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Adamantane-Monoterpenoid Conjugates Linked via Heterocyclic Linkers Enhance the Cytotoxic Effect of Topotecan. (2022)
Journal Article
Reynisson. (2022). Adamantane-Monoterpenoid Conjugates Linked via Heterocyclic Linkers Enhance the Cytotoxic Effect of Topotecan. Molecules, https://doi.org/10.3390/molecules27113374

Inhibiting tyrosyl-DNA phosphodiesterase 1 (TDP1) is a promising strategy for increasing the effectiveness of existing antitumor therapy since it can remove the DNA lesions caused by anticancer drugs, which form covalent complexes with topoisomerase... Read More about Adamantane-Monoterpenoid Conjugates Linked via Heterocyclic Linkers Enhance the Cytotoxic Effect of Topotecan..

Highly Antiproliferative Latonduine and Indolo[2,3-c]quinoline Derivatives: Complex Formation with Copper(II) Markedly Changes the Kinase Inhibitory Profile. (2022)
Journal Article
Reynisson. (2022). Highly Antiproliferative Latonduine and Indolo[2,3-c]quinoline Derivatives: Complex Formation with Copper(II) Markedly Changes the Kinase Inhibitory Profile. Journal of Medicinal Chemistry, 2238 - 2261. https://doi.org/10.1021/acs.jmedchem.1c01740

A series of latonduine and indoloquinoline derivatives HL1-HL8 and their copper(II) complexes (1-8) were synthesized and comprehensively characterized. The structures of five compounds (HL6, [CuCl(L1)(DMF)]·DMF, [CuCl(L2)(CH3OH)], [CuCl(L3)]·0.5H2O,... Read More about Highly Antiproliferative Latonduine and Indolo[2,3-c]quinoline Derivatives: Complex Formation with Copper(II) Markedly Changes the Kinase Inhibitory Profile..

Conjugation of Palbociclib with MHI-148 Has an Increased Cytotoxic Effect for Breast Cancer Cells and an Altered Mechanism of Action. (2022)
Journal Article
Reynisson. (2022). Conjugation of Palbociclib with MHI-148 Has an Increased Cytotoxic Effect for Breast Cancer Cells and an Altered Mechanism of Action. Molecules, 1-14. https://doi.org/10.3390/molecules27030880

The CDK4/6 inhibitor palbociclib, combined with endocrine therapy, has been shown to be effective in postmenopausal women with estrogen receptor-positive, HER2-negative advanced or metastatic breast cancer. However, palbociclib is not as effective in... Read More about Conjugation of Palbociclib with MHI-148 Has an Increased Cytotoxic Effect for Breast Cancer Cells and an Altered Mechanism of Action..

Discovery and Characterization of a Cryptic Secondary Binding Site in the Molecular Chaperone HSP70. (2022)
Journal Article
Reynisson. (2022). Discovery and Characterization of a Cryptic Secondary Binding Site in the Molecular Chaperone HSP70. Molecules, https://doi.org/10.3390/molecules27030817

Heat Shock Protein 70s (HSP70s) are key molecular chaperones that are overexpressed in many cancers and often associated with metastasis and poor prognosis. It has proven difficult to develop ATP-competitive, drug-like small molecule inhibitors of HS... Read More about Discovery and Characterization of a Cryptic Secondary Binding Site in the Molecular Chaperone HSP70..

New Deoxycholic Acid Derived Tyrosyl-DNA Phosphodiesterase 1 Inhibitors Also Inhibit Tyrosyl-DNA Phosphodiesterase 2. (2021)
Journal Article
Reynisson. (2021). New Deoxycholic Acid Derived Tyrosyl-DNA Phosphodiesterase 1 Inhibitors Also Inhibit Tyrosyl-DNA Phosphodiesterase 2. Molecules, https://doi.org/10.3390/molecules27010072

A series of deoxycholic acid (DCA) amides containing benzyl ether groups on the steroid core were tested against the tyrosyl-DNA phosphodiesterase 1 (TDP1) and 2 (TDP2) enzymes. In addition, 1,2,4- and 1,3,4-oxadiazole derivatives were synthesized to... Read More about New Deoxycholic Acid Derived Tyrosyl-DNA Phosphodiesterase 1 Inhibitors Also Inhibit Tyrosyl-DNA Phosphodiesterase 2..

Impact of the ferrocenyl group on cytotoxicity and KSP inhibitory activity of ferrocenyl monastrol conjugates (2021)
Journal Article
Reynisson, J., Wieczorek-Błauż, A., Kowalczyk, K., Błauż, A., Makal, A., Pawlędzio, S., Eurtivong, C., Arabshahi, H. J., Hartinger, C. G., Rychlik, B., & Plażuk, D. (2021). Impact of the ferrocenyl group on cytotoxicity and KSP inhibitory activity of ferrocenyl monastrol conjugates. Dalton Transactions, 51(2), 491-508. https://doi.org/10.1039/d1dt03553c

The incorporation of the ferrocenyl moiety into a bioactive molecule may significantly alter the activity of the resulting conjugate. By applying this strategy, we designed ferrocenyl analogs of monastrol - the first low molecular weight kinesin spin... Read More about Impact of the ferrocenyl group on cytotoxicity and KSP inhibitory activity of ferrocenyl monastrol conjugates.

Identification of novel Atg3-Atg8 inhibitors using virtual screening for autophagy modulation (2021)
Journal Article
Leung, E., Ayine-Tora, D. M., Santos-Ledo, A., Korolchuk, V. I., & Reynisson, J. (2021). Identification of novel Atg3-Atg8 inhibitors using virtual screening for autophagy modulation. Bioorganic Chemistry, 114, 105092. https://doi.org/10.1016/j.bioorg.2021.105092

A collection of 9050 natural products, their derivatives, and mimetics, was virtually screened against the human Atg3-Atg8 (Atg - autophagy) binding scaffold. By blocking this interaction, the lipidation of Atg8 does not occur and the formation of au... Read More about Identification of novel Atg3-Atg8 inhibitors using virtual screening for autophagy modulation.

Development of 2-Morpholino-N-hydroxybenzamides as anti-proliferative PC-PLC inhibitors (2021)
Journal Article
Rees, S. W., Leung, E., Reynisson, J., Barker, D., & Pilkington, L. I. (2021). Development of 2-Morpholino-N-hydroxybenzamides as anti-proliferative PC-PLC inhibitors. Bioorganic Chemistry, 114, 105152. https://doi.org/10.1016/j.bioorg.2021.105152

Phosphatidylcholine-specific phospholipase C (PC-PLC) is a key enzyme involved in the metabolism of the mammalian phospholipid phosphatidylcholine into secondary messengers diacylglycerol (DAG) and phosphocholine. DAG and phosphocholine have been ide... Read More about Development of 2-Morpholino-N-hydroxybenzamides as anti-proliferative PC-PLC inhibitors.

New Hybrid Compounds Combining Fragments of Usnic Acid and Monoterpenoids for Effective Tyrosyl-DNA Phosphodiesterase 1 Inhibition. (2021)
Journal Article
Reynisson. (2021). New Hybrid Compounds Combining Fragments of Usnic Acid and Monoterpenoids for Effective Tyrosyl-DNA Phosphodiesterase 1 Inhibition. Biomolecules, https://doi.org/10.3390/biom11070973

Usnic acid (UA) is a secondary metabolite of lichens that exhibits a wide range of biological activities. Previously, we found that UA derivatives are effective inhibitors of tyrosyl-DNA phosphodiesterase 1 (TDP1). It can remove covalent complex DNA-... Read More about New Hybrid Compounds Combining Fragments of Usnic Acid and Monoterpenoids for Effective Tyrosyl-DNA Phosphodiesterase 1 Inhibition..

Validating TDP1 as an Inhibition Target for the Development of Chemosensitizers for Camptothecin-Based Chemotherapy Drugs. (2021)
Journal Article
Reynisson, J. (2021). Validating TDP1 as an Inhibition Target for the Development of Chemosensitizers for Camptothecin-Based Chemotherapy Drugs. Oncology and Therapy,

Cancer chemotherapy sensitizers hold the key to maximizing the potential of standard anticancer treatments. We have a long-standing interest in developing and validating inhibitors of the DNA repair enzyme tyrosyl-DNA phosphodiesterase 1 (TDP1) as ch... Read More about Validating TDP1 as an Inhibition Target for the Development of Chemosensitizers for Camptothecin-Based Chemotherapy Drugs..

Thieno[2,3-b]Pyridine Derivative Targets Epithelial, Mesenchymal and Hybrid CD15s+ Breast Cancer Cells. (2021)
Journal Article
Reynisson. (2021). Thieno[2,3-b]Pyridine Derivative Targets Epithelial, Mesenchymal and Hybrid CD15s+ Breast Cancer Cells. Medicines, https://doi.org/10.3390/medicines8070032

The adhesion of cancer cells to vascular endothelium is a critical process in hematogenous metastasis and might be similar to the recruitment of leukocytes at the site of inflammation. It is mediated by E-selectin and its ligands, of which the most s... Read More about Thieno[2,3-b]Pyridine Derivative Targets Epithelial, Mesenchymal and Hybrid CD15s+ Breast Cancer Cells..

Novel Tdp1 Inhibitors Based on Adamantane Connected with Monoterpene Moieties via Heterocyclic Fragments. (2021)
Journal Article
Reynisson. (2021). Novel Tdp1 Inhibitors Based on Adamantane Connected with Monoterpene Moieties via Heterocyclic Fragments. Molecules, 1-23. https://doi.org/10.3390/molecules26113128

Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is a promising target for anticancer therapy due to its ability to counter the effects topoisomerase 1 (Top1) poison, such as topotecan, thus, decreasing their efficacy. Compounds containing adamantane and monot... Read More about Novel Tdp1 Inhibitors Based on Adamantane Connected with Monoterpene Moieties via Heterocyclic Fragments..

Improving the solubility of anti-proliferative thieno[2,3-b]quinoline-2-carboxamides. (2021)
Journal Article
Reynisson. (2021). Improving the solubility of anti-proliferative thieno[2,3-b]quinoline-2-carboxamides. Bioorganic and Medicinal Chemistry, 1- 10. https://doi.org/10.1016/j.bmc.2021.116092

Thieno[2,3-b]pyridines are a class of compounds known for their potent anti-proliferative activities against a range of human cancer cell lines. In this research, a number of strategies to generate analogues that have improved aqueous solubility whil... Read More about Improving the solubility of anti-proliferative thieno[2,3-b]quinoline-2-carboxamides..

Author Correction: Glycosphingolipid expression at breast cancer stem cells after novel thieno[2,3-b]pyridine anticancer compound treatment (2021)
Journal Article
Marijan, S., Markotić, A., Mastelić, A., Režić-Mužinić, N., Pilkington, L. I., Reynisson, J., & Čulić, V. Č. (in press). Author Correction: Glycosphingolipid expression at breast cancer stem cells after novel thieno[2,3-b]pyridine anticancer compound treatment. Scientific reports, 11(1), https://doi.org/10.1038/s41598-021-87310-y

Discovery of Novel Sultone Fused Berberine Derivatives as Promising Tdp1 Inhibitors. (2021)
Journal Article
Reynisson. (2021). Discovery of Novel Sultone Fused Berberine Derivatives as Promising Tdp1 Inhibitors. Molecules, https://doi.org/10.3390/molecules26071945

A new type of berberine derivatives was obtained by the reaction of berberrubine with aliphatic sulfonyl chlorides. The new polycyclic compounds have a sultone ring condensed to C and D rings of a protoberberine core. The reaction conditions were dev... Read More about Discovery of Novel Sultone Fused Berberine Derivatives as Promising Tdp1 Inhibitors..

Discovery of novel Hsp90 C-terminal domain inhibitors that disrupt co-chaperone binding. (2021)
Journal Article
Reynisson. (2021). Discovery of novel Hsp90 C-terminal domain inhibitors that disrupt co-chaperone binding. Bioorganic and Medicinal Chemistry Letters, https://doi.org/10.1016/j.bmcl.2021.127857

Heat shock protein 90 (Hsp90) is an essential molecular chaperone that performs vital stress-related and housekeeping functions in cells and is a current therapeutic target for diseases such as cancers. Particularly, the development of Hsp90 C-termin... Read More about Discovery of novel Hsp90 C-terminal domain inhibitors that disrupt co-chaperone binding..

An optimised MALDI-TOF assay for phosphatidylcholine-specific phospholipase C. (2021)
Journal Article
Reynisson. (2021). An optimised MALDI-TOF assay for phosphatidylcholine-specific phospholipase C. Analytical Methods, https://doi.org/10.1039/D0AY02208J

The Bacillus cereus phosphatidylcholine-specific phospholipase C (PC-PLCBc) is an enzyme that catalyses the hydrolysis of phosphatidylcholines into phosphocholine and 1,2-diacylglycerols. PC-PLCBc has found applications in both the food industry and... Read More about An optimised MALDI-TOF assay for phosphatidylcholine-specific phospholipase C..