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Center for the Development of Therapeutics

Identification of small molecule inhibitors of PPM1D using an integrated drug discovery platform.

Shaw S, Jiang W, Rush J, et al. Identification of small molecule inhibitors of PPM1D using an integrated drug discovery platform. iScience. 2025;28(3):112069. doi:10.1016/j.isci.2025.112069

Cell Painting for cytotoxicity and mode-of-action analysis in primary human hepatocytes.

Ewald JD, Titterton KL, Bäuerle A, et al. Cell Painting for cytotoxicity and mode-of-action analysis in primary human hepatocytes. bioRxiv : the preprint server for biology. 2025. doi:10.1101/2025.01.22.634152

A non-hormonal reversible contraceptive targeting GSK3α, a protein kinase, essential for epididymal sperm maturation.

Kabi M, Khamamkar A, Kyei-Baffour K, Weïwer M, Vijayaraghavan S, Dey S. A non-hormonal reversible contraceptive targeting GSK3α, a protein kinase, essential for epididymal sperm maturation. Andrology. 2025. doi:10.1111/andr.13838

Disrupted uromodulin trafficking is rescued by targeting TMED cargo receptors.

Bazua-Valenti S, Brown MR, Zavras J, et al. Disrupted uromodulin trafficking is rescued by targeting TMED cargo receptors. The Journal of clinical investigation. 2024;134(24). doi:10.1172/JCI180347

Three million images and morphological profiles of cells treated with matched chemical and genetic perturbations.

Chandrasekaran SN, Cimini BA, Goodale A, et al. Three million images and morphological profiles of cells treated with matched chemical and genetic perturbations. Nature methods. 2024. doi:10.1038/s41592-024-02241-6

The benefits of translating biomedical research at drug discovery institutes.

Huggins DJ, Baell J, Brennan PE, Burgin A, Scott DE. The benefits of translating biomedical research at drug discovery institutes. Nature reviews. Drug discovery. 2024. doi:10.1038/d41573-024-00142-z

BRD-810 is a highly selective MCL1 inhibitor with optimized in vivo clearance and robust efficacy in solid and hematological tumor models.

Rauh U, Wei G, Serrano-Wu M, et al. BRD-810 is a highly selective MCL1 inhibitor with optimized in vivo clearance and robust efficacy in solid and hematological tumor models. Nature cancer. 2024. doi:10.1038/s43018-024-00814-0

Targeting the aminopeptidase ERAP enhances antitumor immunity by disrupting the NKG2A-HLA-E inhibitory checkpoint.

Tsao HW, Anderson S, Finn KJ, et al. Targeting the aminopeptidase ERAP enhances antitumor immunity by disrupting the NKG2A-HLA-E inhibitory checkpoint. Immunity. 2024. doi:10.1016/j.immuni.2024.10.013

Activating point mutations in the MET kinase domain represent a unique molecular subset of lung cancer and other malignancies targetable with MET inhibitors.

Pecci F, Nakazawa S, Ricciuti B, et al. Activating point mutations in the MET kinase domain represent a unique molecular subset of lung cancer and other malignancies targetable with MET inhibitors. Cancer discovery. 2024. doi:10.1158/2159-8290.CD-23-1217

Mapping MAVE data for use in human genomics applications.

Arbesfeld JA, Da EY, Stevenson JS, et al. Mapping MAVE data for use in human genomics applications. bioRxiv : the preprint server for biology. 2024. doi:10.1101/2023.06.20.545702