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
Bruton's tyrosine kinase phosphorylates Toll-like receptor 3 to initiate antiviral response
Toll-like receptor 3 (TLR3) mediates antiviral response by recognizing double-stranded RNA. Its cytoplasmic domain is tyrosine phosphorylated upon ligand binding and initiates downstream signaling via the adapter TIR-containing adaptor inducing ...
Kang, Z.-H. +8 more
core +1 more source
The Role of BTK Inhibition in the Treatment of Chronic Lymphocytic Leukemia: A Clinical View
Francesco Paolo Tambaro,1 Danilo De Novellis,1,2 William G Wierda3 1Unità Operativa di Trapianto di Midollo Osseo e Servizio Trasfusionale, Azienda Ospedaliera di Rilievo Nazionale Santobono-Pausilipon, Napoli, Italy; 2Department of Precision Medicine ...
Tambaro FP, De Novellis D, Wierda WG
doaj
The WHO Classification of Genetic Tumour Syndromes: Considerations for Genetics
The WHO Classification of Tumours underpins the diagnosis of neoplastic conditions. The new WHO classification of genetic tumour syndromes (GTS) provides international standards for their diagnosis. This diagram highlights the chromosomal distribution of the genes involved in the GTS covered in this classification.
Ian A. Cree +18 more
wiley +1 more source
The chemokine regulation of Bruton's tyrosine kinase in acute myeloid leukaemia [PDF]
Acute myeloid leukaemia (AML) and chronic lymphocytic leukaemia (CLL) are common in the elderly. Bruton's tyrosine kinase (BTK) is an important protein that plays a vital role in several signalling pathways including the B cell receptor (BCR) and SDF-1α ...
Keadsanti, S
core +1 more source
Identification of pharmacodynamic biomarker hypotheses through literature analysis with IBM Watson.
BackgroundPharmacodynamic biomarkers are becoming increasingly valuable for assessing drug activity and target modulation in clinical trials. However, identifying quality biomarkers is challenging due to the increasing volume and heterogeneity of ...
Sonja Hatz +9 more
doaj +1 more source
ABSTRACT Immunoglobulin heavy chain variable region‐unmutated (IGHV‐U) chronic lymphocytic leukemia (CLL) represents a biologically aggressive subgroup with limited responsiveness to chemoimmunotherapy (CIT). To clarify the comparative effectiveness of available frontline options, we conducted a comprehensive Bayesian network meta‐analysis of ...
Santino Caserta +13 more
wiley +1 more source
Binding of Bruton's Tyrosine Kinase to Fyn, Lyn, or Hck Through a Src Homology 3 Domain-Mediated Interaction [PDF]
Bruton's tyrosine kinase (Btk) is a recently described B-cell-specific tyrosine kinase. Mutations in this gene lead to human X chromosome-linked agammaglobulinemia and murine X-linked immunodeficiency. Although genetic evidence strongly suggests that Btk
Ye, Zheng-Sheng +2 more
core
Ibrutinib Displays Atrial-Specific Toxicity in Human Stem Cell-Derived Cardiomyocytes
Summary: Ibrutinib (IB) is an oral Bruton's tyrosine kinase (BTK) inhibitor that has demonstrated benefit in B cell cancers, but is associated with a dramatic increase in atrial fibrillation (AF).
Sanam Shafaattalab +11 more
doaj +1 more source
From Time‐Limited Therapy to Treatment‐Free Observation: The Evolving Role of MRD in CLL Management
ABSTRACT The integration of measurable residual disease (MRD) into the management of chronic lymphocytic leukemia (CLL) has emerged as a major advance in risk stratification and trial design, particularly in the context of time‐limited, targeted regimens.
Enrica Antonia Martino +13 more
wiley +1 more source

