Discovery of highly selective inhibitors of calmodulin-dependent kinases that restore insulin sensitivity in the diet-induced obese in vivo mouse model.

Fromont, Christophe; Atzori, Alessio; Kaur, Divneet; Hashmi, Lubna; Greco, Graziella; Cabanillas, Alejandro; Nguyen, Huy Van; Jones, D. Heulyn; Garzón, Miguel; Varela, Ana; Stevenson, Brett; Iacobini, Greg; Lenoir, Marc; Rajesh, Sundaresan; Box, Clare; Kumar, Jitendra; Grant, Paige; Novitskaia, Vera; Morgan, Juliet; Sorrell, Fiona; Redondo, Clara; Kramer, Andreas; Harris, C. John; Leighton, Brendan; Vickers, Steven; Cheetham, Sharon; Kenyon, Colin; Grabowska, Anna M.; Overduin, Michael; Berditchevski, Fedor; Weston, Chris J; Knapp, Stefan; Fischer, Peter M.; Butterworth, Sam

doi:10.1021/acs.jmedchem.9b01803

All Outputs (8)

Modulation of the pre-metastatic bone niche: molecular changes mediated by bone-homing prostate cancer extracellular vesicles (2024)
Journal Article

Prostate cancer (PCa) is a leading male malignancy worldwide, often progressing to bone metastasis, with limited curative options. Extracellular vesicles (EVs) have emerged as key players in cancer communication and metastasis, promoting the formatio... Read More about Modulation of the pre-metastatic bone niche: molecular changes mediated by bone-homing prostate cancer extracellular vesicles.

Free drug and ROS-responsive nanoparticle delivery of synergistic doxorubicin and olaparib combinations to triple negative breast cancer models (2024)
Journal Article

Combinations of the topoisomerase II inhibitor doxorubicin and the poly (ADP-ribose) polymerase inhibitor olaparib offer potential drug-drug synergy for the treatment of triple negative breast cancers (TNBC). In this study we performed in vitro scree... Read More about Free drug and ROS-responsive nanoparticle delivery of synergistic doxorubicin and olaparib combinations to triple negative breast cancer models.

Chain-extension in hyperbranched polymers alters tissue distribution and cytotoxicity profiles in orthotopic models of triple negative breast cancers (2023)
Journal Article

The therapeutic efficacy of nanomedicines is highly dependent on their access to target sites in the body, and this in turn is markedly affected by their size, shape and transport properties in tissue. Although there have been many studies in this ar... Read More about Chain-extension in hyperbranched polymers alters tissue distribution and cytotoxicity profiles in orthotopic models of triple negative breast cancers.

Application of a 3D hydrogel-based model to replace use of animals for passaging patient-derived xenografts (2023)
Journal Article

Purpose This 3D in vitro cancer model for propagation of patient-derived cells, using a synthetic self-assembling peptide gel, allows the formation of a fully characterised, tailorable tumour microenvironment. Unlike many existing 3D cancer models,... Read More about Application of a 3D hydrogel-based model to replace use of animals for passaging patient-derived xenografts.

Targeting FGFRs Using PD173074 as a Novel Therapeutic Strategy in Cholangiocarcinoma (2023)
Journal Article

Cholangiocarcinoma (CCA) is an architecturally complex tumour with high heterogeneity. Discovery at later stages makes treatment challenging. However, the lack of early detection methodologies and the asymptomatic nature of CCA make early diagnosis m... Read More about Targeting FGFRs Using PD173074 as a Novel Therapeutic Strategy in Cholangiocarcinoma.

Clinically Translatable Transcrocetin Delivery Platform for Correction of Tumor Hypoxia and Enhancement of Radiation Therapy Effects (2023)
Journal Article

Improving the tumor reoxygenation to sensitize the tumor to radiation therapy is a cornerstone in radiation oncology. Here, the pre‐clinical development of a clinically transferable liposomal formulation encapsulating trans sodium crocetinate (NP TSC... Read More about Clinically Translatable Transcrocetin Delivery Platform for Correction of Tumor Hypoxia and Enhancement of Radiation Therapy Effects.

Targeting Mre11 overcomes platinum resistance and induces synthetic lethality in XRCC1 deficient epithelial ovarian cancers (2022)
Journal Article

Platinum resistance is a clinical challenge in ovarian cancer. Platinating agents induce DNA damage which activate Mre11 nuclease directed DNA damage signalling and response (DDR). Upregulation of DDR may promote chemotherapy resistance. Here we have... Read More about Targeting Mre11 overcomes platinum resistance and induces synthetic lethality in XRCC1 deficient epithelial ovarian cancers.

Discovery of highly selective inhibitors of calmodulin-dependent kinases that restore insulin sensitivity in the diet-induced obese in vivo mouse model. (2020)
Journal Article