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Relevant bibliographies by topics / Dual inhibitors

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Dissertations / Theses

Academic literature on the topic 'Dual inhibitors'

Author: Grafiati

Published: 24 August 2024

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Dissertations / Theses on the topic "Dual inhibitors"

1

Meschini, Elisa. "Purine-based dual inhibitors of CDK2 and CDK7." Thesis, University of Newcastle Upon Tyne, 2011. http://hdl.handle.net/10443/1363.

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Cyclin-Dependent Kinases (CDKs) play a fundamental role in eukaryotic cell cycle progression, particularly at cell cycle checkpoints, and are therefore important targets for anticancer drug discovery. Activation of CDK2 in complex with Cyclin A regulates entry into S phase of the eukaryotic cell cycle. CDK7, a dual-function enzyme, acts both as a CDK-Activating Kinase (CAK) and as a component of the general transcription factor TFIIH. However, experiments with MAT1-knockdown mice have shown that cell cycle arrest by CAK inhibition would not be detrimental for transcriptional activity in non-di

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2

Green, Ian. "The biology of novel dual histone methyltransferase inhibitors." Thesis, Imperial College London, 2015. http://hdl.handle.net/10044/1/25763.

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Background: EZH2 is a histone methyltransferase (HKMT) responsible for the maintenance of epigenetic silencing of genes through maintenance of the repressive H3K27me3 mark and it is aberrantly regulated in numerous cancers, including breast cancer where it is linked to aggressive phenotypes and poor clinical outcomes. EHMT2 is a related HKMT responsible for gene silencing by mediating H3K9me3 levels. EHMT2 is also responsible for H3K27me1 and has been shown to physically interact with EZH2. Specific inhibitors of EZH2 are available and have been shown to be effective in cancers with EZH2 mutat

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3

Apsel, Beth. "Dual-specificity inhibitors of lipid and protein kinases." Diss., Search in ProQuest Dissertations & Theses. UC Only, 2008. http://gateway.proquest.com/openurl?url_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:dissertation&res_dat=xri:pqdiss&rft_dat=xri:pqdiss:3311357.

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4

Ren, Baiping. "Molecular Design and Discovery of Single and Dual Inhibitors of Amyloid Peptides." University of Akron / OhioLINK, 2019. http://rave.ohiolink.edu/etdc/view?acc_num=akron1555257099229697.

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5

Wong, Jacky Sui Ki. "The Evaluation of Dual PI3K/mTOR Inhibitors as a Superior Alternative to mTOR Inhibitors in Pre-B Acute Lymphoblastic Leukaemia." Thesis, The University of Sydney, 2014. http://hdl.handle.net/2123/13644.

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Acute lymphoblastic leukaemia (ALL) is the most common form of cancer in children. Poor long term survival in adults as well as the bleak outlook for relapsed patients highlights the need for new therapeutic strategies for the treatment of ALL. The major regulators of ALL cell proliferation and survival mediate their effects through the phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin. It has been previously shown that the mTOR inhibitor RAD001 extended survival in a non-obese diabetic/severe combined immune deficient (NOD/SCID) mouse xenograft model of ALL. The work presente

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6

Fraser, Sasha. "Development of Dual-Pathway Inhibitors of Raf/MEK/ERK and PI3K/Akt Signaling Pathways." VCU Scholars Compass, 2011. http://scholarscompass.vcu.edu/etd/2619.

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In the present study, we designed a new chemical template that contains an oxindole moiety as potential dual-pathway inhibitors of the Raf/MEK/ERK and PI3K/Akt signaling pathways. The design hypothesis is to evaluate whether the oxindole ring system will approximately orient functional groups in a similar manner to the thiazolidinedione moiety, and thus maintain biological activity as dual-pathway inhibitors of the Raf/MEK/ERK and PI3K/Akt signaling pathways. Furthermore, the oxindole ring will provide the flexibility to allow the introduction of various substituents on the oxindole moiety, th

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7

Steinemann, Gustav [Verfasser]. "Charakterisierung der Wirkmechanismen des neuartigen, dual wirksamen HDAC-Inhibitors „Animacroxam“ am Beispiel testikulärer Keimzelltumore / Gustav Steinemann." Berlin : Medizinische Fakultät Charité - Universitätsmedizin Berlin, 2021. http://d-nb.info/1234984474/34.

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8

Tamhaev, Rasoul. "Conception, synthèse et caractérisation de dérivés diaryl éthers comme nouveaux inhibiteurs directs de la protéine InhA de Mycobacterium tuberculosis." Electronic Thesis or Diss., Université de Toulouse (2023-....), 2024. http://thesesups.ups-tlse.fr/6088/.

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La tuberculose, bien que maladie très ancienne, est toujours une des causes majeures de mortalité due à un agent infectieux unique. En 2021, 10 millions de personnes ont contracté la maladie et 1.5 millions de décès étaient directement imputables à cette dernière. Malgré la disponibilité de toute une panoplie d'antibiotiques, peu d'entre eux s'avèrent efficaces contre l'agent pathogène responsable de la tuberculose, Mycobacterium tuberculosis. Cette inefficacité est principalement due au caractère imperméable de l'enveloppe cellulaire mycobactérienne, composée majoritairement d'acides mycoliqu

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9

Yule, Ian Andrew. "Design, synthesis and biological evaluation of novel, dual targeting inhibitors of bacterial DNA gyrase and topoisomerase IV." Thesis, University of Leeds, 2012. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.713881.

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The inevitability of bacterial drug resistance to all marketed antibiotic drug classes warrants continual research into the development of novel chemotype antibacterial agents. Drug resistant `superbugs' such as methicillin resistant Staphylococcus aureus (MRSA) and vancomycin resistant Enterococci (VRE) account for >70% of US hospital bound bacteremias. Such infections are associated with vastly increased rates of morbidity and mortality resulting in a heavy economic burden on health care authorities. The bacterial topoisomerase enzymes DNA gyrase and topoisomerase IV are highly conserved amo

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10

Foka, Germaine Boulenoue. "Synthesis and evaluation of novel coumarin-donepezil derivatives as dual acting monoamine oxidase B and cholinesterase in Alzheimer's disease." University of the Western Cape, 2016. http://hdl.handle.net/11394/5549.

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Magister Pharmaceuticae - MPharm<br>Alzheimer's disease is a progressive neurodegenerative disease characterised by low acetylcholine (ACh) levels in the hippocampus and cortex of the brain, causing symptoms like progressive memory loss, decline in language skills and other cognitive impairments to occur. The hallmarks of AD include the presence of extracellular insoluble amyloid beta plaques, intracellular neurofibrillary tangles, and the decrease in ACh concentration. The pathophysiology of AD is not well understood, however, acetylcholinesterase (AChE), butyrylcholinesterase (BuChE) and mon

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