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Janus kinase inhibitors - their current applications and future prospects [PDF]

Farmacja Polska, 2022
Janus kinase inhibitors are a group of drugs that provide an alternative to conventional therapy for numerous diseases. The most studied drug of this group is tofacitinib.
Natalia Wierzbowska, Karolina Żurawska, Maciej Arciszewski, Arnold Kukowka, Bolesław Banach   +4 more
doaj   +1 more source

Differentiating Inhibitors of Closely Related Protein Kinases with Single- or Multi-Target Activity via Explainable Machine Learning and Feature Analysis

Biomolecules, 2022
Protein kinases are major drug targets. Most kinase inhibitors are directed against the adenosine triphosphate (ATP) cofactor binding site, which is largely conserved across the human kinome.
Christian Feldmann, Jürgen Bajorath
doaj   +1 more source

Pharmacokinetic Boosting of Kinase Inhibitors

Pharmaceutics, 2023
(1) Introduction: Pharmacokinetic boosting of kinase inhibitors can be a strategy to enhance drug exposure and to reduce dose and associated treatment costs.
Niels Westra, Daan Touw, Marjolijn Lub-de Hooge, Jos Kosterink, Thijs Oude Munnink   +4 more
doaj   +1 more source

Comparative kinase and cancer cell panel profiling of kinase inhibitors approved for clinical use from 2018 to 2020

Frontiers in Oncology, 2022
During the last two decades, kinase inhibitors have become the major drug class for targeted cancer therapy. Although the number of approved kinase inhibitors increases rapidly, comprehensive in vitro profiling and comparison of inhibitor activities is ...
Jeffrey J. Kooijman, Wilhelmina E. van Riel, Jelle Dylus, Martine B. W. Prinsen, Yvonne Grobben, Tessa J. J. de Bitter, Antoon M. van Doornmalen, Janneke J. T. M. Melis, Joost C. M. Uitdehaag, Yugo Narumi, Yusuke Kawase, Jeroen A. D. M. de Roos, Nicole Willemsen-Seegers, Guido J. R. Zaman   +13 more
doaj   +1 more source

Development of actionable targets of multi-kinase inhibitors (AToMI) screening platform to dissect kinase targets of staurosporines in glioblastoma cells

Scientific Reports, 2022
Therapeutic resistance to kinase inhibitors constitutes a major unresolved clinical challenge in cancer and especially in glioblastoma. Multi-kinase inhibitors may be used for simultaneous targeting of multiple target kinases and thereby potentially ...
Oxana V. Denisova, Joni Merisaari, Amanpreet Kaur, Laxman Yetukuri, Mikael Jumppanen, Carina von Schantz-Fant, Michael Ohlmeyer, Krister Wennerberg, Tero Aittokallio, Mikko Taipale, Jukka Westermarck   +10 more
doaj   +1 more source

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
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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
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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
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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