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Stapled α−helical peptide drug development: A potent dual inhibitor of MDM2 and MDMX for p53-dependent cancer therapy
Significance Stapled α−helical peptides have emerged as a promising new modality for a wide range of therapeutic targets. Here, we describe the development of a stapled α−helical peptide leadExpand
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Functional, Biophysical, and Structural Bases for Antibacterial Activity of Tigecycline
ABSTRACT Tigecycline is a novel glycylcycline antibiotic that possesses broad-spectrum activity against many clinically relevant species of bacterial pathogens. The mechanism of action of tigecyclineExpand
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Identification of a New Member of the Tryptase Family of Mouse and Human Mast Cell Proteases Which Possesses a Novel COOH-terminal Hydrophobic Extension*
Mapping of the tryptase locus on chromosome 17 revealed a novel gene 2.3 kilobase 3′ of the mouse mast cell protease (mMCP) 6 gene. This 3.7-kilobase gene encodes the first example of a protease inExpand
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Modeling mutations in protein structures
We describe an automated method for the modeling of point mutations in protein structures. The protein is represented by all non‐hydrogen atoms. The scoring function consists of several types ofExpand
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Lead optimization via high-throughput molecular docking.
Structure-based lead optimization approaches are increasingly playing a role in the drug-discovery process. Recent advances in 'high-throughput' molecular docking methods and examples of theirExpand
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Influence of a NH2‐terminal extension on the activity of KTX2, a K+ channel blocker purified from Androctonus australis scorpion venom
A cDNA encoding a short polypeptide blocker of K+ channels, kaliotoxin 2 (KTX2), from the venom of the North African scorpion Androctonus australis was expressed in the periplasmic space ofExpand
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A general approach to site-specific antibody drug conjugates
Significance Here we demonstrate the ability to genetically incorporate nonnative amino acids into proteins in mammalian cells using both transient and stable platform expression systems that provideExpand
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Formation of Enzymatically Active, Homotypic, and Heterotypic Tetramers of Mouse Mast Cell Tryptases
Mouse mast cell protease (mMCP) 6 and mMCP-7 are homologous tryptases stored in granules as macromolecular complexes with heparin and/or chondroitin sulfate E containing serglycin proteoglycans. WhenExpand
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Mouse Mast Cell Protease 9, a Novel Member of the Chromosome 14 Family of Serine Proteases that is Selectively Expressed in Uterine Mast Cells*
Mouse mast cell protease (mMCP) 1, mMCP-2, mMCP-4, and mMCP-5 are members of a family of related serine proteases whose genes reside within an ∼850 kilobase (kb) complex on chromosome 14 that doesExpand
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CONFIRM: connecting fragments found in receptor molecules
A novel algorithm for the connecting of fragment molecules is presented and validated for a number of test systems. Within the CONFIRM (Connecting Fragments Found in Receptor Molecules) approach aExpand
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