Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown +2 more
wiley +1 more source
The cervical cancer epidemic that screening has prevented in the UK.
BACKGROUND: Recent reports suggest that the reduction in mortality achieved by the UK national cervical screening programme is too small to justify its financial and psychosocial costs, except perhaps in a few high-risk women. METHODS: We analysed trends
Fletcher, Olivia +3 more
core +1 more source
Anosmin-1 modulates fibroblast growth factor receptor 1 signaling in human gonadotropin-releasing hormone olfactory neuroblasts through a heparan sulfate-dependent mechanism [PDF]
Defects of either anosmin-1 or fibroblast growth factor receptor 1 (FGFR1) are known to underlie hereditary Kallmann's syndrome (KS), a human disorder of olfactory and gonadotropin-releasing hormone (GnRH) neuronal ontogeny.
Bouloux, PM +8 more
core +1 more source
Patient‐derived head and neck squamous cell carcinoma (HNSCC) cells were genomically and cytogenetically characterized, revealing actionable alterations and chromosomal instability. Targeted therapies suppressed growth according to EGFR amplification or PIK3CA mutation status.
Kazue Ito +17 more
wiley +1 more source
Cytology‐First Diagnostic Workflow for Melanoma of Unknown Primary With Molecular Profiling
Cytology‑first diagnostic workflow for melanoma of unknown primary. Fine‑needle aspiration of an enlarged lymph node enables rapid cytologic evaluation and immunocytochemical confirmation of melanocytic lineage (SOX10). This early cytologic diagnosis facilitates timely surgical excision and comprehensive genomic profiling, supporting integrated ...
Hong Yu +3 more
wiley +1 more source
Dong-Wei Fu, Ai-Chun Liu Department of Hematology, Harbin Medical University Cancer Hospital, Harbin, Heilongjiang 150081, People’s Republic of ChinaCorrespondence: Ai-Chun LiuDepartment of Hematology, Harbin Medical University, Cancer Hospital ...
Fu DW, Liu AC
doaj
Relationship and predictive role of the dual expression of FGFR and IL-8 in metastatic renal cell carcinoma treated with targeted agents [PDF]
Background/Aim: The expression of IL-8 and FGFR has been related to prognosis and pathological features in renal cell carcinoma. We investigated the relationship between IL-8 and FGFR and the outcome in metastatic renal cell carcinoma (mRCC) patients ...
Carella, Consiglia +7 more
core +1 more source
Membrane‐type I metalloproteinase (MT1‐MMP): A key modifier of extracellular matrix microenvironment
MT1‐MMP: A cellular microenvironment modifier. MT1‐MMP is a major cellular microenvironment modifier, maintaining collagen homeostasis by degrading excess collagen (A), creating a migration path in motile cells such as cancer cells (B), modulating local microenvironmental signaling by cleaving transmembrane receptors (C), and destroying tissue ...
Yoshifumi Itoh, Masaki Inada
wiley +1 more source
Targeting RTK signaling pathways in cancer [PDF]
The RAS/MAP kinase and the RAS/PI3K/AKT pathways play a key role in the regulation of proliferation, differentiation and survival. The induction of these pathways depends on Receptor Tyrosine Kinases (RTKs) that are activated upon ligand binding.
Regad, T
core +1 more source
Design and synthesis of an erdafitinib-based selective FGFR2 degrader
This study aimed to develop a novel degrader capable of selectively degrading fibroblast growth factor receptor 2 (FGFR2) to overcome the issues of drug resistance and adverse reactions associated with traditional inhibitors in the treatment of FGFR2 ...
Yumeng Jin +7 more
doaj +1 more source

