Results 11 to 20 of about 4,906,436 (344)

Differential effects of selective inhibitors targeting the PI3K/AKT/mTOR pathway in acute lymphoblastic leukemia [PDF]

, 2013
Purpose: Aberrant PI3K/AKT/mTOR signaling has been linked to oncogenesis and therapy resistance in various malignancies including leukemias. In Philadelphia chromosome (Ph) positive leukemias, activation of PI3K by dysregulated BCR-ABL tyrosine kinase ...
Badura, Susanne, Falkenburg, J. H. Frederik, Liebermann, Marcus, Nijmeijer, Bart A., Ottmann, Oliver Gerhard, Pfeifer, Heike, Ruthardt, Martin, Tesanovic, Tamara, Wystub, Sylvia   +8 more
core   +20 more sources

Systematic Exploration of Privileged Warheads for Covalent Kinase Drug Discovery

Pharmaceuticals, 2022
Kinase-targeted drug discovery for cancer therapy has advanced significantly in the last three decades. Currently, diverse kinase inhibitors or degraders have been reported, such as allosteric inhibitors, covalent inhibitors, macrocyclic inhibitors, and ...
Zheng Zhao, Philip E. Bourne
doaj   +1 more source

Discovery of moiety preference by Shapley value in protein kinase family using random forest models

BMC Bioinformatics, 2022
Background Human protein kinases play important roles in cancers, are highly co-regulated by kinase families rather than a single kinase, and complementarily regulate signaling pathways.
Yu-Wei Huang, Yen-Chao Hsu, Yi-Hsuan Chuang, Yun-Ti Chen, Xiang-Yu Lin, You-Wei Fan, Nikhil Pathak, Jinn-Moon Yang   +7 more
doaj   +1 more source

Treatment of anaplastic lymphoma kinase-positive lung adenocarcinoma with pemetrexed and carboplatin after crizotinib failure and significant liver dysfunction; a case report

Cancer Treatment and Research Communications, 2021
Tyrosine kinase inhibitors are the first-line treatment for Anaplastic Lymphoma Kinase-positive lung adenocarcinomas. However, chemotherapy is still an option in patients who are unresponsive or intolerant of tyrosine kinase inhibitors.
Oranus Mohammadi, Kayla Haines, Mohammad Jahanzeb   +2 more
doaj   +1 more source

Kinase Inhibitors as Underexplored Antiviral Agents

Journal of Medicinal Chemistry, 2021
Viral infections are a major health problem; therefore, there is an urgent need for novel therapeutic strategies. Antivirals used to target proteins encoded by the viral genome usually enhance drug resistance generated by the virus.
Javier García-Cárceles, E. Caballero, C. Gil, Ana Martínez   +3 more
semanticscholar   +1 more source

Systematic screening identifies ABCG2 as critical factor underlying synergy of kinase inhibitors with transcriptional CDK inhibitors

Breast Cancer Research, 2023
Background Triple-negative breast cancer (TNBC) is a subtype of breast cancer with limited treatment options and poor clinical prognosis. Inhibitors of transcriptional CDKs are currently under thorough investigation for application in the treatment of ...
Vera E. van der Noord, Wanda van der Stel, Gijs Louwerens, Danielle Verhoeven, Hendrik J. Kuiken, Cor Lieftink, Melanie Grandits, Gerhard F. Ecker, Roderick L. Beijersbergen, Peter Bouwman, Sylvia E. Le Dévédec, Bob van de Water   +11 more
doaj   +1 more source

Structural features of the protein kinase domain and targeted binding by small-molecule inhibitors

Journal of Biological Chemistry, 2022
Protein kinases are key components in cellular signaling pathways as they carry out the phosphorylation of proteins, primarily on Ser, Thr, and Tyr residues.
C. Arter, Luke Trask, Sarah J. Ward, S. Yeoh, R. Bayliss   +4 more
semanticscholar   +1 more source

Overview of Research into mTOR Inhibitors

Molecules, 2022
The mammalian target of rapamycin (mTOR) is a serine/threonine kinase that belongs to the phosphoinositide 3-kinase (PI3K)-related kinase (PIKK) family.
Beibei Mao, Qi Zhang, Li Ma, Dong-Sheng Zhao, Pan Zhao, Peizheng Yan   +5 more
doaj   +1 more source

Tyrosine kinase inhibitors for solid tumors in the past 20 years (2001–2020)

Journal of Hematology & Oncology, 2020
Tyrosine kinases are implicated in tumorigenesis and progression, and have emerged as major targets for drug discovery. Tyrosine kinase inhibitors (TKIs) inhibit corresponding kinases from phosphorylating tyrosine residues of their substrates and then ...
Liling Huang, Shiyu Jiang, Yuankai Shi
semanticscholar   +1 more source

Insights into the binding mode of MEK type-III inhibitors. A step towards discovering and designing allosteric kinase inhibitors across the human kinome. [PDF]

PLoS ONE, 2017
Protein kinases are critical drug targets for treating a large variety of human diseases. Type-III kinase inhibitors have attracted increasing attention as highly selective therapeutics.
Zheng Zhao, Lei Xie, Philip E Bourne
doaj   +1 more source