All Outputs (8)

Synthesis of fluorinated carbocyclic pyrimidine nucleoside analogues (2022)
Journal Article
Benckendorff, C., Slyusarchuk, V. D., Huang, N., Lima, M. A., Smith, M., & Miller, G. J. (2022). Synthesis of fluorinated carbocyclic pyrimidine nucleoside analogues. Organic and Biomolecular Chemistry, 20(47), 9469 - 9489. https://doi.org/10.1039/D2OB01761J

Analogues of the canonical nucleosides have a longstanding presence and proven capability within medicinal chemistry and drug discovery research. The synthesis reported herein successfully replaces furanose oxygen with CF2 and CHF in pyrimidine nucle... Read More about Synthesis of fluorinated carbocyclic pyrimidine nucleoside analogues.

Evidence for multiple binding modes in the initial contact between SARS-CoV-2 spike S1 protein and cell surface glycans. (2022)
Journal Article
Parafioriti, M., Ni, M., Petitou, M., Mycroft‐West, C. J., Rudd, T. R., Gandhi, N. S., …Elli, S. (2023). Evidence for multiple binding modes in the initial contact between SARS-CoV-2 spike S1 protein and cell surface glycans. Chemistry - A European Journal, 29(1), https://doi.org/10.1002/chem.202202599

Infection of host cells by SARS-CoV-2 begins with recognition by the virus S (spike) protein of cell surface heparan sulfate (HS), tethering the virus to the extracellular matrix environment, and causing the subunit S1-RBD to undergo a conformational... Read More about Evidence for multiple binding modes in the initial contact between SARS-CoV-2 spike S1 protein and cell surface glycans..

Phosphorylation and sulfation share a common biosynthetic pathway, but extend biochemical and evolutionary diversity of biological macromolecules in distinct ways (2022)
Journal Article
Andrade De Lima, M., Rudd, T., Fernig, D., & Yates, E. (2022). Phosphorylation and sulfation share a common biosynthetic pathway, but extend biochemical and evolutionary diversity of biological macromolecules in distinct ways. Journal of the Royal Society. Interface, 19(193), https://doi.org/10.1098/rsif.2022.0391

<jats:p>Phosphate and sulfate groups are integral to energy metabolism and introduce negative charges into biological macromolecules. One purpose of such modifications is to elicit precise binding/activation of protein partners. The physico-chemical... Read More about Phosphorylation and sulfation share a common biosynthetic pathway, but extend biochemical and evolutionary diversity of biological macromolecules in distinct ways.

Using NMR to Dissect the Chemical Space and O-Sulfation Effects within the O- and S-Glycoside Analogues of Heparan Sulfate. (2022)
Journal Article
Meneghetti, M., Naughton, L., O'Shea, C., Koffi Teki, D., Chagnault, V., Nader, H., …Andrade De Lima, M. (2022). Using NMR to Dissect the Chemical Space and O-Sulfation Effects within the O- and S-Glycoside Analogues of Heparan Sulfate. ACS Omega, 7(28), 24461 - 24467. https://doi.org/10.1021/acsomega.2c02070

Heparan sulfate (HS), a sulfated linear carbohydrate that decorates the cell surface and extracellular matrix, is ubiquitously distributed throughout the animal kingdom and represents a key regulator of biological processes and a largely untapped res... Read More about Using NMR to Dissect the Chemical Space and O-Sulfation Effects within the O- and S-Glycoside Analogues of Heparan Sulfate..

Synthetic Heparan Sulfate Mimetic Pixatimod (PG545) Potently Inhibits SARS-CoV-2 by Disrupting the Spike-ACE2 Interaction. (2022)
Journal Article
Guimond, S., Mycroft-West, C. J., Gandhi, N. S., Tree, J. A., C.Le, T. T., Spalluto, M., …Turnbull, J. E. (2022). Synthetic Heparan Sulfate Mimetic Pixatimod (PG545) Potently Inhibits SARS-CoV-2 by Disrupting the Spike-ACE2 Interaction. ACS Central Science, 8(5), 527 - 545. https://doi.org/10.1021/acscentsci.1c01293

Heparan sulfate (HS) is a cell surface polysaccharide recently identified as a coreceptor with the ACE2 protein for the S1 spike protein on SARS-CoV-2 virus, providing a tractable new therapeutic target. Clinically used heparins demonstrate an inhibi... Read More about Synthetic Heparan Sulfate Mimetic Pixatimod (PG545) Potently Inhibits SARS-CoV-2 by Disrupting the Spike-ACE2 Interaction..

Analysis of protein-heparin interactions using a portable SPR instrument (2022)
Journal Article
Su, D., Li, Y., Yates, E., Skidmore, M., Andrade De Lima, M., & Fernig, D. (2022). Analysis of protein-heparin interactions using a portable SPR instrument. PeerJ Analytical Chemistry, 4, 1-16. https://doi.org/10.7717/peerj-achem.15

<jats:p>Optical biosensors such as those based on surface plasmon resonance (SPR) are a key analytical tool for understanding biomolecular interactions and function as well as the quantitative analysis of analytes in a wide variety of settings. The a... Read More about Analysis of protein-heparin interactions using a portable SPR instrument.

New anti-angiogenic compound based on chemically modified heparin (2022)
Journal Article
Kniggendorf, V., Souza, M., Russo, T., Andrade De Lima, M., Grupenmacher, A., Regatieri, C., & Dreyfuss, J. (2022). New anti-angiogenic compound based on chemically modified heparin. Graefe's Archive for Clinical and Experimental Ophthalmology, 1 - 9. https://doi.org/10.1007/s00417-022-05828-x

Purpose The purpose of this study was to measure the anti-angiogenic effect of N-desulfated Re–N-acetylated, a chemically modified heparin (mHep). Methods In vitro assays (cell tube formation, viability, proliferation, and migration) with endothelial... Read More about New anti-angiogenic compound based on chemically modified heparin.

Neuroprogenitor Cells From Patients With TBCK Encephalopathy Suggest Deregulation of Early Secretory Vesicle Transport (2022)
Journal Article
Moreira, D., Suzuki, A., Silva, A., Varella-Branco, E., Meneghetti, M., Kobayashi, G., …Passos-Bueno, M. (2022). Neuroprogenitor Cells From Patients With TBCK Encephalopathy Suggest Deregulation of Early Secretory Vesicle Transport. Frontiers in Cellular Neuroscience, 15, https://doi.org/10.3389/fncel.2021.803302

<jats:p>Biallelic pathogenic variants in TBCK cause encephaloneuropathy, infantile hypotonia with psychomotor retardation, and characteristic facies 3 (IHPRF3). The molecular mechanisms underlying its neuronal phenotype are largely unexplored. In thi... Read More about Neuroprogenitor Cells From Patients With TBCK Encephalopathy Suggest Deregulation of Early Secretory Vesicle Transport.