Results 291 to 300 of about 4,906,436 (344)
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Anticancer properties of chimeric HDAC and kinase inhibitors.
Seminars in Cancer Biology, 2020Histone deacetylases (HDACs) are epigenetic regulators of chromatin condensation and decondensation and exert effects on the proliferation and spread of cancer. Thus, HDAC enzymes are promising drug targets for the treatment of cancer.
B. Biersack, Sibel Polat, M. Höpfner
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Current Pharmaceutical Design, 2012
In the last decade kinase inhibitors have emerged as a new class of very potent and relatively safe anticancer drugs. However, despite their success, off-target toxicities and induction of rapid resistance are major drawbacks that highly compromise successful longterm administration.
Harmsen, S,, Kok, R.J.
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In the last decade kinase inhibitors have emerged as a new class of very potent and relatively safe anticancer drugs. However, despite their success, off-target toxicities and induction of rapid resistance are major drawbacks that highly compromise successful longterm administration.
Harmsen, S,, Kok, R.J.
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Kinase Inhibitors: Not Just for Kinases Anymore
Journal of Medicinal Chemistry, 2003Kinase inhibitors are widely employed as biological reagents and as leads for drug design. Their use is often complicated by their lack of specificity. Although binding conserved ATP sites accounts for some of their nonspecificity, some compounds inhibit proteins not known to bind ATP.
Susan L, McGovern, Brian K, Shoichet
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Approach in Improving Potency and Selectivity of Kinase Inhibitors: Allosteric Kinase Inhibitors
Mini-Reviews in Medicinal Chemistry, 2021Allostery is an efficient and particular regulatory mechanism to regulate protein functions. Different from conserved orthosteric sites, allosteric sites have a distinctive functional mechanism to form the complex regulatory network. In drug discovery, kinase inhibitors targeting the allosteric pockets have received extensive attention for the ...
Shangfei, Wei +3 more
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Kinase dysfunction and kinase inhibitors
Veterinary Dermatology, 2013With recent advances in molecular biology, abnormalities in cancer cells that contribute to dysregulation of cell survival and proliferation are being characterized with greater precision. Through this process, key abnormalities in cancer cells involving proteins that regulate signal transduction, migration, mitosis and other critical processes have ...
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Covalent‐Allosteric Kinase Inhibitors
Angewandte Chemie International Edition, 2015AbstractTargeting and stabilizing distinct kinase conformations is an instrumental strategy for dissecting conformation‐dependent signaling of protein kinases. Herein the structure‐based design, synthesis, and evaluation of pleckstrin homology (PH) domain‐dependent covalent‐allosteric inhibitors (CAIs) of the kinase Akt is reported.
Weisner, Jörn +14 more
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New Promise and Opportunities for Allosteric Kinase Inhibitors.
Angewandte Chemie, 2019Drugs that function through allosteric inhibition of kinase signaling represent a promising approach for the targeted discovery of therapeutics with exceptional selectivity.
Xiaoyun Lu, J. Smaill, Ke Ding
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2013
Pulmonary arterial hypertension (PAH) is a fatal disease with poor prognosis characterized by progressive elevation of pulmonary arterial pressure and vascular resistance due to pulmonary artery hyperconstriction and remodeling; however, the precise mechanism of PAH still remains to be elucidated.
Yoshihiro, Fukumoto, Hiroaki, Shimokawa
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Pulmonary arterial hypertension (PAH) is a fatal disease with poor prognosis characterized by progressive elevation of pulmonary arterial pressure and vascular resistance due to pulmonary artery hyperconstriction and remodeling; however, the precise mechanism of PAH still remains to be elucidated.
Yoshihiro, Fukumoto, Hiroaki, Shimokawa
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European journal of medicinal chemistry, 2019
The 4-aminoquinazoline core is an interesting pharmacophore and its applications in medicinal chemistry are wide spread. The core has been used for making many kinase inhibitors in past few years.
Debasis Das, Jiann-Ruey Hong
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The 4-aminoquinazoline core is an interesting pharmacophore and its applications in medicinal chemistry are wide spread. The core has been used for making many kinase inhibitors in past few years.
Debasis Das, Jiann-Ruey Hong
semanticscholar +1 more source
Nihon rinsho. Japanese journal of clinical medicine, 2010
Various kinases phosphorylate their substrates and thereby switch on or off their functions. Dysregulation of kinases that regulate cell growth signals induces carcinogenesis or malignant phenotypes in cancer. Therefore, kinases are considered to be most promising therapeutic targets in cancer treatment, and the development of kinase inhibitors has ...
Takao, Yamori, Dexin, Kong
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Various kinases phosphorylate their substrates and thereby switch on or off their functions. Dysregulation of kinases that regulate cell growth signals induces carcinogenesis or malignant phenotypes in cancer. Therefore, kinases are considered to be most promising therapeutic targets in cancer treatment, and the development of kinase inhibitors has ...
Takao, Yamori, Dexin, Kong
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