion of "undruggable" targets presents both a significant challenge and an intriguing frontier for researchers and pharmaceutical companies. Here, researchers are looking at allosteric modulation—hitting different parts of the molecule to increase selectivity.