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Researchers devise new way to target and correct disease-related proteins

Broad Institute

Also featured are the FKBP12 binding motif (light blue triangle), the DNA barcode (red double helix), and the combinatorial library element (red hexagon). Related groups Xavier lab Over the past two decades, large genetic studies have linked tens of thousands of DNA variants to thousands of human traits and diseases.

Disease 139
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Reviewing the IDH1 Mutation‐Mediated Mechanism of Drug Resistance and Revisiting Its Overcoming Strategies

Chemical Biology and Drug Design

At present, there are few studies on the drug resistance of mIDH1 inhibitors. Currently, the FDA has granted approval for the use of the small molecule inhibitor Ivosidenib (AG-120) in the treatment of IDH1-mutated AML and cholangiocarcinoma.

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How to find a drug: the past, present and future of small molecule drug discovery?

DrugBaron

Despite the current hype around so called “advanced therapies”, which range from gene editing to cell therapies, and the inexorable advance of biologic therapeutics such as monoclonal antibodies, even in 2022 the majority of drugs in development and reaching patients are still small organic molecules.

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Nucleophilic covalent ligand discovery for the cysteine redoxome

Covalent Modifiers

Here we present a global map of a human sulfenome that is susceptible to covalent modification by members of a nucleophilic fragment library. We further show that members of our nucleophilic fragment library can impair functional protein–protein interactions involved in nuclear oncoprotein transport and DNA damage repair.

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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. Beyond Proteins: DNA and RNA Frontier The story doesn’t end with proteins.

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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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Unlocking a new molecular space in rapid drug discovery

Drug Target Review

Technologies for the rapid and efficient testing of small molecules and biologics have greatly accelerated drug discovery. Intermediate-sized molecules such as macrocycles combining the beneficial properties of both small molecules and biologics may enable the targeting of currently undruggable targets.