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Synthesis of donor–acceptor–donor thiophene based ligands that can be utilized for optical assignment of pathological targets
Linköping University, Department of Physics, Chemistry and Biology, Chemistry. Linköping University, Faculty of Science & Engineering.
2022 (English)Doctoral thesis, comprehensive summary (Other academic)
Abstract [en]

Thiophene based ligands represent a class of molecular reporters proven superior in discerning pathological targets involved in neurodegenerative diseases, as well as bacterial infection. By fluorometric detection that depends on the milieu surrounding the ligand these biological processes can be studied with fluorescence spectroscopy and hyper-spectral confocal microscopy. The binding of a thiophene-based ligand to a biological target can entail specific fluorescent read-out through the conformation-sensitive ligand. Thus, the photo-physical properties of these molecules and the optical connection of binding make them valuable tools in the study of pathological events. As optical detection of pathological phenomena can be realized through several fluorescence parameters, including changes in fluorescent intensity, wavelength shifts, energy transfer, or emission lifetime, molecular studies of pathological targets in several biological systems have been realized by employing thiophene-based ligands. For instance, utilization of conjugated polydisperse and monodisperse thiophene-based molecules has in several studies demonstrated detection of disease associated protein aggregates in vitro, ex vivo and in vivo

My doctoral studies have included the synthesis and characterization of thiophene based donor-acceptor-donor (D–A–D) molecules and evaluation of how changes in side-chain positions, molecular length and number of negatively charged carboxylates impact interaction with biological targets. This thesis describes the utilization of the D–A–D molecules as fluorescent ligands for protein aggregates associated with Alzheimer’s disease and optical assignment of specific bacteria. The design and synthesis of these novel D–A–D thiophene-based fluorophores, with alterations in back bone, distribution of side chains and negatively charged groups, have generated novel insights regarding the ligands chemical structure on ligand performance, by the assessment of binding mode of the respective ligand to distinct pathological entities. Furthermore, the D–A–D molecules hold alternative photo-physical properties compared to thiophene-based ligand and these optical properties of the ligands have been employed to provide new insights in questions regarding protein aggregate polymorphism in Alzheimer’s disease. Overall, by organic synthesis we have fine-tuned the properties of thiophene-based D-A-D molecules and evaluated how modifications affect interactions with distinct biological, pathological targets and we foresee that D–A–D thiophene-based ligands will expand the toolbox for studying pathological targets in neurodegenerative diseases, as well as bacterial infection. 

Place, publisher, year, edition, pages
Linköping: Linköping University Electronic Press, 2022. , p. 56
Series
Linköping Studies in Science and Technology. Dissertations, ISSN 0345-7524 ; 2269
National Category
Organic Chemistry
Identifiers
URN: urn:nbn:se:liu:diva-190162ISBN: 978-91-7929-539-4 (print)ISBN: 978-91-7929-540-0 (electronic)OAI: oai:DiVA.org:liu-190162DiVA, id: diva2:1713287
Public defence
2022-12-12, Planck, Fysikhuset, Campus Valla, Linköping, 09:15
Opponent
Supervisors
Available from: 2022-11-24 Created: 2022-11-24 Last updated: 2022-11-24Bibliographically approved
List of papers
1. Synthesis and Characterization of Thiophene-based Donor-Acceptor-Donor Heptameric Ligands for Spectral Assignment of Polymorphic Amyloid-beta Deposits
Open this publication in new window or tab >>Synthesis and Characterization of Thiophene-based Donor-Acceptor-Donor Heptameric Ligands for Spectral Assignment of Polymorphic Amyloid-beta Deposits
2020 (English)In: Chemistry - A European Journal, ISSN 0947-6539, E-ISSN 1521-3765, Vol. 26, no 33, p. 7425-7432Article in journal (Refereed) Published
Abstract [en]

Protein deposits are associated with many devastating diseases and fluorescent ligands able to visualize these pathological entities are essential. Here, we report the synthesis of thiophene-based donor-acceptor-donor heptameric ligands that can be utilized for spectral assignment of distinct amyloid-beta (A beta) aggregates, one of the pathological hallmarks in Alzheimers disease. The ability of the ligands to selectively distinguish A beta deposits was abolished when the chemical composition of the ligands was altered. Our findings provide the structural and functional basis for the development of new fluorescent ligands that can distinguish between aggregated proteinaceous species consisting of the same peptide or protein. In addition, such ligands might aid in interpreting the potential role of polymorphic A beta deposits in the pathogenesis of Alzheimers disease.

Place, publisher, year, edition, pages
WILEY-V C H VERLAG GMBH, 2020
Keywords
Alzheimers disease; fluorescence; luminescent conjugated oligothiophenes; protein aggregates; beta-amyloid
National Category
Biochemistry Molecular Biology
Identifiers
urn:nbn:se:liu:diva-166174 (URN)10.1002/chem.201905612 (DOI)000532854400001 ()32022335 (PubMedID)
Note

Funding Agencies|Swedish Research CouncilSwedish Research Council [2016-00748]; Erling Persson foundation

Available from: 2020-06-09 Created: 2020-06-09 Last updated: 2025-02-20
2. Structural Properties Dictating Selective Optotracer Detection of Staphylococcus aureus
Open this publication in new window or tab >>Structural Properties Dictating Selective Optotracer Detection of Staphylococcus aureus
Show others...
2022 (English)In: ChemBioChem, ISSN 1439-4227, E-ISSN 1439-7633, Vol. 23, no 11, article id e202100684Article in journal (Refereed) Published
Abstract [en]

Optotracers are conformation-sensitive fluorescent tracer molecules that detect peptide- and carbohydrate-based biopolymers. Their binding to bacterial cell walls allows selective detection and visualisation of Staphylococcus aureus (S. aureus). Here, we investigated the structural properties providing optimal detection of S. aureus. We quantified spectral shifts and fluorescence intensity in mixes of bacteria and optotracers, using automatic peak analysis, cross-correlation, and area-under-curve analysis. We found that the length of the conjugated backbone and the number of charged groups, but not their distribution, are important factors for selective detection of S. aureus. The photophysical properties of optotracers were greatly improved by incorporating a donor-acceptor-donor (D-A-D)-type motif in the conjugated backbone. With significantly reduced background and binding-induced on-switch of fluorescence, these optotracers enabled real-time recordings of S. aureus growth. Collectively, this demonstrates that chemical structure and photophysics are key tunable characteristics in the development of optotracers for selective detection of bacterial species.

Place, publisher, year, edition, pages
Wiley-V C H Verlag GMBH, 2022
Keywords
bacterial detection; fluorescence microscopy; fluorescence spectroscopy; optotracers; real-time monitoring
National Category
Analytical Chemistry
Identifiers
urn:nbn:se:liu:diva-184429 (URN)10.1002/cbic.202100684 (DOI)000776536900001 ()35298076 (PubMedID)
Note

Funding Agencies|AIMES -Center for the Advancement of Integrated Medical and Engineering Sciences at Karolinska Institutet [1-249/2019]; KTH Royal Institute of Technology [VF-2019-0110]; Erling-Persson Family Foundation [4-1784/2016]; Swedish Research CouncilSwedish Research CouncilEuropean Commission [00748]; Swedish Foundation for Strategic ResearchSwedish Foundation for Strategic Research [SB12-00347]; Getinge AB [4-1599/2018]

Available from: 2022-04-21 Created: 2022-04-21 Last updated: 2024-07-04Bibliographically approved

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