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Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo.
(AMER CHEMICAL SOC, 2022-06-23)
The transcriptional repressor BCL6 is an oncogenic driver found to be deregulated in lymphoid malignancies. Herein, we report the optimization of our previously reported benzimidazolone molecular glue-type degrader CCT369260 ...
Chromatin regulation of transcriptional enhancers and cell fate by the Sotos syndrome gene NSD1.
(CELL PRESS, 2023-07-20)
Nuclear receptor-binding SET-domain protein 1 (NSD1), a methyltransferase that catalyzes H3K36me2, is essential for mammalian development and is frequently dysregulated in diseases, including Sotos syndrome. Despite the ...
Uridine-derived ribose fuels glucose-restricted pancreatic cancer.
(NATURE PORTFOLIO, 2023-06-01)
Pancreatic ductal adenocarcinoma (PDA) is a lethal disease notoriously resistant to therapy1,2. This is mediated in part by a complex tumour microenvironment3, low vascularity4, and metabolic aberrations5,6. Although altered ...
Beyond the Driver Mutation: Immunotherapies in Gastrointestinal Stromal Tumors.
(FRONTIERS MEDIA SA, 2021-08-20)
Gastrointestinal stromal tumors (GISTs) are a subtype of soft tissue sarcoma (STS), and have become a concept of oncogenic addiction and targeted therapies.The large majority of these tumors develop after a mutation in KIT ...
Antibodies against endogenous retroviruses promote lung cancer immunotherapy.
(NATURE PORTFOLIO, 2023-04-20)
B cells are frequently found in the margins of solid tumours as organized follicles in ectopic lymphoid organs called tertiary lymphoid structures (TLS)1,2. Although TLS have been found to correlate with improved patient ...
CD4 T cell dynamics shape the immune response to combination oncolytic herpes virus and BRAF inhibitor therapy for melanoma.
(BMJ PUBLISHING GROUP, 2022-03-01)
BACKGROUND: Combination herpes simplex virus (HSV) oncolytic virotherapy and BRAF inhibitors (BRAFi) represent promising immunogenic treatments for BRAF mutant melanoma, but an improved understanding of the immunobiology ...
GENCODE 2021.
(OXFORD UNIV PRESS, 2021-01-08)
The GENCODE project annotates human and mouse genes and transcripts supported by experimental data with high accuracy, providing a foundational resource that supports genome biology and clinical genomics. GENCODE annotation ...
Fadraciclib (CYC065), a novel CDK inhibitor, targets key pro-survival and oncogenic pathways in cancer.
(PUBLIC LIBRARY SCIENCE, 2020-07-09)
Cyclin-dependent kinases (CDKs) contribute to the cancer hallmarks of uncontrolled proliferation and increased survival. As a result, over the last two decades substantial efforts have been directed towards identification ...
Antigen retrieval and clearing for whole-organ immunofluorescence by FLASH.
(NATURE RESEARCH, 2020-11-27)
Advances in light-sheet and confocal microscopy now allow imaging of cleared large biological tissue samples and enable the 3D appreciation of cell and protein localization in their native organ environment. However, the ...
Drugging the Undruggable: Advances on RAS Targeting in Cancer.
(MDPI, 2021-06-10)
Around 20% of all malignancies harbour activating mutations in RAS isoforms. Despite this, there is a deficiency of RAS-targeting agents licensed for therapeutic use. The picomolar affinity of RAS for GTP, and the lack of ...