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Residue-Selective Inhibitors Discovery via Covalent DNA-Encoded Chemical Libraries with Diverse Warheads

Covalent Modifiers

5c01712 Covalent small molecule drugs have emerged as a crucial support in precision therapy due to their high selectivity and robust potency. These findings suggest that our work could potentially expand the target space of covalent drugs and promote precision therapy by harnessing the power of the CoDELs.

DNA
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Synthesis and Investigation of Peptide–Drug Conjugates Comprising Camptothecin and a Human Protein‐Derived Cell‐Penetrating Peptide

Chemical Biology and Drug Design

ABSTRACT Drug targeting strategies, such as peptidedrug conjugates (PDCs), have arisen to combat the issue of off-target toxicity that is commonly associated with chemotherapeutic small molecule drugs.

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The future of CNS drug development: signs of real progress

Drug Target Review

2 A raft of emerging therapeutic modalities sits at the centre of this boom, spanning advanced biologics, engineered platforms and next-generation small molecules. This protective barrier prevents more than 98 percent of small-molecule drugs and all macromolecular therapeutics 3 from accessing the brain.

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How GPCR-targeting therapies are advancing the fight against inflammatory disease

Drug Target Review

Targeting GPCRs to fight inflammatory diseases GPCR-targeting drugs are well known therapies for a range of disease types, including cardio-metabolic, central nervous system and endocrinological disorders. GPCR-targeting therapies such as DT-9046 represent a compelling opportunity in that respect, with major clinical and commercial potential.

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Synthesis Methods and Therapeutic Journey of Carprofen and Its Derivatives: A Review

Chemical Biology and Drug Design

Although it is currently only used in veterinary therapy, carprofen proves to be a molecule with a versatile therapeutic potential for human pharmacotherapy. Moreover, the molecule is a target in the drug discovery process for the development of new bioactive compounds.

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Shifting the ADC focus from antibody to payload

Drug Target Review

With an extensive background in small molecule chemistry, bioconjugation and protein science, these expert teams are leading efforts to place payload development at the centre of ADC innovation. The ADC itself is not necessarily a large molecule – it’s a small molecule with aspects of a large molecule, and vice versa.

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PALAZESTRANT

New Drug Approvals

It is a small molecule with a dual mechanism of action, acting as both a complete estrogen receptor antagonist and a selective estrogen receptor degrader (SERD). Combination Therapy: Palazestrant is being evaluated in combination with other drugs like CDK4/6 inhibitors (e.g., ribociclib).