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
Inhibitors of insulin‐degrading enzyme boost PI cytotoxicity through an increased sensitivity of proteasome to PI inhibitors, induction of ISR, DNA damage and Myc down‐regulation. They overcome PI resistance in vitro and induce tumour regression in vivo.
Laetitia Lesire +28 more
wiley +1 more source
A novel male 2;4;14 complex chromosomal translocation with normal semen parameters but 100% embryonic aneuploidy. [PDF]
Mas J, Sabouni R, Bocca S.
europepmc +1 more source
Common fragile sites. Structure, replication and their role in chromosome instabiity [PDF]
BOSCO, NAZARIO
core
GRKs and arrestins: Nomenclature and functions in GPCR‐dependent and ‐independent signalling
G protein‐coupled receptor (GPCR) kinases (GRKs) and arrestins play a critical role in the regulation of GPCR signalling. Historic names of mammalian GRKs were replaced by systematic ones in the 1990s; however, both kinds of names are currently in use for mammalian arrestins.
Vsevolod V. Gurevich
wiley +1 more source
MLL leukemia induction by t(9;11) chromosomal translocation in human hematopoietic stem cells using genome editing. [PDF]
Schneidawind C +10 more
europepmc +1 more source
Clinical and Genetic Landscape of Glioblastoma, IDH‐Wildtype With FGFR Gene Family Alterations
We analyzed 1076 cases of glioblastoma, IDH‐wildtype (GBM, IDH‐wt) using the C‐CAT genomic database to clarify the clinical and genetic features of FGFR alterations. FGFR::TACC fusions and FGFR1 mutations were identified in distinct subsets and were associated with unique co‐mutation patterns.
Yasuhito Kegoya +9 more
wiley +1 more source
Glucose Metabolism Regulating Colorectal Cancer Initiation and Progression
Drugs and compounds targeting glycolysis in CRC and the mechanisms by which these drugs inhibit their respective targets. ABSTRACT Colorectal cancer (CRC) is one of the most common types of invasive cancer worldwide, which has the characteristics of poor curative effect and poor prognosis. Increasing evidence suggests that hyperactivated glucose uptake
Meiyi Lin, Junpeng Cui
wiley +1 more source
NOL7 acts as a tumor‐suppressor in ovarian cancer. Overexpression of NOL7 up‐regulated GADD45A expression by stabilizing GADD45A mRNA in ovarian cancer cells. ABSTRACT Ovarian cancer is one of the most prevalent gynecologic malignancies worldwide. Dysregulated cell proliferation and angiogenesis are well‐recognized to be involved in the pathogenesis of
Xinyu Xu +3 more
wiley +1 more source
Targeting Inflammation and Immune Regulation in Chronic Inflammation Associated Cancers
Chronic inflammation sustains activation of key inflammatory pathways, including Nuclear factor kappa B (NF‐κB), Interleukin‐6‐signal transducer and activator of transcription 3 (IL6‐STAT3), Phosphoinositide 3‐kinase/Akt (PI3K/Akt), and Wingless/β‐catenin (Wnt/β‐catenin) signaling. This promotes immune dysregulation through the expansion and functional
Lawan Rabiu +5 more
wiley +1 more source

