Dissertations / Theses on the topic 'Peptide Prodrugs'
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Potok, Stephanie. "Peptide rotaxanes as potential prodrugs." Thesis, University of Edinburgh, 2004. http://hdl.handle.net/1842/12131.
Full textFernandes, Anthony. "Synthetic molecular nanodevices for selective peptide-based therapy." Thesis, University of Edinburgh, 2009. http://hdl.handle.net/1842/4037.
Full textCong, Qiang. "Acylfulvene analogs with spiro-cyclobutane ring and peptide, estrogen prodrugs or illudin /." Diss., Connect to a 24 p. preview or request complete full text in PDF format. Access restricted to UC campuses, 2004. http://wwwlib.umi.com/cr/ucsd/fullcit?p3123660.
Full textTewari, Kunal Mahesh. "Targeted dendrimeric prodrugs for 5-Aminolaevulinic acid photodynamic therapy." Thesis, University of Bath, 2016. https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.715275.
Full textKotamraj, Phanidhara R. "Binding induced enzyme activated methotrexate-α-peptide prodrugs for integrin targeted drug delivery." Scholarly Commons, 2009. https://scholarlycommons.pacific.edu/uop_etds/2619.
Full textElbakay, Jamal A. M. "Synthesis and pharmacological evaluation of novel anti-tumour prodrugs. Synthesis and pharmacological investigations into novel MMP-activated peptide-based prodrugs of methotrexate as potential cancer therapeutics." Thesis, University of Bradford, 2017. http://hdl.handle.net/10454/15102.
Full textElbakay, Jamal Ali Mohamed. "Synthesis and pharmacological evaluation of novel anti-tumour prodrugs : synthesis and pharmacological investigations into novel MMP-activated peptide-based prodrugs of methotrexate as potential cancer therapeutics." Thesis, University of Bradford, 2017. http://hdl.handle.net/10454/15102.
Full textKansara, Viral Mitra Ashim K. "Ocular delivery of peptide ganciclovir prodrugs following subconjunctival injection evaluation of episcleral drug delivery approach /." Diss., UMK access, 2007.
Find full text"A dissertation in pharmaceutical sciences and pharmacology." Advisor: Ashim K. Mitra. Typescript. Vita. Title from "catalog record" of the print edition Description based on contents viewed May 23, 2008. Includes bibliographical references (leaves 210-225). Online version of the print edition.
Twum, Elvis Asare. "Development of prodrugs to deliver super-potent drugs to prostate tumours." Thesis, University of Bath, 2013. https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.608329.
Full textYoussef, Ahmed M. M. "Pharmacological investigations into matrix metalloproteinase-activated anti-tumour prodrugs. In vitro metabolic and pharmacological investigations into a series of colchicine-based peptide prodrugs activated by tumour-expressed matrix metalloproteinases." Thesis, University of Bradford, 2014. http://hdl.handle.net/10454/13982.
Full textYoussef, Ahmed Mohamed Mohamed. "Pharmacological investigations into matrix metalloproteinase-activated anti-tumour prodrugs : in vitro metabolic and pharmacological investigations into a series of colchicine-based peptide prodrugs activated by tumour-expressed matrix metalloproteinases." Thesis, University of Bradford, 2014. http://hdl.handle.net/10454/13982.
Full textEldridge, Joshua A. "SYNTHESIS AND STABILITY STUDIES OF PRODRUGS AND CODRUGS OF NALTREXONE AND 6-β-NALTREXOL." UKnowledge, 2013. http://uknowledge.uky.edu/pharmacy_etds/16.
Full textLee, Kyujin C. "Self-assembled lipopeptide prodrug depot for sustaned [sic] release : design and synthesis of peptide glutamic acid dialkylamides, their self-assembly into tubules, and their stability to proteolytic degradation /." Thesis, Connect to this title online; UW restricted, 1999. http://hdl.handle.net/1773/9276.
Full textLuo, Wen-Lin, and 駱文琳. "1.Oral Absorption Study of Di- and Tri-peptide Mimetic Prodrugs of L-dopa 2.The Synthesis of Adenosine Prodrugs." Thesis, 1996. http://ndltd.ncl.edu.tw/handle/66527812223720660277.
Full text國立臺灣大學
藥學研究所
84
In this study, we prepared a series of di- and tripeptide prodrugs of L-dopa, in which D-phenylglycine or D-p- hydroxyphenylglycine was attached as tools for intestinal delivery. In order to examine whether the absorption of these prodrugs is improved, bioavailability studies of single dose of either dipeptide D-phenylglycine-L-dopa (1) or tripeptide D-p- hydroxyphenylglycine-L-proline-L-dopa (2) were conducted. In comparison with L-dopa (BA=5.93+/-.34%), compound 1 was well absorbed with absolute oral bioavailability of 83.38+/-8.69%, On the other hand, compound 2, was poorly absorbed with oral bioavailability of 0.45+/-0.15%. From this study, we also found that the absorption of L-dopa and compound 2 is a flip-flop model . In summary, the high fraction of oral absorption presented by prodrug 1 indicated that the nonessential amino acid, D- phenylglycine, proved to be a good delivery tool for the improvement of GI absorption of L-dopa. In this study, small portion of L-dopa was released in plasma from these two prodrugs (3.63+/-0.78% for compound 1 and 3.58+/- 0.87% for compound 2). However, i.p. injection of both prodrugs exhibited anti-Parkinsonism effect with activities significantly higher than that of L-dopa. In order to improve the oral absorption of adenosine, we used D- phenylglycine and D-p- hydroxyphenylglycine as delivery tools to be included in the prodrug molecules. Compounds N(Boc)- phenylglycine-adenosine (22), N(Boc)-p-hydroxyphenylglycine-TPDS -adenosine (21)and N( Boc)-phenylglycine-L-glycine-TPDS-adenosine (26) were synthesized. However, the desired prodrug molecules D- phenylglycine-adenosine and D-p-hydroxyphenylglycine-adenosine were unstable and we were unable to isolate the desired products. Conditions for purification and stabilization of the final products have to be investigated before the studies of oral absorption and metabolism are conducted.
Luo, Wen Lin, and 駱文琳. "Oral absorption study of Di-and tri-peptide mimetic prodrugs of L-dopa." Thesis, 1996. http://ndltd.ncl.edu.tw/handle/68567732884882342482.
Full textN'guessan, Ginette. "Synthèse de prodrogues de l’[aza(p-MeO)F⁴]-GHRP-6, α-acyloxyéthyl carbamates, pour réguler le récepteur CD36." Thesis, 2020. http://hdl.handle.net/1866/24154.
Full textA prodrug is a biologically inactive derivative of a drug which after administration undergoes chemical or enzymatic modification to release the active drug at targeted sites of activity. Prodrugs improve physicochemical properties to enable better transport through biological barriers and enhance activity. They are used to improve formulation and administration, to enhance permeability and absorption, to modify distribution profiles and to avoid metabolism and toxicity. The prodrug approach is useful for improving drug delivery. Prodrugs are classified into two types: carrier-linked prodrugs and bio-precursors. In the first case, the parent drug is linked by a covalent bond to an inert carrier or transport moiety. The carrier should not be active or toxic. The active drug is released by a chemical or enzymatic cleavage in vivo. In the second case, the parent drug is converted metabolically or chemically by hydration, oxidation or reduction reactions. Azapeptides employ a semicarbazide as an amino amide surrogate in a peptide analog in which the backbone α-CH is replaced by nitrogen. Through electronic interactions, the semicarbazide favors backbone β-turn geometry due to a combination of urea planarity and hydrazine nitrogen lone pair – lone pair repulsion. Azapeptides have proven therapeutic utility. Some of them exhibit better selectivity, activity and stability than the parent peptides with increased duration of action and improved metabolic stability. Growth hormone releasing peptide-6 (GHRP-6, H-His-D-Trp-Ala-Trp-D-Phe-Lys-NH₂) is a synthetic peptide possessing an affinity for two different receptors: growth hormone secretagogue receptor 1a (GHS-R1a) and cluster of differentiation receptor 36 (CD36). The GHRP-6 azapeptide analogue, [aza(p-MeO)F⁴]-GHRP-6, has exhibited good affinity for CD36 and reduced nitric oxide overproduction in macrophage cells stimulated with the TLR-2 agonist R-FSL-1. Azapeptide ligands of CD36, such as [aza(p-MeO)F⁴]-GHRP-6, offers potential as prototypes for developing treatments of diseases such as atherosclerosis and age-related macular degeneration. A prodrug strategy has been pursued to improve the pharmacokinetic properties, such as duration of action, of [aza(p-MeO)F⁴]-GHRP-6. The first examples of α-acyloxyethyl carbamate peptides have been prepared. Five α-acyloxyethyl carbamate analogues of [aza(p-MeO)F⁴]-GHRP-6 have been synthesized by routes featuring acylation of the resin-bound peptide using different activated α-acyloxyethyl carbonates prior to resin cleavage and side chain deprotection. The evaluation of the activity of the pharmacokinetic properties of the [aza(p-MeO)F⁴]-GHRP-6 prodrugs is currently in progress and will be reported in due time.
Zaman, Hadar, A. G. Bright, Kevin Adams, D. M. Goodall, and Robert T. Forbes. "Characterisation of aggregates of cyclodextrin-drug complexes using Taylor Dispersion Analysis." 2017. http://hdl.handle.net/10454/14020.
Full textThere is a need to understand the nature of aggregation of cyclodextrins (CDs) with guest molecules in increasingly complex formulation systems. To this end an innovative application of Taylor dispersion analysis (TDA) and comparison with dynamic light scattering (DLS) have been carried out to probe the nature of ICT01-2588 (ICT-2588), a novel tumor-targeted vascular disrupting agent, in solvents including a potential buffered formulation containing 10% hydroxypropyl-β-cyclodextrin. The two hydrodynamic sizing techniques give measurement responses are that fundamentally different for aggregated solutions containing the target molecule, and the benefits of using TDA in conjunction with DLS are that systems are characterised through measurement of both mass- and z-average hydrodynamic radii. Whereas DLS measurements primarily resolve the large aggregates of ICT01-2588 in its formulation medium, methodology for TDA is described to determine the size and notably to quantify the proportion of monomers in the presence of large aggregates, and at the same time measure the formulation viscosity. Interestingly TDA and DLS have also distinguished between aggregate profiles formed using HP-β-CD samples from different suppliers. The approach is expected to be widely applicable to this important class of drug formulations where drug solubility is enhanced by cyclodextrin and other excipients.
Gill, Jason H., Paul M. Loadman, Steven D. Shnyder, Patricia A. Cooper, Jennifer M. Atkinson, Morais Goreti Ribeiro, Laurence H. Patterson, and Robert A. Falconer. "Tumor-Targeted Prodrug ICT2588 Demonstrates Therapeutic Activity Against Solid Tumors and Reduced Potential For Cardiovascular Toxicity." 2014. http://hdl.handle.net/10454/8823.
Full textDevelopment of therapeutic strategies for tumor-selective delivery of therapeutics through exploitation of the proteolytic tumor phenotype has significant scope for improvement of cancer treatment. ICT2588 is a peptide-conjugated prodrug of the vascular disrupting agent (VDA) azademethylcolchicine developed to be selectively hydrolyzed by matrix metalloproteinase-14 (MMP-14) within the tumor. In this report, we extend our previous proof-of-concept studies and demonstrate the therapeutic potential of this agent against models of human colorectal, lung, breast, and prostate cancer. In all tumor types, ICT2588 was superior to azademethylcolchicine and was greater or comparable to standard clinically used agents for the respective tumor type. Prodrug activation in clinical human lung tumor homogenates relative to stability in human plasma and liver was observed, supporting clinical translation potential. A major limiting factor to the clinical value of VDAs is their inherent cardiovascular toxicity. No increase in plasma von Willebrand factor (vWF) levels, an indicator of systemic vascular dysfunction and acute cardiovascular toxicity, was detected with ICT2588, thereby supporting the tumor-selective activation and reduced potential of ICT2588 to cause cardiovascular toxicity. Our findings reinforce the improved therapeutic index and tumorselective approach offered by ICT2588 and this nanotherapeutic approach.