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

Chemical Biology and Drug Design

Therefore, this article first summarizes terms of IDH1 function from the molecular mechanism of IDH1, the mechanism of mutation, and the metabolism of substances due to mutations. In addition, this article introduces representative mIDH1 inhibitors according to the differences of mutation sites.

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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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#ScienceSaturday: January 27, 2024

KIF1A

Rare Roundup KRIBB develops new gene therapy candidate for hereditary spastic paraplegia This week we’re flipping the format and starting with our Rare Roundup, after families contacted us with this article about a gene therapy candidate for hereditary spastic paraplegia.

Therapies 111
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The power of combinations in blood cancers

Drug Target Review

These regimens frequently include one or two small molecule inhibitors and immuno-oncology (IO) therapies, such as monoclonal antibodies and T-cell engagers. This article was written and developed by AstraZeneca.

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Driving Toward Nanopores

Codon

And unlike traditional DNA sequencers, which parse genetic material by breaking it up into fragments and interpreting it chunk-by-chunk, a nanopore device unspools a long strand of DNA and reads it all at once. A scientist can isolate DNA and load up a flow cell in fifteen minutes. Sign up to get articles from Asimov Press.

DNA 87
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Reaching cruising altitude: New discovery tools to target RNA

Dark Matter Blog

The majority of small molecule drugs induce their therapeutic effects by seeking out and binding to their intended target while avoiding most other molecules in the dense milieu of the cell interior. Our overall mission at Arrakis is to expand the set of “druggable” targets for small-molecule medicines to include RNA.

RNA 52
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Missing Metabolites

Metabolite Tales Blog

Trapping agents are described for reactive metabolites that could ordinarily be overlooked due to quenching with endogenous small molecules and protein nucleophiles. Journal of Medicinal Chemistry Article ASAP. Christopher, Robert S. Foti, Chungang Gu, S. Cyrus Khojasteh, Joyce Liu, Shuguang Ma, Bin Ma, R.