Results 71 to 80 of about 655,557 (182)
Summary Most patients treated for chronic lymphocytic leukaemia (CLL) fail to achieve measurable residual disease (MRD) negativity. The role of maintenance with the immunomodulatory drug lenalidomide in these patients is unclear. A randomised multicentre phase III trial (ACTRN12610000060044) was conducted in Australia and France to assess the effect of
Thérèse Aurran‐Schleinitz +45 more
wiley +1 more source
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
Clinical development of BTK kinase inhibitors for treating autoimmune diseases has lagged behind development of these drugs for treating cancers, due in part from concerns over the lack of selectivity and associated toxicity profiles of first generation ...
Matthew Wampole (11639998) +2 more
core +1 more source
Thermodynamic characterisation of covalent ligand binding
Background and Purpose Differential scanning fluorimetry (DSF) is a common and straightforward method to evaluate the thermal stability of proteins and has been heavily used for ligand binding characterisation as well as for screening. One class of compounds that is less typically evaluated by DSF are covalent binders.
Rebecca Hertzman +4 more
wiley +1 more source
Heart failure medication to prevent cancer therapy–related cardiac dysfunction: A narrative review
Advances in oncological therapies have improved cancer survival but also have increased the clinical incidence of cancer therapy–related cardiac dysfunction (CTRCD), a spectrum of conditions ranging from subclinical biomarker or strain abnormalities to progressive heart failure and cardiogenic shock.
Fabian Voß +3 more
wiley +1 more source
Irreversible dual inhibitory mode: the novel Btk inhibitor PLS-123 demonstrates promising anti-tumor activity in human B-cell lymphoma. [PDF]
The B-cell receptor (BCR) signaling pathway has gained significant attention as a therapeutic target in B-cell malignancies. Recently, several drugs that target the BCR signaling pathway, especially the Btk inhibitor ibrutinib, have demonstrated notable ...
Li, Xitao +10 more
core +1 more source
Clinical development of BTK kinase inhibitors for treating autoimmune diseases has lagged behind development of these drugs for treating cancers, due in part from concerns over the lack of selectivity and associated toxicity profiles of first generation ...
Matthew Wampole (11639998) +2 more
core +1 more source
Bruton tyrosine kinase inhibitors and cardiovascular adverse events
Abstract Bruton tyrosine kinase inhibitors (BTKi) have transformed the management of chronic lymphocytic leukaemia and other B‐cell malignancies, yet their therapeutic benefit is tempered by clinically relevant cardiovascular toxicities (predominantly atrial fibrillation, hypertension, bleeding and ventricular arrhythmias).
Massimiliano Camilli +4 more
wiley +1 more source
An immune‐related 12‐gene signature developed through integrative machine learning stratified overall survival across multiple myeloma cohorts and remained independently associated with outcome. Single‐cell, somatic mutation, and transcriptome‐based drug‐response analyses further linked the signature to multicellular bone marrow context, distinct ...
Kai Wang +10 more
wiley +1 more source
Loss of A20 and BTK C481F mutation as mechanisms of BTK inhibitor resistance in TMD8.
(A) Cell viability of BTK inhibitor (BTKi)-sensitive (TMD8BTKi-S) and BTKi-resistant (TMD8BTKi-R) cells to ibrutinib, 96 hour CellTiterGlo assay, mean ± SEM, n = 4.
Rick A. Sorensen (3727219) +9 more
core +1 more source

