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  1. No Access

    Article

    Novel Multiplexed High Throughput Screening of Selective Inhibitors for Drug-Metabolizing Enzymes Using Human Hepatocytes

    Selective chemical inhibitors are critical for reaction phenoty** to identify drug-metabolizing enzymes that are involved in the elimination of drug candidates. Although relatively selective inhibitors are a...

    Jianhua Liu, Daria Vernikovskaya, Gary Bora, Anthony Carlo… in The AAPS Journal (2024)

  2. No Access

    Article

    Characterization of CYP3A5 Selective Inhibitors for Reaction Phenoty** of Drug Candidates

    CYP3A is one of the most important classes of enzymes and is involved in the metabolism of over 70% drugs. While several selective CYP3A4 inhibitors have been identified, the search for a selective CYP3A5 inhi...

    Jie Chen, Lloyd Wei Tat Tang, Samantha Jordan, Makayla Harrison… in The AAPS Journal (2024)

  3. No Access

    Article

    Snapshots and ensembles of BTK and cIAP1 protein degrader ternary complexes

    Heterobifunctional chimeric degraders are a class of ligands that recruit target proteins to E3 ubiquitin ligases to drive compound-dependent protein degradation. Advancing from initial chemical tools, protein...

    James Schiemer, Reto Horst, Yilin Meng, Justin I. Montgomery… in Nature Chemical Biology (2021)

  4. No Access

    Protocol

    Design of Cyclic Peptides as Protein Recognition Motifs

    Protein–protein interactions are ubiquitous, essential to almost all known biological processes, and offer attractive opportunities for therapeutic intervention. Linear peptide drugs, however, can be applied t...

    Ye Che in Cyclic Peptide Design (2019)

  5. No Access

    Article

    Detection of conformation types of cyclosporin retaining intramolecular hydrogen bonds by mass spectrometry

    Cyclosporin is a family of neutral cyclic undecapeptides widely used for the prevention of organ transplant rejection and controlling viral infection. The equilibrium of conformations assumed by cyclosporin A ...

    Suk-Joon Hyung, **dong Feng, Ye Che… in Analytical and Bioanalytical Chemistry (2014)

  6. No Access

    Protocol

    Chemogenomics with Protein Secondary-Structure Mimetics

    During molecular recognition of proteins in biological systems, helices, reverse turns, and β-sheets are dominant motifs. Often there are therapeutic reasons for blocking such recognition sites, and significan...

    Garland R. Marshall, Daniel J. Kuster, Ye Che in Chemogenomics (2009)