6 research outputs found

    Advances in triterpene drug discovery

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    Triterpenes are structurally complex natural products with promising therapeutic properties. Recalcitrance to chemical synthesis has hindered their use in drug development. Recent advances now make it possible to access and harness triterpene structural diversity using engineering biology approaches, enabling the discovery and optimisation of a new generation of drug leads

    Light-activated azobenzene peptide inhibitor of the PD-1/PD-L1 interaction

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    Inhibiting the PD-1/PD-L1 protein–protein interaction is a key immunotherapy for cancer. Antibodies dominate the clinical space but are costly, with limited applicability and immune side effects. We developed a photo-controlled azobenzene peptide that selectively inhibits the PD-1/PD-L1 interaction when in the cis isomer only. Activity is demonstrated in in vitro and cellular assays

    Borylation via iridium catalysed C–H activation: a new concise route to duocarmycin derivatives

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    The synthesis of the ethyl ester analogue of the ultrapotent antitumour antibiotic seco-duocarmycin SA has been achieved in eleven linear steps from commercially available starting materials. The DSA alkylation subunit can be made in ten linear steps from the same precursor. The route involves C–H activation at the equivalent of the C7 position on indole leading to a borylated intermediate 9 that is stable enough for peptide coupling reactions but can be easily converted to the free hydroxyl analogue

    Multi-laboratory compilation of atmospheric carbon dioxide data for the period 1957-2023; obspack_co2_1_GLOBALVIEWplus_v10.0_2024-09-26

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    This product is constructed using the Observation Package (ObsPack) framework [Masarie et al., 2014; www.earth-syst-sci-data.net/6/375/2014/]. The framework is designed to bring together atmospheric greenhouse gas (GHG) observations from a variety of sampling platforms, prepare them with specific applications in mind, and package and distribute them in a self-consistent and well-documented product. ObsPack products are intended to support GHG budget studies and represent a new generation of cooperative value-added GHG data products. This product includes 625 atmospheric carbon dioxide datasets derived from observations made by 79 laboratories from 28 countries. Data for the period 1957-2023 (where available) are included

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