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Bruton tyrosine kinase

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https://www.readbyqxmd.com/read/29652138/development-of-a-selective-labeling-probe-for-bruton-s-tyrosine-kinase-quantification-in-live-cells
#1
Jiahui Chen, Xiafeng Wang, Fengli He, Zhengying Pan
As a key regulator of the B-cell receptor signaling pathway, Bruton's tyrosine kinase (Btk) has emerged as an important therapeutic target for various malignancies and autoimmune disorders. However, data on the expression profiles of Btk are lacking. Here, we report the discovery of a new, selective Btk probe and of a sandwich-type ELISA quantification method to detect endogenous Btk in live cells. We achieved selective labeling of Btk in vivo and quantified Btk levels in seven types of human lymphoma cell lines...
April 13, 2018: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/29628774/management-of-relapsed-refractory-marginal-zone-lymphoma-focus-on-ibrutinib
#2
REVIEW
Nathan M Denlinger, Narendranath Epperla, Basem M William
Marginal zone lymphomas (MZLs) consist of a diverse family of malignancies, which are derived from B-cells. The disease subtypes are recognized extranodal, nodal, and splenic MZLs. The disease characteristics, clinical course, and treatment vary considerably based on the site of involvement. In 2017, the US Food and Drug Administration approved ibrutinib, a first in class Bruton's tyrosine kinase inhibitor that revolutionized the care of chronic lymphocytic leukemia patients; for, the treatment of relapsed/refractory MZL based on pivotal open-label Phase II trial demonstrated an overall response rate of 48%, with a complete response rate of 3%, median progression-free survival of 14...
2018: Cancer Management and Research
https://www.readbyqxmd.com/read/29587203/inhibitor-of-bruton-s-tyrosine-kinases-pci-32765-decreases-pro-inflammatory-mediators-production-in-high-glucose-induced-macrophages
#3
Zhe Fan, Yan Wang, Xingxin Xu, Yonggui Wu
Accumulating evidence has shown that macrophages play a vital role in development and pathogenesis of diabetic nephropathy (DN) by secreting inflammatory cytokines. Although Bruton's tyrosine kinases (Btk) is a biologically important molecule implicated in immune regulation, the role of Btk in high glucose (HG)-stimulated inflammatory response in macrophages and the mechanism involved need further investigation. In our study, we used bone marrow-derived macrophages (BMMs) to investigate the involvement of Btk on HG-induced inflammatory cytokines expression and to explore the underlying mechanisms...
March 24, 2018: International Immunopharmacology
https://www.readbyqxmd.com/read/29572581/marginal-zone-lymphoma-clinicopathologic-variations-and-approaches-to-therapy
#4
REVIEW
Sabarish Ayyappan, Basem M William
PURPOSE OF REVIEW: The purpose of the study is to summarize the current conundrums in the management of marginal zone lymphomas (MZL). RECENT FINDINGS: In 2017, the US Food and Drug Administration (FDA) approved ibrutinib, a first in class Bruton Tyrosine Kinase inhibitor, for the treatment of relapsed/refractory MZL based on pivotal open-label phase II trial demonstrating an overall response rates of 48%. Clinical trials design utilizing chemotherapy-free regimens for relapsed/refractory disease are gaining popularity...
March 23, 2018: Current Oncology Reports
https://www.readbyqxmd.com/read/29567799/pan-src-kinase-inhibition-blocks-b-cell-receptor-oncogenic-signaling-in-non-hodgkin-lymphoma
#5
Elena Battistello, Natalya Katanayeva, Elie Dheilly, Daniele Tavernari, Maria C Donaldson, Luca Bonsignore, Margot Thome-Miazza, Amanda L Christie, Mark A Murakami, Olivier Michielin, Giovanni Ciriello, Vincent Zoete, Elisa Oricchio
In diffuse large B-cell lymphoma (DLBCL), activation of the B-cell receptor (BCR) promotes multiple oncogenic signals, which are essential for tumor proliferation. Inhibition of the Bruton's tyrosine kinase (BTK), a BCR downstream target, is therapeutically effective only in a subgroup of DLBCL patients. Here, we used lymphoma cells isolated from DLBCL patients to measure the effects of targeted therapies on BCR signaling and to anticipate response. In lymphomas resistant to BTK inhibition, we show that blocking BTK activity enhanced tumor dependencies from alternative oncogenic signals downstream of the BCR, converging on MYC up-regulation...
March 22, 2018: Blood
https://www.readbyqxmd.com/read/29567473/bruton-s-tyrosine-kinase-regulates-tlr7-8-induced-tnf-transcription-via-nuclear-factor-%C3%AE%C2%BAb-recruitment
#6
Theresa H Page, Anna M Urbaniak, Ana I Espirito Santo, Lynett Danks, Timothy Smallie, Lynn M Williams, Nicole J Horwood
Tumour necrosis factor (TNF) is produced by primary human macrophages in response to stimulation by exogenous pathogen-associated molecular patterns (PAMPs) and endogenous damage-associated molecular patterns (DAMPs) via Toll-like receptor (TLR) signalling. However, uncontrolled TNF production can be deleterious and hence it is tightly controlled at multiple stages. We have previously shown that Bruton's tyrosine kinase (Btk) regulates TLR4-induced TNF production via p38 MAP Kinase by stabilising TNF messenger RNA...
March 19, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29567295/design-synthesis-and-biological-evaluation-of-novel-3-substituted-pyrazolopyrimidine-derivatives-as-potent-bruton-s-tyrosine-kinase-btk-inhibitors
#7
Nan Zheng, Jing Pan, Qun Hao, Yingxia Li, Weicheng Zhou
A series of 3-substituted pyrazolopyrimidine derivatives as BTK inhibitors were designed by structure-based drug design and they were synthesized, evaluated by enzyme-based assay and anti-proliferation against Ramos and Raji cells. Most of them displayed good inhibitory activities against both BTK and B-cell lymphoblastic leukemia lines in vitro. Among them, compound 8a exhibited excellent potency (IC50  = 7.95 nM against BTK enzyme, 8.91 μM against Ramos cells and 1.80 μM against Raji cells), with a better hydrophilicity (ClogP = 3...
March 12, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29567142/molecular-characterization-and-function-analysis-of-grouper-epinephelus-coioides-bruton-s-tyrosine-kinase-btk
#8
Ze-Quan Mo, Qing Han, Yu-Long Zeng, Jiu-Le Wang, Xue-Zhu Li, Yan-Wei Li, Hong-Yan Sun, An-Xing Li, Xiao-Chun Luo, Xue-Ming Dan
Bruton's tyrosine kinase (BTK) is a Tec-family tyrosine kinase and plays a crucial role in B cell antigen receptor (BCR) signal pathway. Mutations in humans and mice BTK gene results in X-linked agammaglobulinemia (XLA) and X-linked immunodeficiency (XLD), respectively. To study the function of BTK in teleost, we cloned a BTK gene from orange-spotted grouper. Homology analysis showed that the grouper BTK (EcBTK) had a high amino acid identity with other vertebrates (63%-92%) and shared the highest amino acid identity with ballan wrasse Labrus bergylta BTK...
March 19, 2018: Fish & Shellfish Immunology
https://www.readbyqxmd.com/read/29561760/novel-indications-for-bruton-s-tyrosine-kinase-inhibitors-beyond-hematological-malignancies
#9
REVIEW
Robert Campbell, Geoffrey Chong, Eliza A Hawkes
Bruton's tyrosine kinase (BTK) is a critical terminal enzyme in the B-cell antigen receptor (BCR) pathway. BTK activation has been implicated in the pathogenesis of certain B-cell malignancies. Targeting this pathway has emerged as a novel target in B-cell malignancies, of which ibrutinib is the first-in-class agent. A few other BTK inhibitors (BTKi) are also under development (e.g., acalabrutinib). While the predominant action of BTKi is the blockade of B-cell receptor pathway within malignant B-cells, increasing the knowledge of off-target effects as well as a potential role for B-cells in proliferation of solid malignancies is expanding the indication of BTKi into non-hematological malignancies...
March 21, 2018: Journal of Clinical Medicine
https://www.readbyqxmd.com/read/29560128/first-in-human-phase-1-study-of-the-btk-inhibitor-gdc-0853-in-relapsed-or-refractory-b-cell-nhl-and-cll
#10
John C Byrd, Stephen Smith, Nina Wagner-Johnston, Jeff Sharman, Andy I Chen, Ranjana Advani, Bradley Augustson, Paula Marlton, S Renee Commerford, Kwame Okrah, Lichuan Liu, Elaine Murray, Elicia Penuel, Ashley F Ward, Ian W Flinn
GDC-0853 is a selective, reversible, and non-covalent inhibitor of Bruton's tyrosine kinase (BTK) that does not require interaction with the Cys481 residue for activity. In this first-in-human phase 1 study we evaluated safety, tolerability, pharmacokinetics, and activity of GDC-0853 in patients with relapsed or refractory non-Hodgkin lymphoma (NHL) or chronic lymphocytic leukemia (CLL). Twenty-four patients, enrolled into 3 cohorts, including 6 patients who were positive for the C481S mutation, received GDC-0853 at 100, 200, or 400 mg once daily, orally...
February 27, 2018: Oncotarget
https://www.readbyqxmd.com/read/29559479/oral-bruton-tyrosine-kinase-inhibitors-selectively-block-atherosclerotic-plaque-triggered-thrombus-formation
#11
Kristina Busygina, Janina Jamasbi, Till Seiler, Hans Deckmyn, Christian Weber, Richard Brandl, Reinhard Lorenz, Wolfgang Siess
Interaction of Von Willebrand factor (VWF) with platelet glycoprotein (GP) Ib and of collagen with GPVI is essential for thrombus formation on ruptured or eroded atherosclerotic plaques (atherothrombosis). GPIb and GPVI signal through Bruton tyrosine kinase (Btk) which can irreversibly be blocked by oral application of ibrutinib, an established therapy for chronic lymphocytic leukemia (CLL) with long term safety. We found that ibrutinib and the novel Btk-inhibitors acalabrutinib and ONO/GS-4059 block GPVI-dependent static platelet aggregation in blood exposed to human plaque homogenate and collagen but not to ADP or arachidonic acid...
March 20, 2018: Blood
https://www.readbyqxmd.com/read/29546831/development-of-bruton-s-tyrosine-kinase-inhibitors-for-rheumatoid-arthritis
#12
Lv Jiahui, Wu Jingde, He Feng, Qu Ying, Zhang Qiuqiong, Yu Chenggong
Rheumatoid Arthritis (RA) is a chronic autoimmune disease and becomes one of the major causes of disability and work force loss. The presence of abnormal B cell and autoantibodies produced by most RA patients, primarily ACPA and RF, indicate that the function of B cell was involved in the development of RA disease. Accordingly, the drug targeting B cell has become a hot spot in the treatment of RA. Studies have shown that Bruton's tyrosine kinase (BTK) is involved in the regulation of B cell proliferation and activation process...
March 16, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29526963/paraneoplastic-pemphigus-associated-with-b-cell-chronic-lymphocytic-leukemia-treated-with-ibrutinib-and-rituximab
#13
Yuta Ito, Shinichi Makita, Akiko Miyagi Maeshima, Shunsuke Hatta, Tomotaka Suzuki, Sayako Yuda, Suguru Fukuhara, Wataru Munakata, Tatsuya Suzuki, Dai Maruyama, Koji Izutsu
Paraneoplastic pemphigus (PNP) is a severe autoimmune blistering disease associated with an underlying malignancy, and its prognosis is poor. We herein report the first patient with B-cell chronic lymphocytic leukemia/small lymphocytic lymphoma (B-CLL/SLL)-associated PNP successfully treated with the Bruton's tyrosine kinase inhibitor ibrutinib and rituximab. Although his PNP lesions did not improve with ibrutinib monotherapy, the combination of ibrutinib and rituximab was effective against B-CLL/SLL-associated PNP...
March 9, 2018: Internal Medicine
https://www.readbyqxmd.com/read/29516781/inhibiting-bruton-s-tyrosine-kinase-rescues-mice-from-lethal-influenza-induced-acute-lung-injury
#14
Jon M Florence, Agnieszka Krupa, Laela M Booshehri, Sandra A Davis, Michael A Matthay, Anna K Kurdowska
Infection with seasonal influenza A virus (IAV) leads to lung inflammation and respiratory failure, a main cause of death in influenza infected patients. Previous experiments in our laboratory indicated that Bruton's tyrosine kinase (Btk) plays a substantial role in regulating inflammation in the respiratory region during acute lung injury (ALI) in mice, therefore we sought to determine if blocking Btk activity had a protective effect in the lung during influenza induced inflammation. A Btk inhibitor (Btk Inh...
March 8, 2018: American Journal of Physiology. Lung Cellular and Molecular Physiology
https://www.readbyqxmd.com/read/29512173/practical-management-of-ibrutinib-in-the-real-life-focus-on-atrial-fibrillation-and-bleeding
#15
REVIEW
Giuseppe Boriani, Paolo Corradini, Antonio Cuneo, Anna Falanga, Robin Foà, Gianluca Gaidano, Paolo Prospero Ghia, Maurizio Martelli, Roberto Marasca, Massimo Massaia, Francesca Romana Mauro, Giorgio Minotti, Stefano Molica, Marco Montillo, Antonio Pinto, Alessandra Tedeschi, Umberto Vitolo, Pier Luigi Zinzani
The Bruton tyrosine kinase inhibitor ibrutinib (IB) has attained an important role in the treatment of patients with chronic lymphocytic leukaemia, mantle cell lymphoma, and Waldenström macroglobulinemia, significantly improving clinical outcomes. However, IB therapy has been associated with an increased risk of atrial fibrillation (AF) and bleeding. We report on the expert opinion that a group of Italian haematologists, cardiologists, and pharmacologists jointly released to improve the practical management of patients at risk for AF and bleeding during treatment with IB...
March 7, 2018: Hematological Oncology
https://www.readbyqxmd.com/read/29509845/serious-infections-in-patients-receiving-ibrutinib-for-treatment-of-lymphoid-malignancies
#16
Tilly Varughese, Ying Taur, Nina Cohen, M Lia Palomba, Susan K Seo, Tobias M Hohl, Gil Redelman-Sidi
Background: Ibrutinib is a Bruton's tyrosine kinase inhibitor that is used for the treatment of lymphoid malignancies, including chronic lymphocytic leukemia (CLL), Waldenström's macroglobulinemia and mantle cell lymphoma (MCL). Several case series have described opportunistic infections among ibrutinib recipients, but the full extent of these infections is unknown. We sought to determine the spectrum of serious infections associated with ibrutinib treatment. Methods: We reviewed the electronic medical records of patients with lymphoid malignancies at Memorial Sloan Kettering Cancer Center who received ibrutinib during a five-year period from January 1, 2012 to December 31, 2016...
March 2, 2018: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/29503650/dried-blood-spots-an-affordable-tool-to-collect-ship-and-sequence-gdna-from-patients-with-an-x-linked-agammaglobulinemia-phenotype-residing-in-a-developing-country
#17
Gesmar R S Segundo, Anh T V Nguyen, Huyen T Thuc, Le N Q Nguyen, Roger H Kobayashi, Hai T Le, Huong T M Le, Troy R Torgerson, Hans D Ochs
Background: New sequencing techniques have revolutionized the identification of the molecular basis of primary immunodeficiency disorders (PID) not only by establishing a gene-based diagnosis but also by facilitating defect-specific treatment strategies, improving quality of life and survival, and allowing factual genetic counseling. Because these techniques are generally not available for physicians and their patients residing in developing countries, collaboration with overseas laboratories has been explored as a possible, albeit cumbersome, strategy...
2018: Frontiers in Immunology
https://www.readbyqxmd.com/read/29484638/safety-pharmacokinetics-and-pharmacodynamics-in-healthy-volunteers-treated-with-gdc-0853-a-selective-reversible-bruton-s-tyrosine-kinase-inhibitor
#18
Ann E Herman, Leslie W Chinn, Shweta G Kotwal, Elaine R Murray, Rui Zhao, Marilyn Florero, Alyse Lin, Anita Moein, Rena Wang, Meire Bremer, Serika Kokubu, Adrian P Serone, Eva L Hanze, Anders Viberg, Alyssa M Morimoto, Helen R Winter, Tamiko R Katsumoto
GDC-0853 is a small molecule inhibitor of Bruton's tyrosine kinase (BTK) that is highly selective and non-covalent, leading to reversible binding. In double-blind, randomized, and placebo-controlled phase I healthy volunteer studies, GDC-0853 was well-tolerated with no dose-limiting adverse events (AEs) or serious AEs. The maximum tolerated dose was not reached during dose escalation (≤600 mg, single ascending dose [SAD] study; ≤250 mg twice daily [BID] and ≤500 mg once daily, 14-day multiple ascending dose (MAD) study)...
February 27, 2018: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29483358/bruton-s-tyrosine-kinase-is-not-essential-for-b-cell-survival-beyond-early-developmental-stages
#19
Lindsay E Nyhoff, Emily S Clark, Bridgette L Barron, Rachel H Bonami, Wasif N Khan, Peggy L Kendall
Bruton's tyrosine kinase (Btk) is a crucial regulator of B cell signaling and is a therapeutic target for lymphoma and autoimmune disease. BTK-deficient patients suffer from humoral immunodeficiency, as their B cells fail to progress beyond the bone marrow. However, the role of Btk in fully developed, mature peripheral B cells is not well understood. Analysis using BTK inhibitors is complicated by suboptimal inhibition, off-target effects, or failure to eliminate BTK's adaptor function. Therefore a Btk flox /Cre-ERT2 mouse model was developed and used to excise Btk after B cell populations were established...
April 1, 2018: Journal of Immunology: Official Journal of the American Association of Immunologists
https://www.readbyqxmd.com/read/29483220/p110%C3%AE-inhibition-overcomes-stromal-cell-mediated-ibrutinib-resistance-in-mantle-cell-lymphoma
#20
Jiyu Guan, Dan Huang, Konstantin Yakimchuk, Sam Okret
Acquired resistance to cancer drugs is common, also for modern targeted drugs like the Bruton's tyrosine kinase (BTK) inhibitor ibrutinib, a new drug approved for the treatment of the highly aggressive and relapsing mantle cell lymphoma (MCL). The tumor microenvironment often impacts negatively on drug response. Here we demonstrate that stromal cells protect MCL cells from ibrutinib-induced apoptosis and support MCL cell regrowth after drug removal by impairing ibrutinib-mediated down-regulation of phosphoinositide-3-kinase (PI3K)/AKT signaling...
February 26, 2018: Molecular Cancer Therapeutics
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