Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 9 of 9 for “"Integrin antagonists"”.
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Development of screening assays to test novel integrin antagonists in allergic inflammation
… screening (HTS) for identification of novel integrin antagonists for the treatment of ocular allergy and to better understand the mechanisms of action of integrin-mediated levocabastine antiallergic action. Results: This thesis provides evidence that adopting scintillation proximity assay …
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Evaluation of new succinimide-based small molecules as alphavbeta3 integrin antagonists: from design to preliminary biological testing
Integrins are a family of cell surface protein receptors consisting of two subunits, called α and β, involved in several biological processes, including regulation of signalling between cells and other cells or ECM. Integrins are overexpressed in diseases, first of all cancer. Being able to bind …
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Synthetic Methodology and Application of Enamine [2+2] Cyclisations for Cyclobutane Synthesis. Development of Integrin Antagonists as Anticancer Therapeutics Towards a Total Synthesis of Providencin
… cyclobutanes. A library of 30 cyclobutane based integrin antagonists have been designed and synthesised to explore the SAR around the hit dual β3 integrin antagonist ICT9055. Several of which were shown to be highly potent antagonists inhibiting cancer cell adhesion, migration and invasion while …
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Zur Rolle von C5 und [alpha]5[beta]1-Integrin für die Entstehung von renaler Fibrose und mögliche therapeutische Konsequenzen
… as well as specific C5aR-and alpha5beta1-Integrin antagonists to detect the influence of the anaphylatoxin C5a and alpha5beta1-Integrin in the development of renal tubulo-interstitial fibrosis. First, we induced a unilateral ureterobstruction (UUO) in C5 deficient mice and suitable wild …
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Development of in vitro models of invasion for the pharmacological investigation of small molecule inhibitors of tumour progression. Development and validation of a 3-dimensional tumour spheroid invasion model to evaluate the pharmacological effects of novel small molecule β3 integrin antagonists.
… novel targets & therapies. The αIIbβ3 and αvβ3 integrins have been demonstrated to have significant involvement at many stages of the tumour dissemination process including, tumour cell adhesion, migration, metastasis and angiogenesis, and thus the β3 integrins are a potential target for …
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Functional Investigation of Dual αvβ3 and αllbβ3 Integrin Inhibition in Haematological and Solid Tumour Models
… will inhibit cancer progression are required. Integrin adhesion receptors, particularly the RGD-binding integrin subfamily comprising αvβ3, αvβ5, αvβ6, αvβ8, αllbβ3, α5β1, α8β1 and αvβ1 are related to progress and spread of cancer and poor prognosis. Because of the importance of integrin …
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An immunohistopathological and functional investigation of β3 integrin antagonism as a therapeutic strategy in cancer. Characterisation, development, and utilisation of preclinical cancer models to investigate novel ¿3 integrin anatgonists.
… control this process are needed. Antagonism of integrins highly expressed in tumours is one potential strategy. The integrins are transmembrane glycoprotein adhesive receptors. Two of the integrins, αVβ3 and αIIbβ3, are highly expressed in a number of tumours and induce bi-directional signalling …
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Correlation between the expression of integrins and their role in cancer progression. Expression pattern of integrins αvβ3, αvβ5 and α5β1 in clinical and experimental tumour samples
The integrins play a crucial role in cancer cell proliferation, migration, differentiation, survival and angiogenesis. It has been shown that integrin expression is positively correlated to cancer dissemination, this suggests targeting selected integrins as an anti-metastatic strategy. The aim of …
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INTEGRIN ALPHAVBETA3 AS THERAPEUTIC TARGET AND IMAGING BIOMARKER FOR VASCULAR ENDOTHELIAL CELLS AND CANCER EPITHELIAL CELLS
Integrins are heterodimeric transmembrane proteins belonging to a family of cell adhesion receptors evolutionary old and that play pivotal roles in physiological and pathological processes, such as neo-angiogenesis and cancer spreading. Integrins are composed by an extracellular domain, a single …