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 38 for “"Antibody-drug conjugates (ADCs)"”.
-
TUMOR-TARGETED RELEASE OF IMMUNOSTIMULATORY AGENTS: SYNTHESIS AND BIOLOGICAL EVALUATION OF IMIDAZOQUINOLINE-BASED PRODRUGS AND ANTIBODY CONJUGATES
… the different delivery vehicles proposed, antibody drug conjugates (ADCs) have been especially successful in the clinic. Recently, the involvement of the immune system in cancer treatment has been exploited. Following this strategy, immune-stimulating antibody conjugates (ISACs) have …
-
Exploration of novel linker scaffolds enabling the simultaneous rebridging of disulfide bonds for the synthesis of antibody-drug conjugates
Antibody-drug conjugates (ADCs) are a class of targeted therapeutic, typically used for the treatment of cancers. By attaching drugs site-selectively to antibodies, off-target toxicity of the drug can be reduced, leading to significant benefits for the patient. In order to improve the homogeneity …
-
Epiregulin as a Novel Target for Antibody-Drug Conjugate Development for the Treatment of Colorectal Cancer
<p>Antibody-drug conjugates (ADCs) are a fast-growing class of molecularly targeted therapies with 13 currently approved and over a 100 in clinical trials. ADCs consist of a monoclonal antibody (mAb) conjugated to a potent cytotoxic payload to selectively target tumor antigens highly expressed on …
-
Design of Novel Antigen-Specific Immunotherapies for the Treatment of Autoimmune Disorders
… development of a new therapeutic class, antigen-drug conjugates (AgDCs). By reversing the paradigm of antibody-drug conjugates (ADCs), AgDCs exploit the directing effect of the autoantigen towards diseased cell populations, coupled with the immunomodulatory effects of a small molecule drug. …
-
CAR-T και Antibody–Drug Conjugates στη σύγχρονη ογκολογία: Φαρμακοεπαγρύπνηση, προφίλ ασφάλειας και προκλήσεις στην κλινική εφαρμογή και πρόσβαση
… θεραπείες, όπως οι κυτταρικές CAR-T και τα Antibody–Drug Conjugates, ADCs, που εμφανίζουν σημαντική ανταπόκριση τόσο στην αντιμετώπιση αιματολογικών κακοηθειών όσο και συμπαγών όγκων. Στην παρούσα εργασία, τονίζεται η σημαντικότητα των νέων ογκολογικών θεραπειών, αναλύοντας συγκεκριμένα …
-
ANTIBODY-DRUG CONJUGATES FOR THE TREATMENT OF BREAST CANCER.
… and trastuzumab emtansine (T-DM1) are anti-HER2 antibody-drug conjugates (ADCs) which have shown robust efficacy for treating breast cancer. For both ADCs, however, we lack effective biomarkers to predict outcomes from pre-treatment samples. Methods: To unveil predictive biomarkers for ADCs, we …
-
Azobenzenes for the development of therapeutics
… of azobenzenes for the development of antibody-drug conjugates (ADCs), a rapidly growing class of targeted cancer therapeutics. Previous reports have shown that ortho-methoxy azobenzenes undergo reductive cleavage in reducing environments, making them ideal candidates for the …
-
Development of a Novel Bioconjugation Platform for the Generation of Homogenous Antibody-Drug Conjugates
Antibody-drug conjugates (ADCs) are therapeutic entities which leverage the specificity of antibodies to selectively deliver potent cytotoxins to specific cell types, such as cancer cells. The pharmacology of an ADC is critically dependent on its stability, homogeneity, and drug-to-antibody ratio …
-
Development of stapled peptide targeted covalent inhibitors and synthesis of novel ADC payloads for applications in cancer therapy
… of hemiasterlin and its use as a payload in antibody–drug conjugates (ADCs). This thesis details the novel synthesis of hemiasterlin, an anti-mitotic marine natural product with low- to sub-nM potencies against several cancer cell lines. Rapid construction of hemiasterlin was achieved, …
-
Cysteine arylation
… fluorescent dyes, affinity and radio labels, drug molecules, and polymers and nanocomposites. These traditional reactions generate sulfur-sp³ carbon bonds between the cysteine thiol and the labeling reagents. The goal of this thesis is to develop new cysteine arylation reactions to generate …
-
CYCLIZATION-BASED SITE-SELECTIVE N-TERMINAL CYSTEINE CONJUGATION, PEPTIDE STAPLING AND HISTONE DEACETYLASE (HDAC) PROBING
… scaffolds for various purposes, including drug discovery. However, the application of cyclization reactions in the modifications of biomolecules in a single step is still limited. This dissertation reports a stereoselective thiomorpholine ring formation reaction to site-selectively modify …
-
The Development of a Tumour-Responsive Format for Antibody Conjugates
Antibody-drug conjugates (ADCs) are an emerging class of targeted therapeutics which exploit the selectivity of monoclonal antibodies towards particular membrane receptors, to deliver potent cytotoxins to a desired cell type. A significant amount of research has been undertaken to improve the …
-
Synthesis and biological evaluation of structurally diverse indole-based analogues as inhibitors of tubulin polymerization and synthesis of drug-linker constructs cleavable by enzymes present in the tumor microenvironment.
… OXi8006, and its water-soluble phosphate prodrug salt, OXi8007, which functioned as a promising VDA in mouse models of cancer. To expand our understanding of the relationship between structure and activity, we generated analogues that incorporated indole modifications and separately …
-
Design and synthesis of indole-based analogues of OXi8006 as inhibitors of tubulin polymerization and their incorporation as payloads in drug-linker constructs.
… In previous studies, OXi8007, the phosphate prodrug of OXi8006, demonstrated vascular disrupting activity within 2 hours of administration by targeting tumor vasculature. OXi8006 binds to the colchicine site on α,β-tubulin heterodimers, inducing a conformation shift from a straight to a curved …
-
Design and synthesis of benzosuberene and tetracyclic-based molecules inspired by natural products as inhibitors of tubulin polymerization and preparation of drug-linker constructs to facilitate tumor selective targeted delivery.
… improving selectivity of active compounds via prodrug and drug-linker strategies. A series of benzosuberene and tetracyclic analogues were designed and synthesized, structurally inspired by related molecules discovered and developed by the Pinney Laboratory as promising anti-cancer agents. These …
-
Αποτελεσματικότητα των συζευγμένων αντισωμάτων στον καρκίνο των ωοθηκών: Συστηματική ανασκόπηση και μετα-ανάλυση κλινικών δοκιμών φάσης II και III / Efficacy of antibody-drug conjugates in ovarian cancer: a systematic review and meta-analysis of phase ΙΙ and ΙΙΙ clinical trials
Εισαγωγή: Τα συζεύγματα αντισωμάτων (antibody–drug conjugates, ADCs) αποτελούν μια αναδυόμενη θεραπευτική προσέγγιση στον καρκίνο των ωοθηκών, συνδυάζοντας την ειδικότητα των μονοκλωνικών αντισωμάτων με την κυτταροτοξική δράση ισχυρών φαρμακευτικών παραγόντων. Οι υπάρχουσες μετα-αναλύσεις εστιάζουν …
-
The Development of Peroxide-Responsive Arylboronic Acids for Antibody-Drug Conjugates and Small-Molecule Prodrugs
… can be exploited for the targeted delivery of drugs. Section I of this thesis describes the design, synthesis, and evaluation of antibody-drug conjugates (ADCs) comprising arylboronic acid linkers, which give responsive drug release in the presence of the elevated hydrogen peroxide in cancer. …
-
The Development of Vinylheteroarene Linkers for Proteinogenic Cysteine Modification and Studies Towards Applying (+)-Discodermolide as a Novel Payload in Antibody-Drug Conjugates
… (+)-Discodermolide as a Novel Payload in Antibody-Drug Conjugates Hikaru Seki Antibody-drug conjugates (ADCs) are an emerging class of anticancer agents which combine the cell-targeting properties of a monoclonal antibody and the cytotoxicity of a small molecule drug. The antibody, …
-
Designed Bond Cleavage Reactions for Next-Generation Therapeutics
Creating ways for tissue-specific drug activation remains a significant challenge in modern medicine. Traditional approaches to drug delivery often lack precision, leading to unwanted side effects and reduced therapeutic efficacy. This PhD thesis explores two innovative approaches to overcome these …
-
Investigation and application of heterochiral proteins enabled by flow-based peptide synthesis
… In the second system, we examined heterochiral antibody-drug conjugates (ADCs) for the treatment of P. aeruginosa infection. New therapeutic modalities are needed to address bacterial resistance to conventional antibiotics. We developed a biologically expressed antibody that targets P. …
Page 1 of 2