Chair of Medicinal and Bioinorganic Chemistry

2025

An organogold compound impairs Leishmania amazonensis amastigotes survival and delays lesion progression in murine cutaneous leishmaniasis: Mechanistic insights

Minori, K., Gadelha, F. R., Bonsignore, R., Alcántar, G. M., Fontes, J. V., Abbehausen, C., Brioschi, M. B. C., de Sousa, L. M., Consonni, S. R., Casini, A. & Miguel, D. C., Feb 2025, In: Biochemical Pharmacology. 232, 116716.

Research output: Contribution to journal › Article › peer-review

2024

(SiFA)SeFe: A Hydrophilic Silicon-Based Fluoride Acceptor Enabling Versatile Peptidic Radiohybrid Tracers

Deiser, S., Fenzl, S., König, V., Drexler, M., Smith, L. M., George, M. E., Beck, R., Witney, T. H., Inoue, S. & Casini, A., 22 Aug 2024, In: Journal of Medicinal Chemistry. 67, 16, p. 14077-14094 18 p.

Research output: Contribution to journal › Article › peer-review

Open Access

A Golden Touch in the Design of Multifunctional Porphyrin Metallacages: Host-Guest Chemistry for Drug-Target Interactions

Rodríguez-Prieto, T., Wragg, D., Heiduk, N., Park, M., Strittmatter, N., Fischer, R. A., Casini, A. & Moreno-Alcántar, G., 1 Jul 2024, In: CCS Chemistry. 6, 7, p. 1662-1671 10 p.

Research output: Contribution to journal › Article › peer-review

Open Access

1 Scopus citations

A graft-to strategy of poly(vinylphosphonates) on dopazide-coated gold nanoparticles using in situ catalyst activation

Weingarten, P., Thomas, S. R., Luiza de Andrade Querino, A., Halama, K., Kränzlein, M., Casini, A. & Rieger, B., 8 Mar 2024, In: RSC Advances. 14, 12, p. 8145-8149 5 p.

Research output: Contribution to journal › Article › peer-review

Open Access

3 Scopus citations

Blockage of aquaporin-3 peroxiporin activity by organogold compounds affects melanoma cell adhesion, proliferation and migration

da Silva, I. V., Pimpão, C., Paccetti-Alves, I., Thomas, S. R., Barateiro, A., Casini, A. & Soveral, G., 1 Jul 2024, In: Journal of Physiology. 602, 13, p. 3111-3129 19 p.

Research output: Contribution to journal › Article › peer-review

Open Access

4 Scopus citations

Gold-templated covalent targeting of the CysSec-dyad of thioredoxin reductase 1 in cancer cells

Skos, L., Schmidt, C., Thomas, S. R., Park, M., Geiger, V., Wenisch, D., Bonsignore, R., Del Favero, G., Mohr, T., Bileck, A., Gerner, C., Casini, A. & Meier-Menches, S. M., 17 Jul 2024, In: Cell Reports Physical Science. 5, 7, 102072.

Research output: Contribution to journal › Article › peer-review

Open Access

1 Scopus citations

Introducing Metal–Organic Frameworks to Melt Electrowriting: Multifunctional Scaffolds with Controlled Microarchitecture for Tissue Engineering Applications

Mansi, S., Dummert, S. V., Topping, G. J., Hussain, M. Z., Rickert, C., Mueller, K. M. A., Kratky, T., Elsner, M., Casini, A., Schilling, F., Fischer, R. A., Lieleg, O. & Mela, P., 9 Jan 2024, In: Advanced Functional Materials. 34, 2, 2304907.

Research output: Contribution to journal › Article › peer-review

Open Access

12 Scopus citations

Liposomal Formulation of an Organogold Complex Enhancing Its Activity as Antimelanoma Agent—In Vitro and In Vivo Studies

Pinho, J. O., Coelho, M., Pimpão, C., Konwar, J., Godinho-Santos, A., Noiva, R. M., Thomas, S. R., Casini, A., Soveral, G. & Gaspar, M. M., Dec 2024, In: Pharmaceutics. 16, 12, 1566.

Research output: Contribution to journal › Article › peer-review

Open Access

Micellar Transfer Hydrogenation Catalysis in Water with Monocarbonyl Ruthenium(II)-poly(vinylphosphonate)-Containing Polymers: Achieving Reduction of Biomass-Derived Aldehydes

Lovison, D., Weingarten, P., Sebeschuk, A., Rieger, B. & Casini, A., 22 Nov 2024, In: ACS Applied Polymer Materials. 6, 22, p. 13855-13864 10 p.

Research output: Contribution to journal › Article › peer-review

Open Access

Potent Anticancer Activity of a Dinuclear Gold(I) bis-N-Heterocyclic Imine Complex Related to Thioredoxin Reductase Inhibition in Vitro

Park, M., Schmidt, C., Türck, S., Hanusch, F., Hirmer, S. V., Ott, I., Casini, A. & Inoue, S., Apr 2024, In: ChemPlusChem. 89, 4, e202300557.

Research output: Contribution to journal › Article › peer-review

Open Access

4 Scopus citations

Preclinical evaluation of ²²⁵Ac-labeled minigastrin analog DOTA-CCK-66 for Targeted Alpha Therapy

Holzleitner, N., Vilangattil, M., Swaidan, A., Garcia-Prada, C. D., Taddio, M. F., Jeanjean, P., Mona, C. E., Lapa, C., Casini, A., Günther, T. & Carlucci, G., 2024, (Accepted/In press) In: European Journal of Nuclear Medicine and Molecular Imaging.

Research output: Contribution to journal › Article › peer-review

Open Access

Preclinical Evaluation of Gastrin-Releasing Peptide Receptor Antagonists Labeled with ¹⁶¹Tb and ¹⁷⁷Lu: A Comparative Study

Holzleitner, N., Cwojdzinski, T., Beck, R., Urtz-Urban, N., Hillhouse, C. C., Grundler, P. V., van der Meulen, N. P., Talip, Z., Ramaekers, S., Van de Voorde, M., Ponsard, B., Casini, A. & Günther, T., 2024, In: Journal of Nuclear Medicine. 65, 3, p. 481-484 4 p.

Research output: Contribution to journal › Article › peer-review

2 Scopus citations

2023

Application of Machine Learning Algorithms to Metadynamics for the Elucidation of the Binding Modes and Free Energy Landscape of Drug/Target Interactions: a Case Study

Siddiqui, G. A., Stebani, J. A., Wragg, D., Koutsourelakis, P. S., Casini, A. & Gagliardi, A., 8 Nov 2023, In: Chemistry - A European Journal. 29, 62, e202302375.

Research output: Contribution to journal › Article › peer-review

Open Access

3 Scopus citations

Beyond Metal-Arenes: Monocarbonyl Ruthenium(II) Catalysts for Transfer Hydrogenation Reactions in Water and in Cells

Lovison, D., Berghausen, T., Thomas, S. R., Robson, J., Drees, M., Jandl, C., Pöthig, A., Mollik, P., Halter, D. P., Baratta, W. & Casini, A., 18 Aug 2023, In: ACS Catalysis. 13, 16, p. 10798-10823 26 p.

Research output: Contribution to journal › Article › peer-review

9 Scopus citations

Bioinorganic supramolecular coordination complexes and their biomedical applications

Moreno-Alcántar, G. & Casini, A., Jan 2023, In: FEBS Letters. 597, 1, p. 191-202 12 p.

Research output: Contribution to journal › Article › peer-review

Open Access

26 Scopus citations

Electrochemical Detection of Drugs via a Supramolecular Cucurbit[7]uril-Based Indicator Displacement Assay

Kumar, N. M., Gruhs, P., Casini, A., Biedermann, F., Moreno-Alcántar, G. & Picchetti, P., 28 Jul 2023, In: ACS Sensors. 8, 7, p. 2525-2532 8 p.

Research output: Contribution to journal › Article › peer-review

Open Access

9 Scopus citations

Elucidating the Multimodal Anticancer Mechanism of an Organometallic Terpyridine Platinum(II) N-Heterocyclic Carbene Complex against Triple-Negative Breast Cancer In Vitro and In Vivo

Zhang, J. J., Xu, Q. J., Schmidt, C., Maaty, M. A. A. E., Song, J., Yu, C., Zhou, J., Han, K., Sun, H., Casini, A., Ott, I. & Wölfl, S., 23 Mar 2023, In: Journal of Medicinal Chemistry. 66, 6, p. 3995-4008 14 p.

Research output: Contribution to journal › Article › peer-review

16 Scopus citations

Exploring the Anticancer Activity of Tamoxifen-Based Metal Complexes Targeting Mitochondria

Scalcon, V., Bonsignore, R., Aupič, J., Thomas, S. R., Folda, A., Heidecker, A. A., Pöthig, A., Magistrato, A., Casini, A. & Rigobello, M. P., 27 Jul 2023, In: Journal of Medicinal Chemistry. 66, 14, p. 9823-9841 19 p.

Research output: Contribution to journal › Article › peer-review

Open Access

14 Scopus citations

Organogold(III)-dithiocarbamate compounds and their coordination analogues as anti-tumor and anti-leishmanial metallodrugs

de Andrade Querino, A. L., de Sousa, A. M., Thomas, S. R., de Lima, G. M., Dittz, D., Casini, A., do Monte-Neto, R. L. & Silva, H., Oct 2023, In: Journal of Inorganic Biochemistry. 247, 112346.

Research output: Contribution to journal › Article › peer-review

4 Scopus citations

Organometallic Pillarplexes That Bind DNA 4-Way Holliday Junctions and Forks

Craig, J. S., Melidis, L., Williams, H. D., Dettmer, S. J., Heidecker, A. A., Altmann, P. J., Guan, S., Campbell, C., Browning, D. F., Sigel, R. K. O., Johannsen, S., Egan, R. T., Aikman, B., Casini, A., Pöthig, A. & Hannon, M. J., 28 Jun 2023, In: Journal of the American Chemical Society. 145, 25, p. 13570-13580 11 p.

Research output: Contribution to journal › Article › peer-review

Open Access

9 Scopus citations

PET Imaging of Self-Assembled ¹⁸F-Labelled Pd₂L₄ Metallacages for Anticancer Drug Delivery

Cosialls, R., Simó, C., Borrós, S., Gómez-Vallejo, V., Schmidt, C., Llop, J., Cuenca, A. B. & Casini, A., 12 Jan 2023, In: Chemistry - A European Journal. 29, 3, e202202604.

Research output: Contribution to journal › Article › peer-review

Open Access

17 Scopus citations

Synthesis of ¹⁷⁷Lu-Labeled, Somatostatin-2 Receptor-Targeted Metalla-Assemblies: Challenges in the Design of Supramolecular Radiotherapeutics

Deiser, S., Drexler, M., Moreno-Alcántar, G., Irl, M., Schmidt, C., Günther, T. & Casini, A., 18 Dec 2023, In: Inorganic Chemistry. 62, 50, p. 20710-20720 11 p.

Research output: Contribution to journal › Article › peer-review

6 Scopus citations

2022

Bottom-up Synthesis of Water-Soluble Gold Nanoparticles Stabilized by N-Heterocyclic Carbenes: From Structural Characterization to Applications

Thomas, S. R., Yang, W., Morgan, D. J., Davies, T. E., Li, J. J., Fischer, R. A., Huang, J., Dimitratos, N. & Casini, A., 7 Oct 2022, In: Chemistry - A European Journal. 28, 56, e202201575.

Research output: Contribution to journal › Article › peer-review

Open Access

17 Scopus citations

Competitive profiling of ligandable cysteines in Staphylococcus aureus with an organogold compound

Schmidt, C., Zollo, M., Bonsignore, R., Casini, A. & Hacker, S. M., 7 Apr 2022, In: Chemical Communications. 58, 36, p. 5526-5529 4 p.

Research output: Contribution to journal › Article › peer-review

Open Access

15 Scopus citations

"dynamical Docking" of Cyclic Dinuclear Au(I) Bis-N-heterocyclic Complexes Facilitates Their Binding to G-Quadruplexes

Kaußler, C., Wragg, D., Schmidt, C., Moreno-Alcántar, G., Jandl, C., Stephan, J., Fischer, R. A., Leoni, S., Casini, A. & Bonsignore, R., 19 Dec 2022, In: Inorganic Chemistry. 61, 50, p. 20405-20423 19 p.

Research output: Contribution to journal › Article › peer-review

Open Access

6 Scopus citations

Highly-fluorescent BODIPY-functionalised metallacages as drug delivery systems: synthesis, characterisation and cellular accumulation studies

Aikman, B., Bonsignore, R., Woods, B., Doellerer, D., Scotti, R., Schmidt, C., Heidecker, A. A., Pöthig, A., Sayers, E. J., Jones, A. T. & Casini, A., 2022, (Accepted/In press) In: Dalton Transactions.

Research output: Contribution to journal › Article › peer-review

Open Access

10 Scopus citations

Indenyl and Allyl Palladate Complexes Bearing N-Heterocyclic Carbene Ligands: an Easily Accessible Class of New Anticancer Drug Candidates

Scattolin, T., Pessotto, I., Cavarzerani, E., Canzonieri, V., Orian, L., Demitri, N., Schmidt, C., Casini, A., Bortolamiol, E., Visentin, F., Rizzolio, F. & Nolan, S. P., 8 Jun 2022, In: European Journal of Inorganic Chemistry. 2022, 16, e202200103.

Research output: Contribution to journal › Article › peer-review

Open Access

28 Scopus citations

Optimization of the Pharmacokinetic Profile of [^99mTc]Tc-N₄-Bombesin Derivatives by Modification of the Pharmacophoric Gln-Trp Sequence

Günther, T., Konrad, M., Stopper, L., Kunert, J. P., Fischer, S., Beck, R., Casini, A. & Wester, H. J., Sep 2022, In: Pharmaceuticals. 15, 9, 1133.

Research output: Contribution to journal › Article › peer-review

Open Access

5 Scopus citations

2021

An Organogold Compound as Potential Antimicrobial Agent against Drug-Resistant Bacteria: Initial Mechanistic Insights

Chakraborty, P., Oosterhuis, D., Bonsignore, R., Casini, A., Olinga, P. & Scheffers, D. J., 6 Oct 2021, In: ChemMedChem. 16, 19, p. 3060-3070 11 p.

Research output: Contribution to journal › Article › peer-review

Open Access

27 Scopus citations

Aquaporin-3 is involved in NLRP3-inflammasome activation contributing to the setting of inflammatory response

da Silva, I. V., Cardoso, C., Martínez-Banaclocha, H., Casini, A., Pelegrín, P. & Soveral, G., Mar 2021, In: Cellular and Molecular Life Sciences. 78, 6, p. 3073-3085 13 p.

Research output: Contribution to journal › Article › peer-review

Open Access

42 Scopus citations

Bioconjugate Supramolecular Pd²⁺Metallacages Penetrate the Blood Brain Barrier in Vitro and in Vivo

Woods, B., Silva, R. D. M., Schmidt, C., Wragg, D., Cavaco, M., Neves, V., Ferreira, V. F. C., Gano, L., Morais, T. S., Mendes, F., Correia, J. D. G. & Casini, A., 21 Jul 2021, In: Bioconjugate Chemistry. 32, 7, p. 1399-1408 10 p.

Research output: Contribution to journal › Article › peer-review

41 Scopus citations

C−C Cross-Couplings from a Cyclometalated Au(III) C∧ N Complex: Mechanistic Insights and Synthetic Developments

Bonsignore, R., Thomas, S. R., Rigoulet, M., Jandl, C., Pöthig, A., Bourissou, D., Barone, G. & Casini, A., 13 Oct 2021, In: Chemistry - A European Journal. 27, 57, p. 14322-14334 13 p.

Research output: Contribution to journal › Article › peer-review

Open Access

7 Scopus citations

Host–Guest Interactions in a Metal–Organic Framework Isoreticular Series for Molecular Photocatalytic CO₂ Reduction

Stanley, P. M., Haimerl, J., Thomas, C., Urstoeger, A., Schuster, M., Shustova, N. B., Casini, A., Rieger, B., Warnan, J. & Fischer, R. A., 9 Aug 2021, In: Angewandte Chemie International Edition in English. 60, 33, p. 17854-17860 7 p.

Research output: Contribution to journal › Article › peer-review

Open Access

78 Scopus citations

Identifying and validating the presence of guanine-quadruplexes (G4) within the blood fluke parasite schistosoma mansoni

Craven, H. M., Bonsignore, R., Lenis, V., Santi, N., Berrar, D., Swain, M., Whiteland, H., Casini, A. & Hoffmann, K. F., Feb 2021, In: PLoS Neglected Tropical Diseases. 15, 2, p. 1-24 24 p., e0008770.

Research output: Contribution to journal › Article › peer-review

Open Access

6 Scopus citations

Interfering with Metabolic Profile of Triple-Negative Breast Cancers Using Rationally Designed Metformin Prodrugs

Babak, M. V., Chong, K. R., Rapta, P., Zannikou, M., Tang, H. M., Reichert, L., Chang, M. R., Kushnarev, V., Heffeter, P., Meier-Menches, S. M., Lim, Z. C., Yap, J. Y., Casini, A., Balyasnikova, I. V. & Ang, W. H., 7 Jun 2021, In: Angewandte Chemie International Edition in English. 60, 24, p. 13405-13413 9 p.

Research output: Contribution to journal › Article › peer-review

48 Scopus citations

Investigation of solvatomorphism and its photophysical implications for archetypal trinuclear Au₃(1-methylimidazolate)₃

Guan, S., Mayer, D. C., Jandl, C., Weishäupl, S. J., Casini, A. & Pöthig, A., 1 Aug 2021, In: Molecules. 26, 15, 4404.

Research output: Contribution to journal › Article › peer-review

Open Access

Mechanisms of irreversible aquaporin-10 inhibition by organogold compounds studied by combined biophysical methods and atomistic simulations

Pimpão, C., Wragg, D., Bonsignore, R., Aikman, B., Pedersen, P. A., Leoni, S., Soveral, G. & Casini, A., 1 Sep 2021, In: Metallomics. 13, 9, mfab053.

Research output: Contribution to journal › Article › peer-review

Open Access

5 Scopus citations

Therapeutic potential of a copper complex loaded in pH-sensitive long circulating liposomes for colon cancer management

Pinho, J. O., da Silva, I. V., Amaral, J. D., Rodrigues, C. M. P., Casini, A., Soveral, G. & Gaspar, M. M., 15 Apr 2021, In: International Journal of Pharmaceutics. 599, 120463.

Research output: Contribution to journal › Article › peer-review

39 Scopus citations

2020

An Organometallic Gold(I) Bis-N-Heterocyclic Carbene Complex with Multimodal Activity in Ovarian Cancer Cells

Meier-Menches, S. M., Neuditschko, B., Zappe, K., Schaier, M., Gerner, M. C., Schmetterer, K. G., Del Favero, G., Bonsignore, R., Cichna-Markl, M., Koellensperger, G., Casini, A. & Gerner, C., 1 Dec 2020, In: Chemistry - A European Journal. 26, 67, p. 15528-15537 10 p.

Research output: Contribution to journal › Article › peer-review

Open Access

46 Scopus citations

Aquaporin-driven hydrogen peroxide transport: A case of molecular mimicry?

Wragg, D., Leoni, S. & Casini, A., 2020, In: RSC Chemical Biology. 1, 5, p. 390-394 5 p.

Research output: Contribution to journal › Article › peer-review

Open Access

24 Scopus citations

Carbon–Phosphorus Coupling from C^N Cyclometalated Au^III Complexes

Bonsignore, R., Thomas, S. R., Klooster, W. T., Coles, S. J., Jenkins, R. L., Bourissou, D., Barone, G. & Casini, A., 1 Apr 2020, In: Chemistry - A European Journal. 26, 19, p. 4226-4231 6 p.

Research output: Contribution to journal › Article › peer-review

Open Access

21 Scopus citations

Comparative biological evaluation and G-quadruplex interaction studies of two new families of organometallic gold(I) complexes featuring N-heterocyclic carbene and alkynyl ligands

Meier-Menches, S. M., Aikman, B., Döllerer, D., Klooster, W. T., Coles, S. J., Santi, N., Luk, L., Casini, A. & Bonsignore, R., Jan 2020, In: Journal of Inorganic Biochemistry. 202, 110844.

Research output: Contribution to journal › Article › peer-review

Open Access

44 Scopus citations

Comparing the Antileishmanial Activity of Gold(I) and Gold(III) Compounds in L. amazonensis and L. braziliensis in Vitro

Minori, K., Rosa, L. B., Bonsignore, R., Casini, A. & Miguel, D. C., 18 Nov 2020, In: ChemMedChem. 15, 22, p. 2146-2150 5 p.

Research output: Contribution to journal › Article › peer-review

Open Access

27 Scopus citations

Design Strategies and Medicinal Applications of Metal-Peptidic Bioconjugates

Meier-Menches, S. M. & Casini, A., 20 May 2020, In: Bioconjugate Chemistry. 31, 5, p. 1279-1288 10 p.

Research output: Contribution to journal › Article › peer-review

45 Scopus citations

Exploring the Chemoselectivity towards Cysteine Arylation by Cyclometallated Au^III Compounds: New Mechanistic Insights

Thomas, S. R., Bonsignore, R., Sánchez Escudero, J., Meier-Menches, S. M., Brown, C. M., Wolf, M. O., Barone, G., Luk, L. Y. P. & Casini, A., 2 Nov 2020, In: ChemBioChem. 21, 21, p. 3071-3076 6 p.

Research output: Contribution to journal › Article › peer-review

Open Access

28 Scopus citations

Exploring the Reactivity and Biological Effects of Heteroleptic N-Heterocyclic Carbene Gold(I)-Alkynyl Complexes

Oberkofler, J., Aikman, B., Bonsignore, R., Pöthig, A., Platts, J., Casini, A. & Kühn, F. E., 27 Mar 2020, In: European Journal of Inorganic Chemistry. 2020, 11-12, p. 1040-1051 12 p.

Research output: Contribution to journal › Article › peer-review

Open Access

32 Scopus citations

Glutathione-responsive cyclodextrin-nanosponges as drug delivery systems for doxorubicin: Evaluation of toxicity and transport mechanisms in the liver

Daga, M., de Graaf, I. A. M., Argenziano, M., Barranco, A. S. M., Loeck, M., Al-Adwi, Y., Cucci, M. A., Caldera, F., Trotta, F., Barrera, G., Casini, A., Cavalli, R. & Pizzimenti, S., Jun 2020, In: Toxicology in Vitro. 65, 104800.

Research output: Contribution to journal › Article › peer-review

Open Access

39 Scopus citations

Human red blood cell uptake and sequestration of arsenite and selenite: Evidence of seleno-bis(S-glutathionyl) arsinium ion formation in human cells

Kaur, G., Javed, W., Ponomarenko, O., Shekh, K., Swanlund, D. P., Zhou, J. R., Summers, K. L., Casini, A., Wenzel, M. N., Casey, J. R., Cordat, E., Pickering, I. J., George, G. N. & Leslie, E. M., Oct 2020, In: Biochemical Pharmacology. 180, 114141.

Research output: Contribution to journal › Article › peer-review

Open Access

8 Scopus citations

Insights into the selectivity mechanisms of grapevine NIP aquaporins

Sabir, F., Di Pizio, A., Loureiro-Dias, M. C., Casini, A., Soveral, G. & Prista, C., 2 Sep 2020, In: International Journal of Molecular Sciences. 21, 18, p. 1-14 14 p., 6697.

Research output: Contribution to journal › Article › peer-review

Open Access

10 Scopus citations

Targeted imaging of integrins in cancer tissues using photocleavable Ru(ii) polypyridine complexes as mass-tags

Han, J., Sun, J., Song, S., Beljaars, L., Groothuis, G. M. M., Permentier, H., Bischoff, R., Halmos, G. B., Verhoeven, C. J., Amstalden van Hove, E. R., Horvatovich, P. & Casini, A., 4 Jun 2020, In: Chemical Communications. 56, 44, p. 5941-5944 4 p.

Research output: Contribution to journal › Article › peer-review

Open Access

12 Scopus citations

Chair of Medicinal and Bioinorganic Chemistry

Research output

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