Results 81 to 90 of about 636,170 (221)

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

British Journal of Pharmacology, EarlyView.
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, Alan Armstrong, David J. Mann   +2 more
wiley   +1 more source

Thermodynamic characterisation of covalent ligand binding

British Journal of Pharmacology, EarlyView.
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, Maayan Lavie, Almog Nadir, Ronen Gabizon, Nir London   +4 more
wiley   +1 more source

Targeting Bruton’s tyrosine kinase (BTK) as a signaling pathway in immune-mediated diseases: from molecular mechanisms to leading treatments

Advances in Rheumatology
Bruton’s tyrosine kinase (BTK), a nonreceptor tyrosine kinase, plays a remarkable role in the transmission and amplification of extracellular signals to intracellular signaling pathways.
Gita Manzari Tavakoli, Niloufar Yazdanpanah, Nima Rezaei   +2 more
doaj   +1 more source

Heart failure medication to prevent cancer therapy–related cardiac dysfunction: A narrative review

British Journal of Pharmacology, EarlyView.
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, Paul Goerke, Malte Kelm, Amin Polzin   +3 more
wiley   +1 more source

Bruton tyrosine kinase inhibitors and cardiovascular adverse events

British Journal of Pharmacology, EarlyView.
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, Cristina Madaudo, Emanuela Salvatorelli, Giorgio Minotti, Pierantonio Menna   +4 more
wiley   +1 more source

BTK Inhibitors and BTK Degraders for the Treatment of Mantle Cell Lymphoma - Current Status and Perspectives

The introduction of Bruton tyrosine kinase inhibitors (BTKis) has significantly improved prognosis in the treatment of MCL. BTK inhibitors have demonstrated strong activity in the treatment of relapsed/refractory patients with mantle cell lymphoma (MCL),
Tadeusz Robak, Paweł Robak, Anna Wolska-Washer   +2 more
core   +1 more source

Machine Learning‐Derived Immune Gene Signature Predicts Prognosis and Therapeutic Vulnerabilities in Multiple Myeloma

Cancer Science, EarlyView.
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, Chenfei Zhao, Jingru Shi, Shiwei Liu, Yi Chen, Jujuan Wang, Zhengxu Sun, Sanmei Wang, Lei Fan, Jin Fan, Xiaoyan Qu   +10 more
wiley   +1 more source

Combining structure-based pharmacophore modeling and machine learning for the identification of novel BTK inhibitors

, 2022
Bruton's tyrosine kinase (BTK) is a critical enzyme which is involved in multiple signaling pathways that regulate cellular survival, activation, and proliferation, making it a major cancer therapeutic target.
동재준, 이덕철
core   +1 more source

BTK Inhibition in Hematology: From CLL/SLL to Emerging Applications Across B-Cell and Immune Disorders

Biomolecules
BTK (Bruton’s tyrosine kinase) has become a key therapeutic target across several hematologic diseases, beginning with its original use in CLL/SLL.
Andrea Duminuco, Paola De Luca, Gaia Stanzione, Laura Anastasia Caruso, Giulio Lavenia, Salvatore Scarso, Bruno Garibaldi, Fanny Erika Palumbo, Calogero Vetro, Giuseppe Alberto Palumbo   +9 more
doaj   +1 more source

Economic Burden of Chronic Lymphocytic Leukaemia in Australia

European Journal of Haematology, EarlyView.
ABSTRACT Background The treatment landscape for chronic lymphocytic leukaemia (CLL) has transformed over the past decade. This study aimed to estimate the healthcare costs and health burden associated with CLL in Australia. Methods A Markov model was developed to simulate the lifetime healthcare costs and health outcomes associated with CLL in ...
Lan Gao, Dieu Nguyen, Victoria White, Patricia M. Livingston, Chan Y. Cheah   +4 more
wiley   +1 more source