Results 101 to 110 of about 80,266 (330)

The phosphoinositide 3-kinase-dependent activation of Btk is required for optimal eicosanoid production and generation of reactive oxygen species in antigen-stimulated mast cells

, 2008
Activated mast cells are a major source of the eicosanoids PGD(2) and leukotriene C(4) (LTC(4)), which contribute to allergic responses. These eicosanoids are produced following the ERK1/2-dependent activation of cytosolic phospholipase A(2), thus ...
Beaven, Michael A., Gilfillan, Alasdair M., Kim, Mi-Sun, Kuehn, Hye Sun, Metcalfe, Dean D., Swindle, Emily J.   +5 more
core   +1 more source

New means and challenges in the targeting of BTK.

Clinical Cancer Research
Bruton's tyrosine kinase (BTK) is central to the survival of malignant and normal B-lymphocytes and has been a crucial therapeutic target of several generations of kinase inhibitors and newly developed degraders.
Vindhya Nawaratne, Anya K. Sondhi, Omar Abdel-Wahab, Justin Taylor   +3 more
semanticscholar   +1 more source

Involvement of Bruton's tyrosine kinase in FcepsilonRI-dependent mast cell degranulation and cytokine production. [PDF]

, 1998
We investigated the role of Bruton's tyrosine kinase (Btk) in FcepsilonRI-dependent activation of mouse mast cells, using xid and btk null mutant mice.
Alt, FW, Galli, SJ, Goldfeld, AE, Han, W, Hartman, SE, Hata, D, Inagaki, N, Kawakami, T, Kawakami, Y, Khan, WN, Kitamura, T, Lantz, CS, Maeda-Yamamoto, M, Miura, T, Nagai, H, Witte, ON, Yao, L   +16 more
core  

Structure-Function Relationships of Covalent and Non-Covalent BTK Inhibitors

Frontiers in Immunology, 2021
Low-molecular weight chemical compounds have a longstanding history as drugs. Target specificity and binding efficiency represent major obstacles for small molecules to become clinically relevant. Protein kinases are attractive cellular targets; however,
R. Zain, M. Vihinen
semanticscholar   +1 more source

Artificial intelligence strategies for predicting kinase inhibitor resistance: A comprehensive review of methods, challenges, and future perspectives

Journal of Intelligent Medicine, EarlyView.
Abstract Kinase inhibitors are essential in targeted cancer therapy, yet resistance often emerges through secondary mutations, activation of compensatory signaling pathways, or drug‐efflux mechanisms. Artificial intelligence (AI) provides a workflow‐based strategy rather than a list of unrelated tools for predicting and addressing kinase‐inhibitor ...
Faris Hassan, Mohanad Ali Deifallah, Alaa Zaghloul, Rania Elgohary   +3 more
wiley   +1 more source

Quantitative Systems Pharmacology Model to Predict Target Occupancy by Bruton Tyrosine Kinase Inhibitors in Patients With B‐Cell Malignancies

CPT: Pharmacometrics & Systems Pharmacology
The effectiveness of Bruton tyrosine kinase (BTK) inhibitors is influenced by the level of BTK occupancy in target tissues. In randomized phase 3 studies, progression‐free survival (PFS) with zanubrutinib was superior to ibrutinib, whereas acalabrutinib ...
Oleg Demin Jr, Ying Ou, Galina Kolesova, Dmitry Shchelokov, Alexander Stepanov, Veronika Musatova, Sri Sahasranaman, Yating Zhao, Xiangyu Liu, Zhiyu Tang, William D. Hanley   +10 more
doaj   +1 more source

Prolonged and tunable residence time using reversible covalent kinase inhibitors. [PDF]

, 2015
Drugs with prolonged on-target residence times often show superior efficacy, yet general strategies for optimizing drug-target residence time are lacking.
Angelina Bisconte, Dane E. Karr, Danny Tam, David Finkle, David G. Loughhead, David M. Goldstein, Erik Verner, J. Hill, J. Michael Bradshaw, Jack Taunton, Jens Oliver Funk, Jesse M. Mcfarl, Jin Shu, Ken A. Brameld, Mary E, Philip A. Nunn, Principia Biopharma, Sergei Romanov, Timothy D. Owens, Tony Ton, Vaishali Patel, Vernon T. Phan, Ville O. Paavilainen, Xiaoyan Li   +23 more
core  

Mathematical existence results for the Doi-Edwards polymer model [PDF]

, 2015
In this paper, we present some mathematical results on the Doi-Edwards model describing the dynamics of flexible polymers in melts and concentrated solutions.
Chupin, Laurent
core   +3 more sources

Monitoring and Managing BTK Inhibitor Treatment-Related Adverse Events in Clinical Practice

Frontiers in Oncology, 2021
Bruton tyrosine kinase (BTK) inhibitors represent an important therapeutic advancement for B cell malignancies. Ibrutinib, the first-in-class BTK inhibitor, is approved by the US FDA to treat patients with chronic lymphocytic leukemia (CLL)/small ...
S. O'brien, Jennifer R. Brown, J. Byrd, R. Furman, P. Ghia, J. Sharman, W. Wierda   +6 more
semanticscholar   +1 more source

New Biologic and Small Molecule Therapies for Hidradenitis Suppurativa

JEADV Clinical Practice, EarlyView.
ABSTRACT Hidradenitis suppurativa (HS) is an inflammatory skin disease that has historically been underdiagnosed and, until recently, under‐researched. Furthermore, the pathophysiology of HS is complex, and not fully understood. Just three biologic medications—adalimumab (anti‐TNF‐α), secukinumab (anti‐IL17A) and bimekizumab (anti‐IL17A/F) are licensed
Emily Pender, Rosalind Hughes, Brian Kirby   +2 more
wiley   +1 more source