Results 21 to 30 of about 7,490 (233)

Disrupting enzyme fluidity

eLife, 2021
A combination of X-ray crystallography, NMR, and mass spectrometry has revealed how diverse small-molecule inhibitors bind Bruton’s tyrosine kinase and alter the conformation of this enzyme.
Ganesh Srinivasan Anand
doaj   +1 more source

Reining in BTK: Interdomain Interactions and Their Importance in the Regulatory Control of BTK

Frontiers in Cell and Developmental Biology, 2021
Since Dr. Ogden Bruton’s 1952 paper describing the first human primary immunodeficiency disease, the peripheral membrane binding signaling protein, aptly named Bruton’s tyrosine kinase (BTK), has been the target of intense study. Dr. Bruton’s description
Lauren E. Kueffer, Raji E. Joseph, Amy H. Andreotti   +2 more
doaj   +1 more source

Nucleocytoplasmic Shuttling of Bruton's Tyrosine Kinase [PDF]

Journal of Biological Chemistry, 2000
Bruton's tyrosine kinase (Btk), a nonreceptor cytoplasmic tyrosine kinase belonging to the Tec family of kinases, has been shown to be critical for B cell proliferation, differentiation, and signaling. Loss-of-function mutations in the Btk gene lead to X-linked agammaglobulinemia (XLA), a primary immunodeficiency in humans, and the less severe ...
A J, Mohamed, L, Vargas, B F, Nore, C M, Backesjo, B, Christensson, C I, Smith   +5 more
openaire   +2 more sources

Managing toxicities of Bruton tyrosine kinase inhibitors [PDF]

Hematology, 2020
Abstract Inhibition of Bruton’s tyrosine kinase (BTK) has revolutionized the treatment landscape for patients with chronic lymphocytic leukemia (CLL). By targeting this critical kinase in proximal B-cell receptor signaling, BTK inhibitors (BTKis) impair cell proliferation, migration, and activation of NF-κB.
Andrew, Lipsky, Nicole, Lamanna
openaire   +2 more sources

BTK (Bruton agammaglobulinemia tyrosine kinase) [PDF]

Atlas of Genetics and Cytogenetics in Oncology and Haematology, 2011
Review on BTK (Bruton agammaglobulinemia tyrosine kinase), with data on DNA, on the protein encoded, and where the gene is implicated.
Hendriks, RW, van, Loo PF
openaire   +2 more sources

Bruton tyrosine kinase inhibitors for multiple sclerosis

Nature Reviews Neurology, 2023
Current therapies for multiple sclerosis (MS) reduce both relapses and relapse-associated worsening of disability, which is assumed to be mainly associated with transient infiltration of peripheral immune cells into the central nervous system (CNS). However, approved therapies are less effective at slowing disability accumulation in patients with MS ...
Julia Krämer, Amit Bar-Or, Timothy J. Turner, Heinz Wiendl   +3 more
openaire   +2 more sources

Bruton's Tyrosine Kinase Inhibitors: Recent Updates. [PDF]

Int J Mol Sci
Bruton’s tyrosine kinase (BTK) inhibitors have revolutionized the landscape for the treatment of hematological malignancies, solid tumors, and, recently, autoimmune disorders. The BTK receptor is expressed in several hematopoietic cells such as macrophages, neutrophils, mast cells, and osteoclasts.
Fares A, Carracedo Uribe C, Martinez D, Rehman T, Silva Rondon C, Sandoval-Sus J.   +5 more
europepmc   +3 more sources

Targeting BTK for the treatment of FLT3-ITD mutated acute myeloid leukemia [PDF]

, 2015
Approximately 20% of patients with acute myeloid leukaemia (AML) have a mutation in FMS-like-tyrosine-kinase-3 (FLT3). FLT3 is a trans-membrane receptor with a tyrosine kinase domain which, when activated, initiates a cascade of phosphorylated proteins ...
A Puissant, AJ Mohamed, BD Smith, BJ Druker, C Chung, C Dos Santos, C Thiede, C Venkataraman, CC Smith, CK Hahn, F Heidel, F Honda, G Juliusson, H Kiyoi, HS Ma, J Adolfsson, JA Dubovsky, JA Dubovsky, JA Woyach, JA Woyach, JB Petro, K Fiedler, KU Birkenkamp, L Zaitseva, M Levis, M Nakao, ML Wang, N Feldhahn, NJ Horwood, PP Zarrinkar, Q Xu, RF Schlenk, RM Stone, S Knapper, S Meshinchi, SA Ezell, SA Rushworth, SA Rushworth, SA Rushworth, SA Rushworth, T Kindler, T Matsunaga, T Oellerich, T-l Gu, V Vijayan, W Gao, Y Alvarado, Y Baba, Y Yamamoto, Y-T Tai   +49 more
core   +2 more sources

A covalent BTK ternary complex compatible with targeted protein degradation

Nature Communications, 2023
Bridging covalent ligand discovery with chimeric degrader design has emerged as a mechanism to target proteins that lack enzymatic activity or are intractable.
James Schiemer, Andrew Maxwell, Reto Horst, Shenping Liu, Daniel P. Uccello, Kris Borzilleri, Nisha Rajamohan, Matthew F. Brown, Matthew F. Calabrese   +8 more
doaj   +1 more source

The role of B-cell receptor inhibitors in the treatment of patients with chronic lymphocytic leukemia

Haematologica, 2015
Chronic lymphocytic leukemia is a malignancy of mature auto-reactive B cells. Genetic and functional studies implicate B-cell receptor signaling as a pivotal pathway in its pathogenesis.
Adrian Wiestner
doaj   +1 more source