Results 21 to 30 of about 1,694,367 (292)

Special Issue: Kinase inhibitors

Molecules, 2018
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Pierre Koch, Stefan Laufer
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Allosteric inhibition enhances the efficacy of ABL kinase inhibitors to target unmutated BCR-ABL and BCR-ABL-T315I [PDF]

, 2012
Background: Chronic myelogenous leukemia (CML) and Philadelphia chromosome-positive (Ph+) acute lymphatic leukemia (Ph + ALL) are caused by the t(9;22), which fuses BCR to ABL resulting in deregulated ABL-tyrosine kinase activity.
Ruimi, Nili, Martin Ruthardt, Mahajna, Jamal, Khateb, Mamduh, Jamal Mahajna, Ruthardt, Martin, Ottmann, Oliver G., Oliver Gerhard Ottmann, Mian, Afsar Ali, Nili Ruimi, Yousef Najajreh, Afsar Ali Mian, Ottmann, Oliver Gerhard, Susanne Badura, Metodieva, Anna, Najajreh, Yousef, Anna Metodieva, Mamduh Khateb, Badura, Susanne   +18 more
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6-Br-5methylindirubin-3′oxime (5-Me-6-BIO) targeting the leishmanial glycogen synthase kinase-3 (GSK-3) short form affects cell-cycle progression and induces apoptosis-like death: Exploitation of GSK-3 for treating leishmaniasis [PDF]

, 2009
Indirubins known to target mammalian cyclin-dependent kinases (CDKs) and glycogen synthase kinase (GSK-3) were tested for their antileishmanial activity.
Smirlis, Despina, Soteriadou, Ketty, Myrianthopoulos, Vassilios, Meijer, Laurent, Prokopios, Magiatis, Grant, Karen, Mikros, Emmanuel, Xingi, Evangelia, Skaltsounis, Alexios-Leandros   +8 more
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Advances in RIPK1 kinase inhibitors

Frontiers in Pharmacology, 2022
Programmed necrosis is a new modulated cell death mode with necrotizing morphological characteristics. Receptor interacting protein 1 (RIPK1) is a critical mediator of the programmed necrosis pathway that is involved in stroke, myocardial infarction ...
Lu Chen, Lu Chen, Xiaoqin Zhang, Yaqing Ou, Maoyu Liu, Maoyu Liu, Dongke Yu, Dongke Yu, Zhiheng Song, Lihong Niu, Lijuan Zhang, Lijuan Zhang, Jianyou Shi, Jianyou Shi   +13 more
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Combinatorial strategy using protein kinase inhibitors and a cytotoxic compound for highly resistant glioblastoma cells : "in vitro studies" [PDF]

, 2007
Glioblastoma multiforme (GBM) is the most frequent and the most aggesssive malignant neoplasm of the human central nervous system (CNS), with a median survival of less than one year. These neoplasms are radio- and chemo-resistant, and are highly invasive,
Failly, Mike
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Analysis of Tumor Heterogeneity Through AXL Activation in Primary Resistance to EGFR Tyrosine Kinase Inhibitors

JTO Clinical and Research Reports, 2023
Introduction: EGFR tyrosine kinase inhibitors are standard therapeutic agents for patients with advanced NSCLC harboring EGFR mutations. Nevertheless, some patients exhibit primary resistance to EGFR tyrosine kinase inhibitors in the first-line treatment
Ryota Nakamura, MD, Hiroyuki Fujii, MD, Tadaaki Yamada, MD, PhD, Yohei Matsui, MD, Takeshi Yaoi, MS, Mizuki Honda, MD, Noriyuki Tanaka, MD, PhD, Aya Miyagawa-Hayashino, MD, PhD, Akihiro Yoshimura, MD, PhD, Kenji Morimoto, MD, PhD, Masahiro Iwasaku, MD, PhD, Shinsaku Tokuda, MD, PhD, Young Hak Kim, MD, PhD, Eiichi Konishi, MD, PhD, Kyoko Itoh, MD, PhD, Koichi Takayama, MD, PhD   +15 more
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Selective anticancer activity of a hexapeptide with sequence homology to a non-kinase domain of Cyclin Dependent Kinase 4 [PDF]

, 2011
Background: cyclin-dependent kinases 2, 4 and 6 (Cdk2, Cdk4, Cdk6) are closely structurally homologous proteins which are classically understood to control the transition from the G1 to the S-phases of the cell cycle by combining with their appropriate ...
Maurer, RI, Jon W Essex, Warenius Hilmar M, Kilburn, Jeremy D., Richard I Maurer, Seabra, LA, Usha Agarwala, Laurence A Seabra, Warenius, Hilmar M., Warenius, HM, Blaydes, JP, Seabra Laurence A, Jeremy D Kilburn, Essex, JW, Agarwala, U, Essex Jon W, Agarwala, Usha, Blaydes Jeremy P, Essex, Jon W., Jeremy P Blaydes, Maurer, Richard I., Agarwala Usha, Seabra, Laurence A., Kilburn Jeremy D, Hilmar M Warenius, Blaydes, Jeremy P., Maurer Richard I, Kilburn, Jeremy D, Kilburn, JD   +28 more
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Flavopiridol Protects Against Inflammation by Attenuating Leukocyte-Endothelial Interaction via Inhibition of Cyclin-Dependent Kinase 9 [PDF]

, 2011
Objective: The cyclin-dependent kinase (CDK) inhibitor flavopiridol is currently being tested in clinical trials as anticancer drug. Beyond its cell death–inducing action, we hypothesized that flavopiridol affects inflammatory processes.
Mayer, Bettina A., Nina Berberich, Stefan Zahler, Sass, Gabriele, Fritz Krombach, Vollmar, Angelika M., Tiegs, Gisa, Krombach, Fritz, Fürst, Robert, Robert Fürst, Totzke, Frank, Angelika M. Vollmar, Jos Joore, Gisa Tiegs, Berberich, Nina, Alexander G. Khandoga, Bettina A. Mayer, Joore, Jos, Ulrike K. Schmerwitz, Gabriele Sass, Zahler, Stefan, Frank Totzke, Schmerwitz, Ulrike K., Khandoga, Alexander G.   +23 more
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On the origins of enzyme inhibitor selectivity and promiscuity: a case study of protein kinase binding to staurosporine [PDF]

, 2009
Protein kinases are important regulatory enzymes in signal transduction and in cell regulation. Understanding inhibition mechanisms of kinases is important for the further development of new therapies for cancer and inflammatory diseases.
William R. Pitt, Duangrudee Tanramluk, Tom L. Blundell, Adrian Schreyer   +3 more
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Non-linear Deep Neural Network for Rapid and Accurate Prediction of Phenotypic Responses to Kinase Inhibitors

iScience, 2020
Summary: Protein kinase inhibitors are one of the most successful targeted therapies to date. Despite this progress, additional kinase inhibitors are needed to expand the target space as well as overcome drug resistance that has emerged in clinical ...
Siddharth Vijay, Taranjit S. Gujral
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