Results 131 to 140 of about 7,833 (210)

Acalabrutinib in Chronic Lymphocytic Leukemia: Pharmacology and Emerging Clinical Perspectives

European Journal of Haematology, Volume 116, Issue 6, Page 759-770, June 2026.
ABSTRACT Acalabrutinib, a second‐generation Bruton's tyrosine kinase inhibitor (BTKi), is characterized by enhanced specificity and selectivity for BTK with minimal off‐target effects, offering a significant evolution in the treatment of chronic lymphocytic leukemia (CLL). Its mechanism of action, a covalent binding to Cys481 within the BTK active site,
Gianluca Gaidano, Romano Danesi
wiley   +1 more source

Design and Synthesis of Novel Amino-triazine Analogues as Selective Bruton’s Tyrosine Kinase Inhibitors for Treatment of Rheumatoid Arthritis

, 2018
Bruton’s tyrosine kinase (BTK) is a promising drug target for the treatment of multiple diseases, such as B-cell malignances, asthma, and rheumatoid arthritis.
Masaaki Sawa (5801243), Takao Kiyoi (5801234), Yuko Asamitsu (5801240), Takayuki Irie (2438509), Haruka Taniguchi (5801237), Tomoko Inoue (528192), Tokiko Asami (5801231), Takahiro Miyake (2419702), Wataru Kawahata (5801228)   +8 more
core   +1 more source

Fragment‐Based Design of Targeted Covalent Inhibitors: The Scope and Limitation of Linking Approaches

ChemMedChem, Volume 21, Issue 10, 27 May 2026.
This paper by Kollár et al. reports a covalent fragment linking study against the SARS‐CoV‐2 main protease (3CLPro). Beginning with inactive fragment hits, the application of rational linker design enabled the generation of reversible covalent inhibitors exhibiting low micromolar potency. The study details some general limitations and best practices of
Levente Kollár, Levente M. Mihalovits, Dávid Bajusz, Damijan Knez, József Simon, Blake H. Balcomb, Daren Fearon, Stanislav Gobec, György M. Keserű   +8 more
wiley   +1 more source

Inhibition of Bruton’s tyrosine kinase with PD-1 blockade modulates T cell activation in solid tumors

BACKGROUND Inhibition of Bruton’s tyrosine kinase with ibrutinib blocks the function of myeloid-derived suppressor cells (MDSC). The combination of ibrutinib and nivolumab was tested in patients with metastatic solid tumors.METHODS Sixteen patients ...
Yang Hu, Kristin Bixel, John Hays, Xueliang Pan, Brooke Benner, Dongjun Chung, Kyeong Joo Jung, Anne M. Noonan, Gabriella Lapurga, Hiral A. Shah, Paul Monk, Emily Schwarz, Himanshu Savardekar, Steven H. Sun, Claire Verschraegen, Kari Kendra, Dionisia Quiroga, Robert Wesolowski, Olivier Elemento, Logan Good, Megan C. Duggan, Manisha Shah, Gregory Behbehani, Jami Shaffer, Jianying Li, Bhavana Konda, Gang Xin, William E. Carson III, Bradley W. Blaser, Luke Scarberry, Robert Rupert, Lai Wei   +31 more
core   +1 more source

Bruton’s tyrosine kinase inhibition ameliorated neuroinflammation during chronic white matter ischemia

Journal of Neuroinflammation
Chronic cerebral hypoperfusion (CCH), a disease afflicting numerous individuals worldwide, is a primary cause of cognitive deficits, the pathogenesis of which remains poorly understood. Bruton’s tyrosine kinase inhibition (BTKi) is considered a promising
Lu-Lu Xu, Sheng Yang, Luo-Qi Zhou, Yun-Hui Chu, Xiao-Wei Pang, Yun-Fan You, Hang Zhang, Lu-Yang Zhang, Li-Fang Zhu, Lian Chen, Ke Shang, Jun Xiao, Wei Wang, Dai-Shi Tian, Chuan Qin   +14 more
doaj   +1 more source

Studies of Bruton’s tyrosine kinase inhibitors in B-cell malignancies

, 2018
Despite significant advances, the prognosis in relapsed/refractory (R/R) B-cell malignancies remains poor. In the Phase I study of the selective Bruton’s Tyrosine Kinase inhibitor (BTKi) tirabrutinib in R/R B-cell malignancies, I showed that targeting ...
Harriet Sarah Walter (7785374)
core   +1 more source

EXPLORING THE SENSITIVITY OF MANTLE CELL LYMPHOMA TO INHIBITORS OF BRUTON’S TYROSINE KINASE

, 2019
EXPLORING THE SENSITIVITY OF MANTLE CELL LYMPHOMA TO INHIBITORS OF BRUTON’S TYROSINE KINASE Mantle cell lymphoma (MCL) is an incurable B-cell lymphoma which responds poorly to conventional chemotherapy.
Thompson, Hannah Patricia
core  

Correction to "Comprehensive Characterization of Bruton's Tyrosine Kinase Inhibitor Specificity, Potency, and Biological Effects: Insights into Covalent and Noncovalent Mechanistic Signatures". [PDF]

ACS Pharmacol Transl Sci
Darragh AC, Hanna AM, Lipner JH, King AJ, Servant NB, Jahic M.   +5 more
europepmc   +2 more sources

Evaluating ibrutinib in the treatment of symptomatic Waldenstrom’s macroglobulinemia

Journal of Blood Medicine, 2019
Aristea-Maria Papanota,* Ioannis Ntanasis-Stathopoulos,* Efstathios Kastritis, Meletios A Dimopoulos, Maria GavriatopoulouDepartment of Clinical Therapeutics, National and Kapodistrian University of Athens, School of Medicine, Alexandra General Hospital,
Papanota AM, Ntanasis-Stathopoulos I, Kastritis E, Dimopoulos MA, Gavriatopoulou M   +4 more
doaj  

Response to Bruton’s tyrosine kinase inhibitors in aggressive lymphomas linked to chronic selective autophagy

Diffuse large B cell lymphoma (DLBCL) is an aggressive, profoundly heterogeneous cancer, presenting a challenge for precision medicine. Bruton’s tyrosine kinase (BTK) inhibitors block B cell receptor (BCR) signaling and are particularly effective in ...
Kasbekar, M., Choi, J., Enssle, J., Young, R., Doebele, C., Häupl, B., Wang, Z., Collinge, B., Morris, V., Tran, A., Zindel, A., Rieke, S., Yu, X., Staudt, L., Phelan, J., Zhuang, X., Pape, M., Coulibaly, Z., Xu, W., Ji, Y., Shaffer, A., Scheich, S., Urlaub, H., Wotapek, T., Yang, Y., Huang, D., Shevchenko, G., Hodson, D., Shoemaker, C., Oellerich, T., Wright, G., Bolomsky, A., Zhao, H.   +32 more
core   +1 more source