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Article
Development of an 18F-labeled anti-human CD8 VHH for same-day immunoPET imaging
Cancer immunotherapies (CITs) have revolutionized the treatment of certain cancers, but many patients fail to respond or relapse from current therapies, prompting the need for new CIT agents. CD8+ T cells play a ...
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Article
Correction to: Preclinical development of ZED8, an 89Zr immuno‑PET reagent for monitoring tumor CD8 status in patients undergoing cancer immunotherapy
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Article
Preclinical development of ZED8, an 89Zr immuno-PET reagent for monitoring tumor CD8 status in patients undergoing cancer immunotherapy
ZED8 is a novel monovalent antibody labeled with zirconium-89 for the molecular imaging of CD8. This work describes nonclinical studies performed in part to provide rationale for and to inform expectations in ...
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Article
A BCMA/CD16A bispecific innate cell engager for the treatment of multiple myeloma
Despite the recent progress, multiple myeloma (MM) is still essentially incurable and there is a need for additional effective treatments with good tolerability. RO7297089 is a novel bispecific BCMA/CD16A-dire...
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Article
Open AccessTrastuzumab does not bind rat or mouse ErbB2/neu: implications for selection of non-clinical safety models for trastuzumab-based therapeutics
Assessment of non-clinical safety signals relies on understanding species selectivity of antibodies. This is particularly important with antibody–drug conjugates, where it is key to determine target-dependent ...
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Article
Water molecules in protein–ligand interfaces. Evaluation of software tools and SAR comparison
Targeting the interaction with or displacement of the ‘right’ water molecule can significantly increase inhibitor potency in structure-guided drug design. Multiple computational approaches exist to predict whi...
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Article
Structural basis for dual-mode inhibition of the ABC transporter MsbA
The movement of core-lipopolysaccharide across the inner membrane of Gram-negative bacteria is catalysed by an essential ATP-binding cassette transporter, MsbA. Recent structures of MsbA and related transporte...
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Article
An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells
KDM5 histone demethylases promote the survival of drug-tolerant persister (DTP) cells in certain cancers. CPI-455, a chemical probe specific for KDM5, elevates cellular H3K4 methylation levels and reduces DTP ...
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Article
Structure of mammalian poly(ADP-ribose) glycohydrolase reveals a flexible tyrosine clasp as a substrate-binding element
Poly ADP-ribosylation regulates cellular processes such as genomic stability maintenance, transcription and cell death. The structure of a mammalian poly(ADP-ribose) glycohydrolase gives insight into the enzym...
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Article
Structural insights into the stereochemistry of the cyclooxygenase reaction
Cyclooxygenases are bifunctional enzymes that catalyse the first committed step in the synthesis of prostaglandins, thromboxanes and other eicosanoids1,2,3. The two known cyclooxygenases isoforms share a high deg...
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Article
Visualizing DNA replication in a catalytically active Bacillus DNA polymerase crystal
DNA polymerases copy DNA templates with remarkably high fidelity, checking for correct base-pair formation both at nucleotide insertion and at subsequent DNA extension steps1,2,3. Despite extensive biochemical, g...
