Search Results - "Derksen, Darren J."

From Inhibition to Degradation: Targeting the Antiapoptotic Protein Myeloid Cell Leukemia 1 (MCL1) by Papatzimas, James W, Gorobets, Evgueni, Maity, Ranjan, Muniyat, Mir Ishruna, MacCallum, Justin L, Neri, Paola, Bahlis, Nizar J, Derksen, Darren J

“…Protein–protein interactions (PPIs) have emerged as significant targets for therapeutic development, owing to their critical nature in diverse biological…”
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Rapid synthesis of pomalidomide-conjugates for the development of protein degrader libraries by Brownsey, Duncan K, Rowley, Ben C, Gorobets, Evgueni, Gelfand, Benjamin S, Derksen, Darren J

“…Current methods for the preparation of heterobifunctional pomalidomide-conjugates rely on methods that are often low yielding and produce intractable…”
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Pannexin-1 channel inhibition alleviates opioid withdrawal in rodents by modulating locus coeruleus to spinal cord circuitry by Kwok, Charlie H. T., Harding, Erika K., Burma, Nicole E., Markovic, Tamara, Massaly, Nicolas, van den Hoogen, Nynke J., Stokes-Heck, Sierra, Gambeta, Eder, Komarek, Kristina, Yoon, Hye Jean, Navis, Kathleen E., McAllister, Brendan B., Canet-Pons, Julia, Fan, Churmy, Dalgarno, Rebecca, Gorobets, Evgueni, Papatzimas, James W., Zhang, Zizhen, Kohro, Yuta, Anderson, Connor L., Thompson, Roger J., Derksen, Darren J., Morón, Jose A., Zamponi, Gerald W., Trang, Tuan

“…Opioid withdrawal is a liability of chronic opioid use and misuse, impacting people who use prescription or illicit opioids. Hyperactive autonomic output…”
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macroH2A2 antagonizes epigenetic programs of stemness in glioblastoma by Nikolic, Ana, Maule, Francesca, Bobyn, Anna, Ellestad, Katrina, Paik, Seungil, Marhon, Sajid A., Mehdipour, Parinaz, Lun, Xueqing, Chen, Huey-Miin, Mallard, Claire, Hay, Alexander J., Johnston, Michael J., Gafuik, Christopher J., Zemp, Franz J., Shen, Yaoqing, Ninkovic, Nicoletta, Osz, Katalin, Labit, Elodie, Berger, N. Daniel, Brownsey, Duncan K., Kelly, John J., Biernaskie, Jeff, Dirks, Peter B., Derksen, Darren J., Jones, Steven J. M., Senger, Donna L., Chan, Jennifer A., Mahoney, Douglas J., De Carvalho, Daniel D., Gallo, Marco

“…Self-renewal is a crucial property of glioblastoma cells that is enabled by the choreographed functions of chromatin regulators and transcription factors…”
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Generation of Benzyne Species from Diphenylphosphoryl Derivatives: Simultaneous Exchange of Three Functional Groups by Gorobets, Evgueni, Parvez, Masood, Derksen, Darren J., Keay, Brian A.

“…Interaction of (2‐diphenylphosphoryl‐3‐iodo‐4‐methoxy‐phenyl) methanol with NaH in DMF at ambient temperature results in the generation of benzyne…”
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Natural-Product-Derived Transient Receptor Potential Melastatin 8 (TRPM8) Channel Modulators by LeGay, Christina M, Gorobets, Evgueni, Iftinca, Mircea, Ramachandran, Rithwik, Altier, Christophe, Derksen, Darren J

“…A library of novel structural hybrids of menthol and cubebol was tested for each derivative’s ability to interact with the transient receptor potential…”
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Hydrophobic Interactions as Substitutes for a Conserved Disulfide Linkage in the Type IIa Bacteriocins, Leucocin A and Pediocin PA-1 by Derksen, Darren J, Boudreau, Marc A, Vederas, John C

“…High and dry: Three analogues of leucocin A (shown in figure) and six analogues of pediocin PA‐1 were synthesized in which conserved cysteines that form a…”
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Metformin Prevents Hyperglycemia-Associated, Oxidative Stress-Induced Vascular Endothelial Dysfunction: Essential Role for the Orphan Nuclear Receptor Human Nuclear Receptor 4A1 (Nur77) by Venu, Vivek Krishna Pulakazhi, Saifeddine, Mahmoud, Mihara, Koichiro, Faiza, Muniba, Gorobets, Evgueni, Flewelling, Andrew J., Derksen, Darren J., Hirota, Simon A., Marei, Isra, Al-Majid, Dana, Motahhary, Majid, Ding, Hong, Triggle, Chris R., Hollenberg, Morley D.

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Pannexin 1 Channels as a Therapeutic Target: Structure, Inhibition, and Outlook by Navis, Kathleen E, Fan, Churmy Y, Trang, Tuan, Thompson, Roger J, Derksen, Darren J

“…Pannexin 1 (Panx1) channels are transmembrane proteins that release adenosine triphosphate and play an important role in intercellular communication. They are…”
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ADAM protease inhibition overcomes resistance of breast cancer stem-like cells to γδ T cell immunotherapy by Dutta, Indrani, Dieters-Castator, Dylan, Papatzimas, James W., Medina, Anais, Schueler, Julia, Derksen, Darren J., Lajoie, Gilles, Postovit, Lynne-Marie, Siegers, Gabrielle M.

“…Gamma delta T cells (γδTc) have tremendous anti-tumoral activity, thus γδTc immunotherapy is currently under development for various malignancies. We targeted…”
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Leveraging Pyrazolium Ylide Reactivity to Access Indolizine and 1,2‐Dihydropyrimidine Derivatives by Tran, Ricky, Brownsey, Duncan K., O'Sullivan, Leonie, Brandow, Connor M. J., Chang, Emily S., Zhou, Wen, Patel, Ketul V., Gorobets, Evgueni, Derksen, Darren J.

“…N‐Heterocyclic ylides are important synthetic precursors to rapidly build molecular complexity. Pyrazolium ylides have largely been unexplored, and we…”
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Regioselective Synthesis of C3-Hydroxyarylated Pyrazoles by O'Sullivan, Leonie, Patel, Ketul V, Rowley, Ben C, Brownsey, Duncan K, Gorobets, Evgueni, Gelfand, Benjamin S, Van Humbeck, Jeffrey F, Derksen, Darren J

“…Pyrazoles are ubiquitous structures in medicinal chemistry. We report the first regioselective route to C3-hydroxyarylated pyrazoles obtained through reaction…”
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Utilising the intrinsic fluorescence of pomalidomide for imaging applications by Brownsey, Duncan K, Gafuik, Christopher J, Kim, Dae-Sun, O'Sullivan, Leonie, Gorobets, Evgueni, Krukowski, Samuel, Turk, Madison, Jenne, Craig N, Mahoney, Douglas J, Derksen, Darren J

“…Optimisation of protein degraders requires balancing multiple factors including potency, cell permeability and solubility. Here we show that the fluorescence…”
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Development of Tetrahydroquinoline-Based Inhibitors for Chronic Pain by Patel, Ketul V., Gadotti, Vinicius M., Garcia-Caballero, Agustin, Antunes, Flavia T. T., Ali, Md Yousof, Zamponi, Gerald W., Derksen, Darren J.

“…Chronic pain affects a substantial portion of the population, posing a significant health challenge. Current treatments often come with limitations and side…”
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Divergent Photocyclization/1,4-Sigmatropic Rearrangements for the Synthesis of Sesquiterpenoid Derivatives by Gorobets, Evgueni, Wong, Norman E, Paton, Robert S, Derksen, Darren J

“…Combined experimental and computational efforts have demonstrated the utility of divergent photocyclization/1,4-sigmatropic rearrangement reactions for…”
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Photolysis of Diacyl Peroxides:  A Radical-Based Approach for the Synthesis of Functionalized Amino Acids by Spantulescu, M. Daniel, Jain, Rajendra P, Derksen, Darren J, Vederas, John C

“…Photolysis of the amino acid derived symmetrical and unsymmetrical diacyl peroxides at 254 nm at low temperature (−78 to −196 °C) generates various bis(amino…”
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Synthesis and evaluation of anti-inflammatory activity of derivatives of the marine natural products fuscol and eunicol by Kerr, Russell G., Brophy, Shawn, Derksen, Darren J.

“…The octocoral-derived terpenes fuscol and eunicol are known, potent anti-inflammatory agents. While total syntheses of one of the parent natural products have…”
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Identification of ligand linkage vectors for the development of p300/CBP degraders by Brownsey, Duncan K, Rowley, Ben C, Gorobets, Evgueni, Mihara, Koichiro, Maity, Ranjan, Papatzimas, James W, Gelfand, Benjamin S, Hollenberg, Morley D, Bahlis, Nizar J, Derksen, Darren J

“…To develop new degrader molecules from an existing protein ligand a linkage vector must be identified and then joined with a suitable E3 ligase without…”
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Inhibition of serine and proline racemases by substrate-product analogues by Harty, Matthew, Nagar, Mitesh, Atkinson, Logan, Legay, Christina M, Derksen, Darren J, Bearne, Stephen L

“…d-Amino acids can play important roles as specific biosynthetic building blocks required by organisms or act as regulatory molecules. Consequently, amino acid…”
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Antimicrobial Leucocin Analogues with a Disulfide Bridge Replaced by a Carbocycle or by Noncovalent Interactions of Allyl Glycine Residues by Derksen, Darren J., Stymiest, Jake L., Vederas, John C.

“…The type IIa bacteriocins are antimicrobial peptides isolated from lactic acid bacteria that act as food preservation agents and have nanomolar activity…”
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