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Dissertations / Theses on the topic 'Integrin-targeting'

Author: Grafiati

Published: 3 June 2025

Last updated: 31 July 2025

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1

Pilkington-Miksa, Michael. "The synthesis of modified integrin-targeting peptides for incorporation into lipid/integrin-targeting peptide/DNA transfection complexes." Thesis, University College London (University of London), 2005. http://discovery.ucl.ac.uk/1445789/.

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Integrin-targeting peptides have been shown to increase transfection efficiency when included in a number of different non-viral vectors. In the case of Lipofectin/DN A complexes (LD), transfection efficiency has been shown to increase on incorporation of an integrin- targeting peptide (Lipid/Integrin-targeting peptide/DNA complexes), as seen by a 100-fold increase in luciferase expression. Efforts to improve the Lipofectin component of Lipid/Integrin-targeting peptide/DNA complexes continue to be made and consequently ways of increasing transfection efficiency through modifications to the int

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2

DiCara, Danielle. "Targeting alpha v beta 6 integrin for cancer imaging." Thesis, Queen Mary, University of London, 2006. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.522319.

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3

Forgey, Cady. "Prevention of Chronic Inflammation by Targeting Macrophage Integrin aDb2." Digital Commons @ East Tennessee State University, 2020. https://dc.etsu.edu/etd/3849.

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Macrophage integrin aDb2 promotes macrophage retention and accumulation within inflamed tissue, a key event in development of chronic inflammation. Recently, the P5 peptide was identified as a specific inhibitor for integrin aDb2 interaction with 2-(ω-carboxyethyl) pyrole (CEP), a ligand at inflammatory sites. This thesis aims to identify integrin aD I-domain amino acids involved in binding P5 peptide and likewise to CEP. We propose that non-conserved, basic amino acids of the integrin aDb2 I-domain are responsible for binding to P5 peptide and likewise to CEP. Eight amino acids were analyzed

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4

Waterhouse, Jodie Elizabeth. "Synthesis and application of integrin targeting lipopeptides in gene therapy." Thesis, Imperial College London, 2004. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.405829.

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5

Emmons, Michael Foster. "Targeting α4 Integrin Containing Complexes in Multiple Myeloma Using Peptidomimetics". Scholar Commons, 2012. http://scholarcommons.usf.edu/etd/4314.

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In our previous work we demonstrated that the integrin antagonist, HYD1, induced necrotic cell death in myeloma cell lines in vitro and in vivo as a single agent. In order to further delineate biomarkers of response to HYD1 we developed an isogenic drug resistant variant named H929-60. We show that the acquisition of resistance towards HYD1 correlates with reduced expression of the cleaved α4 integrin subunit and beta 1 integrin. Moreover, we demonstrate that HYD1 interacts with α4 integrin in myeloma cells. Consistent with reduced VLA-4 expression, the resistant variant showed ablated funct

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6

Brunton, Fiona. "Targeting the osteoclast alpha v beta 3 integrin by phage display." Thesis, Queen Mary, University of London, 2008. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.511761.

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7

PINA, ARIANNA. "SYNTHESIS OF NEW RGD PEPTIDOMIMETIC-DRUG CONJUGATES TARGETING ΑVΒ3 INTEGRIN." Doctoral thesis, Università degli Studi di Milano, 2019. http://hdl.handle.net/2434/606167.

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Abstract Nowadays, systemic administration of cytotoxic agents is one of the main keystones of modern anticancer chemotherapy. However, many drugs do not selectively localize into solid tumors, as they normally accumulate also in healthy organs (e.g. liver and kidney). As a result, severe side effects are caused by the suboptimal biodistribution profile, in combination with the non-specific mode of action of cytotoxic agents, preventing the drug administration at therapeutic doses. The targeted delivery of anticancer agents into solid tumors is emerging as encouraging approach to overcome the

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8

Harbottle, Richard Paul. "Development of a non-viral gene delivery system based on integrin targeting peptides." Thesis, Imperial College London, 2000. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.326256.

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9

CORSO, A. DAL. "TUMOR TARGETING VIA INTEGRIN LIGANDS: SYNTHESIS AND BIOLOGICAL EVALUATION OF RGD PEPTIDOMIMETIC-DRUG CONJUGATES." Doctoral thesis, Università degli Studi di Milano, 2015. http://hdl.handle.net/2434/331100.

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Peptides and peptidomimetics bearing the Arg-Gly-Asp peptide sequence have been demonstrated to bind with high affinity to αvβ3 Integrin, a heterodimeric transmembrane receptor overexpressed in several tumor cells. For these reasons, integrin ligands have been coupled to a variety of anticancer drugs, aiming at the selective delivery of the payload at the tumor site. This PhD work describes the conjugation of the peptidomimetic αvβ3 Integrin ligand cyclo[DKP-RGD] to different anticancer drugs (i.e. paclitaxel, daunorubicin and camptothecin) through peptide and disulfide linkers. The resulting

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10

LOPEZ, RIVAS PAULA. "SYNTHESIS OF INTEGRIN-TARGETING PRO-DRUGS FOR THE SELECTIVE RELEASE OF ANTI-TUMOR AGENTS." Doctoral thesis, Università degli Studi di Milano, 2018. http://hdl.handle.net/2434/584099.

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In this PhD work, a variety of new SMDCs were designed and synthesized featuring different types of linkers and cytotoxic payloads. All of them were characterized and conjugated to peptidomimetic ligands bearing the RGD sequence (namely, the cyclo[DKP-RGD] and cyclo[RDGfK] compounds) aimed at targeting αVβ3 integrin receptor, which is overexpressed in many human cancers. Firstly, six new conjugates containing peptide linkers prone to cleavage in intracellular vesicles (such as the lysosomes) were synthesized and evaluated in vitro. The loss of potency generally displayed by these SMDCs in ant

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11

Raj, April. "Mechanistic studies to evaluate the targeting specificity of novel RGD Micelles to the αVβ3 integrin receptor". Scholarly Commons, 2012. https://scholarlycommons.pacific.edu/uop_etds/830.

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Current chemotherapeutics pose many di sadvantages due to their lack of specificity and low therapeutic index. To overcome these challenges, research has focused its attention on the development of nano-based delivery systems that can penetrate the leaky vasculature of tumor endothelium, use site-directed ligands that can bind with high affinity and specific ity to tumor cells, physically entrap poorly soluble drugs, and deliver these cytotoxic agents directly to the tumor site. One approach to nanosystem drug delivery is with the use of peptide amphiphiles (PAs) that are conjugated with the A

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12

Edwards, Danielle Nichele. "INTEGRIN α5β1 AS A NOVEL TARGET WITH THE SMALL PEPTIDE, ATN-161, IN THE TREATMENT OF ISCHEMIC STROKE". UKnowledge, 2019. https://uknowledge.uky.edu/neurobio_etds/21.

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Stroke is the 5th leading cause of death and the leading cause of disability in the United States, but there are only two available therapies, tissue plasminogen activator and endovascular thrombectomy. As both therapies focus on removal of the clot, the subsequent pathologic processes, i.e. inflammation, cerebrovascular breakdown, ATP depletion, etc. are left untreated, contributing to worsened patient outcome. Many clinical trials have unsuccessfully attempted to address these mechanisms. The blood-brain barrier (BBB), a system of non-fenestrated endothelial cells, extracellular matrix, and

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13

RAPOSO, MOREIRA DIAS ANDRE FILIPE. "SYNTHESIS OF RGD PEPTIDOMIMETIC-DRUG CONJUGATES FOR THE TUMOR-TARGETED DELIVERY OF CYTOTOXIC AGENTS." Doctoral thesis, Università degli Studi di Milano, 2018. http://hdl.handle.net/2434/583313.

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Integrins are a large family of heterodimeric transmembrane glycoprotein receptors, composed by two non-covalently associated subunits (α and β). Integrins αVβ3 and αVβ5 are overexpressed on blood vessels in human tumors but not on vessels in normal tissues and, for this reason, they have become attractive targets for pharmacological studies in oncology. Thus, in this PhD thesis, the synthesis of new Small Molecule-Drug Conjugates (SMDCs) targeting αvβ3 integrin is described. The structure of such SMDCs consists in the connection of three core components: i) LIGAND - the cyclo[DKP-RGD] peptido

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14

White, Elaine Joanna. "Evaluation of receptor-mediated gene transfer using an integrin-targeting vector as a potential form of therapy for lysosomal storage diseases." Thesis, University College London (University of London), 2000. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.340643.

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15

Zanella, S. "SYNTHESIS OF PEPTIDOMIMETIC LIGANDS TARGETING CELL-SURFACE RECEPTORS INVOLVED IN TUMOR ANGIOGENESIS." Doctoral thesis, Università degli Studi di Milano, 2017. http://hdl.handle.net/2434/473075.

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In the first part of the Thesis, the synthesis of different classes of peptidomimetics targeting integrin receptors is described. Both simple ligands and drug conjugates were synthesized and tested to assess their biological activity. In cancer therapy, peptides and peptidomimetics targeting integrins are employed as carriers to deliver cytotoxic drugs at the tumor site, taking advantage of integrin over-expression on the surface of tumor cells. Within this frame, synthetic efforts have been focused on the synthesis and on the conjugation to the cytotoxic agent paclitaxel of isoDGR-based integ

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16

Hahn, Eva Maria [Verfasser], Fritz E. [Akademischer Betreuer] [Gutachter] Kühn, and Joao D. G. [Gutachter] Correia. "Ruthenium and Gold Complexes as potential Anticancer Drugs targeting selectively Integrin Receptors / Eva Maria Hahn ; Gutachter: Fritz E. Kühn, Joao D. G. Correia ; Betreuer: Fritz E. Kühn." München : Universitätsbibliothek der TU München, 2016. http://d-nb.info/1115856383/34.

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17

Saraf, Poonam S. "RGD based peptide amphiphiles as drug carriers for cancer targeting." Scholarly Commons, 2014. https://scholarlycommons.pacific.edu/uop_etds/137.

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Specific interactions of ligands with receptors is one of the approaches for active targeting of anticancer drugs to cancer cells. Over expression of integrin receptors is a physiological manifestation in several cancers and is associated with cancer progression and metastasis, which makes it an attractive target for cancer chemotherapy. The peptide sequence for this integrin recognition is the Arg-Gly-Asp (RGD). Self-assembly offers a unique way of presenting ligands to target receptors for recognition and binding. This study focuses on development of integrin specific peptide amphiphile self

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18

Zhang, Liefen [Verfasser], Yahya [Akademischer Betreuer] Acil, and Medina Oula Antti Rafael [Gutachter] Peñate. "Effect of Cilengitide and Vismodegib on Primary Cell Cultures and Cell Lines of Head and Neck Squamous Cell Carcinoma (HNSCC) after Targeting Integrin and Hedgehog Pathways / Liefen Zhang ; Gutachter: Oula Antti Rafael Peñate Medina ; Betreuer: Yahya Acil." Kiel : Universitätsbibliothek Kiel, 2020. http://d-nb.info/121164930X/34.

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19

Cao, Lizhi. "Development of conformation-sensitive probes to fibronectin for ECM targeting and imaging of fibrosis." Diss., Georgia Institute of Technology, 2014. http://hdl.handle.net/1853/53417.

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Fibronectin (Fn) is an adhesive extracellular matrix protein assembled by fibroblasts into fibrils within ECMs of developing and remodeling tissues. Fn is sensitive to mechanical forces exerted by contractile cells, and can alter its structural conformations in response to mechanical strain within Fn fibrils. We developed probes (both peptide and antibody) to Fn to detect mechano-sensitive perturbations of Fn conformation. Probes were characterized for their binding characteristics (affinity, epitope, mechano-sensitivity) and validated on multiple in vitro and in vivo ECM models. Furthermore,

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20

Lee, Su-Lin. "Targeting the phosphoinositide-dependent protein kinase-2 for anticancer drug discovery." The Ohio State University, 2012. http://rave.ohiolink.edu/etdc/view?acc_num=osu1337980277.

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21

Marusak, Charles. "MT1-MMP: TARGETING THE CENTER OF MELANOMA METASTASIS, GROWTH AND TREATMENT RESISTANCE." Case Western Reserve University School of Graduate Studies / OhioLINK, 2019. http://rave.ohiolink.edu/etdc/view?acc_num=case1548327646756039.

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22

Duret, Damien. "Développement de sondes polymères fluorescentes à propriétés de ciblage améliorées pour des applications en imagerie cellulaire et en oncologie." Thesis, Lyon, 2016. http://www.theses.fr/2016LYSEI060/document.

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Ce travail est axé sur l’amélioration des propriétés de biospécificité de sondes polymères fluorescentes, d’architectures contrôlées synthétisées par polymérisation RAFT, pour deux applications principales : le ciblage de tumeurs cancéreuses in vivo et le marquage de protéines pour des études in cellulo. Pour une imagerie ciblée de l’angiogénèse tumorale in vivo, des systèmes de ciblage multivalents à deux niveaux ont été élaborés en combinant à la fois i) des polymères bien contrôlés synthétisés par polymérisation RAFT et par le procédé PISA, ii) des clusters peptidiques tétravalents présenta

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23

Wang, Hsu-Yuan, and 王栩沅. "Integrin-targeting ferritin nanoparticles for tumor imaging and drug delivery." Thesis, 2017. http://ndltd.ncl.edu.tw/handle/43662993575719339389.

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碩士<br>國立臺灣大學<br>生化科技學系<br>105<br>In tradition, drugs for cancer treatment always belong to a dump release system. Furthermore, people are devoted to developing the new drug delivery for cancer therapy. Recently, liposomes, primarily composed of phospholipids, are the major drug delivery system. However, liposomes still have some disadvantages as follows. In recent years, there are many research for find new drug delivery, and the ferritin is the one of them. Ferritin is composed of 24 subunits and able to self-assemble to form a nanocage structure with external and internal diameters of 12 and

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24

Pellegrini, Paul P. "The synthesis and biological evaluation of integrin receptor targeting molecules as potential radiopharmaceuticals." Thesis, 2008. http://handle.uws.edu.au:8081/1959.7/507131.

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This thesis reports on the synthesis, characterisation and biological evaluation of a number of metal complexes designed to interact with the α vβ3 integrin receptor, an important biological target that is heavily involved in angiogenesis, and thus cancer related processes. Two approaches were used to synthesise the integrin-avid targets. The first was to attach a variety of bifunctional chelators (BFC's) for the incorporation of different metal centres to a known integrin antagonist, L-748,415, developed by Merck. The BFC's used were the hydrazinonicotinamide (HYNIC) and monoamine monoamide d

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25

Shuhendler, Adam Jason. "A Novel Lipid-based Nanotechnology Platform For Biomedical Imaging And Breast Cancer Chemotherapy." Thesis, 2012. http://hdl.handle.net/1807/36253.

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A novel, lipid-based platform nanotechnology has been designed to overcome limitations of in vivo fluorescent imaging, multidrug resistance (MDR) phenotypes hindering breast cancer chemotherapy, and shortcomings of magnetic resonance imaging (MRI) thermometry. Using this platform, three nanoparticle systems have been developed: QD-SLN (quantum dot-loaded solid lipid nanoparticles), DMsPLN (doxorubicin and mitomycin C co-loaded polymer-lipid hybrid nanoparticles), and HLN (hydrogel-lipid hybrid nanoparticles). Stealth, near-infrared emitting QD-SLN were developed for deep tissue fluorescence im

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