Cancer Therapeutics
Recent submissions
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Development and Validation of a New BAG-1L-Specific Antibody to Quantify BAG-1L Protein Expression in Advanced Prostate Cancer.
(ELSEVIER SCIENCE INC, 2023-08-29)BCL-2-associated athanogene-1L (BAG-1L) is a critical co-regulator that binds to and enhances the transactivation function of the androgen receptor, leading to prostate cancer development and progression. Studies investigating ... -
Developing RAS-binding antibody-derived hit compounds
(Institute of Cancer Research (University Of London), 2023-09-27) -
Hematopoietic Stem Cell (HSC)-Independent Progenitors Are Susceptible to Mll-Af9-Induced Leukemic Transformation.
(MDPI, 2023-07-14)Infant acute myeloid leukemia (AML) is a heterogeneous disease, genetically distinct from its adult counterpart. Chromosomal translocations involving the KMT2A gene (MLL) are especially common in affected infants of less ... -
Expanding Chemical Probe Space: Quality Criteria for Covalent and Degrader Probes.
(American Chemical Society (ACS), 2023-07-27)Within druggable target space, new small-molecule modalities, particularly covalent inhibitors and targeted degraders, have expanded the repertoire of medicinal chemists. Molecules with such modes of action have a large ... -
Prospective Evaluation of Whole-Body MRI versus FDG PET/CT for Lesion Detection in Participants with Myeloma.
(RADIOLOGICAL SOC NORTH AMERICA (RSNA), 2021-09-01)Purpose To compare disease detection of myeloma using contemporary whole-body (WB) MRI and fluorine 18 (18F) fluorodeoxyglucose (FDG) PET/CT protocols and to correlate imaging with laboratory estimates of disease burden, ... -
Immuno-PET Imaging of Tumour PD-L1 Expression in Glioblastoma.
(MDPI, 2023-06-09)There is no established method to assess the PD-L1 expression in brain tumours. Therefore, we investigated the suitability of affibody molecule (ZPD-L1) radiolabelled with F-18 (Al18F) and Ga-68 to measure the expression ... -
iTAG an optimized IMiD-induced degron for targeted protein degradation in human and murine cells.
(CELL PRESS, 2023-07-21)To address the limitation associated with degron based systems, we have developed iTAG, a synthetic tag based on IMiDs/CELMoDs mechanism of action that improves and addresses the limitations of both PROTAC and previous ... -
Genomic and Epigenetic Changes Drive Aberrant Skeletal Muscle Differentiation in Rhabdomyosarcoma.
(MDPI, 2023-05-18)Rhabdomyosarcoma (RMS), the most common soft-tissue sarcoma in children and adolescents, represents an aberrant form of skeletal muscle differentiation. Both skeletal muscle development, as well as regeneration of adult ... -
Dual inhibition of EZH2 and G9A/GLP histone methyltransferases by HKMTI-1-005 promotes differentiation of acute myeloid leukemia cells.
(FRONTIERS MEDIA SA, 2023-03-23)All-trans-retinoic acid (ATRA)-based differentiation therapy of acute promyelocytic leukemia (APL) represents one of the most clinically effective examples of precision medicine and the first example of targeted oncoprotein ... -
HSF1 Pathway Inhibitor Clinical Candidate (CCT361814/NXP800) Developed from a Phenotypic Screen as a Potential Treatment for Refractory Ovarian Cancer and Other Malignancies.
(AMER CHEMICAL SOC, 2023-04-27)CCT251236 1, a potent chemical probe, was previously developed from a cell-based phenotypic high-throughput screen (HTS) to discover inhibitors of transcription mediated by HSF1, a transcription factor that supports ... -
Discovery of an In Vivo Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones.
(AMER CHEMICAL SOC, 2023-04-27)B-cell lymphoma 6 (BCL6) is a transcriptional repressor and oncogenic driver of diffuse large B-cell lymphoma (DLBCL). Here, we report the optimization of our previously reported tricyclic quinolinone series for the ... -
Liquid biopsy for children with central nervous system tumours: Clinical integration and technical considerations.
(FRONTIERS MEDIA SA, 2022-11-16)Circulating cell-free DNA (cfDNA) analysis has the potential to revolutionise the care of patients with cancer and is already moving towards standard of care in some adult malignancies. Evidence for the utility of cfDNA ... -
Lorlatinib with or without chemotherapy in ALK-driven refractory/relapsed neuroblastoma: phase 1 trial results.
(NATURE PORTFOLIO, 2023-05-01)Neuroblastomas harbor ALK aberrations clinically resistant to crizotinib yet sensitive pre-clinically to the third-generation ALK inhibitor lorlatinib. We conducted a first-in-child study evaluating lorlatinib with and ... -
Shortwave Infrared Imaging Enables High-Contrast Fluorescence-Guided Surgery in Neuroblastoma.
(AMER ASSOC CANCER RESEARCH, 2023-06-15)UNLABELLED: Fluorescence-guided surgery is set to play a pivotal role in the intraoperative management of pediatric tumors. Shortwave infrared imaging (SWIR) has advantages over conventional near-infrared I (NIR-I) imaging ... -
Intracellular Antibodies for Drug Discovery and as Drugs of the Future.
(MDPI, 2023-03-16)The application of antibodies in cells was first shown in the early 1990s, and subsequently, the field of intracellular antibodies has expanded to encompass antibody fragments and their use in target validation and as ... -
Modular Synthesis of Semiconducting Graft Copolymers to Achieve "Clickable" Fluorescent Nanoparticles with Long Circulation and Specific Cancer Targeting.
(WILEY-V C H VERLAG GMBH, 2023-03-11)Semiconducting polymer nanoparticles (SPNs) are explored for applications in cancer theranostics because of their high absorption coefficients, photostability, and biocompatibility. However, SPNs are susceptible to aggregation ... -
Harnessing the power of cryo electron microscopy to visualise a full-length kinesin KIFC1 (HSET)
(Institute of Cancer Research (University Of London), 2023-05-30)Cancer cells are known to exhibit a phenomenon typically known as centrosome amplification (CA), which is responsible for multipolar spindle formation during mitosis. This severely impairs cytokinesis and could hence prove ... -
Design and synthesis of bifunctional molecules for directing phosphorylation
(Institute of Cancer Research (University Of London), 2023-05-04)The field of bifunctional molecules such as PROTAC, DUBTAC and PhoRC has demonstrated that inducing proximity between two protein complexes is sufficient to redirect post-translational modifications (PTMs), and effect ... -
Molecular profiling of cell free DNA in patients with paediatric solid tumours
(Institute of Cancer Research (University Of London), 2023-05-02)Tumour tissue profiling studies show that a substantial proportion of paediatric cancer patients have potentially actionable alterations and minimally invasive molecular profiling test using cell free DNA (cfDNA) could ... -
Discovery of 2-(3-Benzamidopropanamido)thiazole-5-carboxylate Inhibitors of the Kinesin HSET (KIFC1) and the Development of Cellular Target Engagement Probes.
(AMER CHEMICAL SOC, 2023-02-23)The existence of multiple centrosomes in some cancer cells can lead to cell death through the formation of multipolar mitotic spindles and consequent aberrant cell division. Many cancer cells rely on HSET (KIFC1) to cluster ...
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