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.
Results
Showing 1 to 20 of 157 for “"Prodrug"”.
-
The characterisation of a fenoprofen prodrug
The term "prodrug" refers to a pharmacologically inactive compound that is converted to an active drug by a metabolic biotransformation. A nonenzymatic process, such as hydrolysis, can activate a prodrug via several routes. Prodrugs are mostly used to improve a drug's physical and chemical …
-
Tetrazine-Triggered Bioorthogonal Decaging Reactions for Prodrug Activation
… been widely applied for the decaging of amine prodrugs. Although amines are common in small molecule drugs, decaging methods for other functional groups are required in order to develop a broadly applicable prodrug activation strategy that can be applied to a wider range of drugs and diseases. …
-
Catalytic antibodies for amide cleavage and prodrug activation
… for the simultaneous activation of multiple prodrugs. To this end, a protective group was designed which could be attached to any kind of cancer drug, in order to convert a cancer drug into a prodrug. The protective group relies on a [beta]-sulfone elimination process to release the active …
-
Transporter-Targeted Prodrug Delivery to Improve Oral Bioavailability of Saquinavir
… to investigate whether stereoisomerized peptide prodrugs targeting influx transporter system could improve intestinal absorption and oral bioavailability of SQV. Four stereoisomeric dipeptide prodrugs of SQV including L-valine-L-valine-SQV (LLS), L-valine-D-valine-SQV (LDS), D-valine-L-valine-SQV …
-
Development & testing of ultrasound enhanced prodrug microbubble drug delivery system
… of a novel microbubble formulation using a prodrug of Bexarotene to make the exterior layer of the microbubble. This started with development and engineering of productions schemes for stable microbubbles. Physical characterization was done to confirm production and was followed by initial …
-
EVASION OF EFFLUX AND ENHANCING BIOAVAILABILITY OF AMPRENAVIR BY PRODRUG DERIVATIZATION
… and brain bioavailability of Amprenavir (APV) by prodrug strategies targeting nutrient transporters to bypass P-glycoprotein (P-gp) mediated efflux. APV has low bioavailability and negligible brain absorption which is attributed by low aqueous solubility, efflux mediated by multidrug resistance …
-
Tumor-Specific STING Agonist Synthesis via a Two-Component Prodrug System
… efficacy. Herein, we explored an unconventional prodrug activation strategy for on-tumor synthesis of a potent agonist. Starting from the scaffold of MSA2, a non-CDN synthetic agonist that requires non-covalent dimerization via its benzo[b]thiophene core before binding to STING, we showed that …
-
A dendrimer-based prodrug for use in an anti-cancer nanocell
Cancer science is a heavily researched and rapidly changing field. Cutting edge research consistently reveals unique features of tumors that can be exploited for treatment. For example, it is well known that cells of varying tumor types have unique molecular markers and cell-surface receptors - …
-
T-cell-directed bioorthogonal catalysis for localised prodrug activation in cancer therapy
… enabled catalytic activation of anticancer prodrugs in vitro, resulting in enhanced antitumour efficacy in target cells. These findings demonstrate a proof-of-concept to a potential strategy for a versatile platform therapy that could addressed key limitations of current therapies to …
-
Development of an IL12 Prodrug to Treat Solid Tumors with Minimal Toxicity
… these problems, we developed a novel IL12 prodrug, pro-IL12, that is actively blocked until it is preferentially activated within the TME. We achieved this by using portions of the IL12 receptor attached with a flexible linker to sterically block the active site of IL12. The linker contains …
-
Prodrug Approach to Improve Oral and Brain Absorption of HIV Protease Inhibitor, Lopinavir
The main objective of this project is to develop prodrug strategies to circumvent efflux pumps such as P-glycoprotein (P-gp) and multidrug resistance associated proteins (MRPs), thereby enhancing oral and brain absorption of lopinavir (LPV). Oral absorption of LPV is severly limited due to low …
-
Synthesis and Characterization of Redox-Sensitive Polymer and Prodrug for Targeted Drug Delivery
… polymer, and DNS-SN38, thiol-sensitive SN-38 prodrug, as potential candidates for targeted drug delivery platforms. By covalently conjugating a redox-trigger (p-nitrobenzyl alcohol) and self-immolative linker (p-hydroxybenzyl alcohol) to the cyclization spacer (n-2-(hydroxyethyl)ethylene …
-
Evaluierung des Antibody Directed Enzyme Prodrug Therapy-Konzepts im Mammakarzinom- und Lymphom-Mausmodell
… neues Therapiekonzept Antibody Directed Enzyme Prodrug Therapy (ADEPT) in Tieren zu evaluieren. Damit sollte eine höhere Spezifität und Selektivität in der Behandlung von Tumoren erreicht werden. Dabei wurden ein orthotopes Mammakarzinom- mit MDA-MB-231-Tumorzellen in weiblichen SCID-Mäusen und …
-
Dual Delivery Systems Based On Polyamine Analog Benspm As Prodrug And Gene Delivery Vectors
… BENSpm free drug verified the success of this prodrug design. Biodegradability of Lipo-SS-BEN contributed to decreased toxicity compared with nondegradable control LipoBEN. However, decreased enhancement of TRAIL activity was observed for Lipo-SS-BEN when compared with BENSpm, indicating that …
-
Ring distortion of the alkaloid sinomenine and novel prodrug approaches to broad-spectrum antibiotics
… involves appendage of ionizable nitrogens on a prodrug moiety such that it crosses the outer membrane and is cleaved within Gram-negative bacteria, releasing the active antibiotic. Such novel strategy can be a powerful approach to combat disease-causing pathogens as it addresses the major …
-
Rational enzyme-directed prodrug development : exploiting tumour hypoxia to target the bioactivation of cytotoxic prodrugs
… the potential to target the activation of inert prodrugs by utilising tumour-specific catalytic enzymes to restrict cytotoxicity to neoplastic tissues. Appropriate expression of therapeutic enzymes can be achieved by exploiting the genetic distinctions that exist between tumour and normal tissues …
-
Synthetic Routes to Therapeutic Agents Via Masked Functionalities: From Orthogonal Peptide Crosslink to Photothermal Cancer Prodrug
… outlines the synthesis of a trimethyl lock-based prodrug model system, wherein photothermal activation of a salt containing a cationic near-IR dye and an anionic prodrug, releases a paclitaxel side-chain fragment via a tandem aryl Claisen rearrangement and lactonization. The prodrug model system …
Page 1 of 8