Results 51 to 60 of about 293,862 (300)

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

Spatiotemporal and quantitative analyses of phosphoinositides – fluorescent probe—and mass spectrometry‐based approaches

FEBS Letters, EarlyView.
Fluorescent probes allow dynamic visualization of phosphoinositides in living cells (left), whereas mass spectrometry provides high‐sensitivity, isomer‐resolved quantitation (right). Their synergistic use captures complementary aspects of lipid signaling. This review illustrates how these approaches reveal the spatiotemporal regulation and quantitative
Hiroaki Kajiho, Shin Morioka, Junko Sasaki, Takehiko Sasaki   +3 more
wiley   +1 more source

Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. [PDF]

, 2008
The clinical success of multitargeted kinase inhibitors has stimulated efforts to identify promiscuous drugs with optimal selectivity profiles. It remains unclear to what extent such drugs can be rationally designed, particularly for combinations of ...
Aizenstein, Brian, Apsel, Beth, Blair, Jimmy A, Feldman, Morri E, Gonzalez, Beatriz, Hoffman, Randy, Knight, Zachary A, Nazif, Tamim M, Shokat, Kevan M, Williams, Roger L   +9 more
core  

Cell wall target fragment discovery using a low‐cost, minimal fragment library

FEBS Letters, EarlyView.
LoCoFrag100 is a fragment library made up of 100 different compounds. Similarity between the fragments is minimized and 10 different fragments are mixed into a single cocktail, which is soaked to protein crystals. These crystals are analysed by X‐ray crystallography, revealing the binding modes of the bound fragment ligands.
Kaizhou Yan, Mathew Stanley, Olawale Raimi, Andrew T. Ferenbach, Helge C Dorfmueller, Daan M. F. van Aalten   +5 more
wiley   +1 more source

Differential responsiveness of MET inhibition in non-small-cell lung cancer with altered CBL. [PDF]

, 2017
Casitas B-lineage lymphoma (CBL) is an E3 ubiquitin ligase and a molecule of adaptor that we have shown is important for non-small-cell lung cancer (NSCLC). We investigated if MET is a target of CBL and if enhanced in CBL-altered NSCLC.
Batra, Surinder K, Husain, Aliya N, Mirzapoiazova, Tamara, Salgia, Ravi, Sharma, Sherven, Srivastava, Minu K, Tan, Yi-Hung Carol, Vokes, Everett E, Won, Brian M, Zhu, Li   +9 more
core   +1 more source

Organizing the interface—Plasma membrane architecture and receptor dynamics in virus‐cell interactions

FEBS Letters, EarlyView.
Plasma membranes contain dynamic nanoscale domains that organize lipids and receptors. Because viruses operate at similar scales, this architecture shapes early infection steps, including attachment, receptor engagement, and entry. Using influenza A virus and HIV‐1 as examples, we highlight how receptor nanoclusters, multivalent glycan interactions ...
Jan Schlegel, Christian Sieben
wiley   +1 more source

Role of Non Receptor Tyrosine Kinases in Hematological Malignances and its Targeting by Natural Products

Molecular Cancer, 2018
Tyrosine kinases belong to a family of enzymes that mediate the movement of the phosphate group to tyrosine residues of target protein, thus transmitting signals from the cell surface to cytoplasmic proteins and the nucleus to regulate physiological ...
Kodappully S. Siveen, Kirti S. Prabhu, Iman W. Achkar, Shilpa Kuttikrishnan, Sunitha Shyam, Abdul Q. Khan, Maysaloun Merhi, Said Dermime, Shahab Uddin   +8 more
doaj   +1 more source

Transcriptional network analysis of PTEN‐protein‐deficient prostate tumors reveals robust stromal reprogramming and signs of senescent paracrine communication

Molecular Oncology, EarlyView.
Combining PTEN protein assessment and transcriptomic profiling of prostate tumors, we uncovered a network enriched in senescence and extracellular matrix (ECM) programs associated with PTEN loss and conserved in a mouse model. We show that PTEN‐deficient cells trigger paracrine remodeling of the surrounding stroma and this information could help ...
Ivana Rondon‐Lorefice, Jose I. Lopez, Aitziber Ugalde‐Olano, Maite Zufiaurre, Ianire Astobiza, Natalia Martin‐Martin, Laura Bozal‐Basterra, Saioa Garcia‐Longarte, Amaia Zabala‐Letona, Sofia Rey, Aida Santos‐Martin, Miguel Unda, Ana Loizaga‐Iriarte, Mariona Graupera, Paolo Nuciforo, Arkaitz Carracedo, Isabel Mendizabal   +16 more
wiley   +1 more source

JAK inhibitors: a new choice for diabetes mellitus?

Diabetology & Metabolic Syndrome
Altered tyrosine kinase signaling is associated with a variety of diseases. Tyrosine kinases can be classified into two groups: receptor type and nonreceptor type. Nonreceptor-type tyrosine kinases are subdivided into Janus kinases (JAKs), focal adhesion
Mengjun Zhou, Qi Shen, Bo Li
doaj   +1 more source

New targets for resolution of airway remodeling in obstructive lung diseases. [PDF]

, 2018
Airway remodeling (AR) is a progressive pathological feature of the obstructive lung diseases, including asthma and chronic obstructive pulmonary disease (COPD).
Deshpande, Deepak A., Nayak, Ajay P., Penn, Raymond B   +2 more
core   +2 more sources