Search Results - "ANDERL, Janet L"

Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2S,3R)‑N‑((S)‑3-(Cyclopent-1-en-1-yl)-1-((R)‑2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-((S)‑2-(2-morpholinoacetamido)­propanamido)­propenamide) by Johnson, Henry W. B, Lowe, Eric, Anderl, Janet L, Fan, Andrea, Muchamuel, Tony, Bowers, Simeon, Moebius, David C, Kirk, Christopher, McMinn, Dustin L

“…Selective immuno­proteasome inhibition is a promising approach for treating autoimmune disorders, but optimal proteolytic active site subunit inhibition…”
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Nonproteasomal Targets of the Proteasome Inhibitors Bortezomib and Carfilzomib: a Link to Clinical Adverse Events by ARASTU-KAPUR, Shirin, ANDERL, Janet L, KIRK, Christopher J, KRAUS, Marianne, PARLATI, Francesco, SHENK, Kevin D, LEE, Susan J, MUCHAMUEL, Tony, BENNETT, Mark K, DRIESSEN, Christoph, BALL, Andrew J

“…Bortezomib (Velcade), a dipeptide boronate 20S proteasome inhibitor and an approved treatment option for multiple myeloma, is associated with a…”
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Signal peptide mimicry primes Sec61 for client-selective inhibition by Rehan, Shahid, Tranter, Dale, Sharp, Phillip P., Craven, Gregory B., Lowe, Eric, Anderl, Janet L., Muchamuel, Tony, Abrishami, Vahid, Kuivanen, Suvi, Wenzell, Nicole A., Jennings, Andy, Kalyanaraman, Chakrapani, Strandin, Tomas, Javanainen, Matti, Vapalahti, Olli, Jacobson, Matthew P., McMinn, Dustin, Kirk, Christopher J., Huiskonen, Juha T., Taunton, Jack, Paavilainen, Ville O.

“…Preventing the biogenesis of disease-relevant proteins is an attractive therapeutic strategy, but attempts to target essential protein biogenesis factors have…”
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Immunoproteasome functions explained by divergence in cleavage specificity and regulation by Winter, Michael B, La Greca, Florencia, Arastu-Kapur, Shirin, Caiazza, Francesco, Cimermancic, Peter, Buchholz, Tonia J, Anderl, Janet L, Ravalin, Matthew, Bohn, Markus F, Sali, Andrej, O'Donoghue, Anthony J, Craik, Charles S

“…The immunoproteasome (iP) has been proposed to perform specialized roles in MHC class I antigen presentation, cytokine modulation, and T cell differentiation…”
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Zetomipzomib (KZR-616) attenuates lupus in mice via modulation of innate and adaptive immune responses by Muchamuel, Tony, Fan, R Andrea, Anderl, Janet L, Bomba, Darrin J, Johnson, Henry W B, Lowe, Eric, Tuch, Brian B, McMinn, Dustin L, Millare, Beatriz, Kirk, Christopher J

“…Zetomipzomib (KZR-616) is a selective inhibitor of the immunoproteasome currently undergoing clinical investigation in autoimmune disorders. Here, we…”
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Antileukemic activity and mechanism of drug resistance to the marine Salinispora tropica proteasome inhibitor salinosporamide A (Marizomib) by Niewerth, Denise, Jansen, Gerrit, Riethoff, Lesley F V, van Meerloo, Johan, Kale, Andrew J, Moore, Bradley S, Assaraf, Yehuda G, Anderl, Janet L, Zweegman, Sonja, Kaspers, Gertjan J L, Cloos, Jacqueline

“…Salinosporamide A (NPI-0052, marizomib) is a naturally occurring proteasome inhibitor derived from the marine actinobacterium Salinispora tropica, and…”
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Carfilzomib demonstrates broad anti-tumor activity in pre-clinical non-small cell and small cell lung cancer models by Baker, Amanda F, Hanke, Neale T, Sands, Barbara J, Carbajal, Liliana, Anderl, Janet L, Garland, Linda L

“…Carfilzomib (CFZ) is a proteasome inhibitor that selectively and irreversibly binds to its target and has been approved in the US for treatment of relapsed and…”
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Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit by Johnson, Henry W. B, Anderl, Janet L, Bradley, Erin K, Bui, John, Jones, Jeffrey, Arastu-Kapur, Shirin, Kelly, Lisa M, Lowe, Eric, Moebius, David C, Muchamuel, Tony, Kirk, Christopher, Wang, Zhengping, McMinn, Dustin

“…Building upon the success of bortezomib (VELCADE) and carfilzomib (KYPROLIS), the design of a next generation of inhibitors targeting specific subunits within…”
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Proteasome composition in immune cells implies special immune‐cell‐specific immunoproteasome function by Inholz, Katharina, Anderl, Janet L., Klawitter, Moritz, Goebel, Heike, Maurits, Elmer, Kirk, Christopher J., Fan, R. Andrea, Basler, Michael

“…Immunoproteasomes are a special class of proteasomes, which can be induced with IFN‐γ in an inflammatory environment. In recent years, it became evident that…”
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Role of Epoxide Hydrolases and Cytochrome P450s on Metabolism of KZR-616, a First-in-Class Selective Inhibitor of the Immunoproteasome by Fang, Ying, Johnson, Henry, Anderl, Janet L, Muchamuel, Tony, McMinn, Dustin, Morisseau, Christophe, Hammock, Bruce D, Kirk, Christopher, Wang, Jinhai

“…KZR-616 is an irreversible tripeptide epoxyketone-based selective inhibitor of the human immunoproteasome. Inhibition of the immunoproteasome results in…”
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Overcoming bortezomib resistance in human B cells by anti-CD20/rituximab-mediated complement-dependent cytotoxicity and epoxyketone-based irreversible proteasome inhibitors by Verbrugge, Sue Ellen, Al, Marjon, Assaraf, Yehuda G, Niewerth, Denise, van Meerloo, Johan, Cloos, Jacqueline, van der Veer, Michael, Scheffer, George L, Peters, Godefridus J, Chan, Elena T, Anderl, Janet L, Kirk, Christopher J, Zweegman, Sonja, Dijkmans, Ben Ac, Lems, Willem F, Scheper, Rik J, de Gruijl, Tanja D, Jansen, Gerrit

“…In clinical and experimental settings, antibody-based anti-CD20/rituximab and small molecule proteasome inhibitor (PI) bortezomib (BTZ) treatment proved…”
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Anti-leukemic activity and mechanisms underlying resistance to the novel immunoproteasome inhibitor PR-924 by Niewerth, Denise, van Meerloo, Johan, Jansen, Gerrit, Assaraf, Yehuda G., Hendrickx, Tessa C., Kirk, Christopher J., Anderl, Janet L., Zweegman, Sonja, Kaspers, Gertjan J.L., Cloos, Jacqueline

“…Despite potent immunoproteasome β5i-subunit inhibition, PR924-sensitive cells require concomitant constitutive β5-subunit inhibtion for apoptosis induction…”
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A neuronal and astrocyte co-culture assay for high content analysis of neurotoxicity by Anderl, Janet L, Redpath, Stella, Ball, Andrew J

“…High Content Analysis (HCA) assays combine cells and detection reagents with automated imaging and powerful image analysis algorithms, allowing measurement of…”
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KZR-616, A Selective Inhibitor of the Immunoproteasome: Preclinical and Clinical Mechanism of Action Studies in Lupus Nephritis: FR-OR38 by Muchamuel, Tony, Fan, Rong A., Anderl, Janet L., Johnson, Henry, Mcminn, Dustin L., Tuch, Brian, Kirk, Christopher

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Abstract 3087: KZR-8834: A novel, small molecule inhibitor of Sec61-dependent protein secretion with anti-tumor activity by Lowe, Eric, Anderl, Janet L., Fan, Andrea R., Jiang, Jing, Johnson, Henry W., Kirk, Christopher J., McMinn, Dustin, Muchamuel, Tony, Taunton, Jack, Whang, Jennifer A.

“…Abstract The majority of secreted and transmembrane (TM) proteins, including growth factors and TM oncogenes, require translocation through Sec61 into the ER…”
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Abstract 3860: Discovery and characterization of novel anti-cancer small molecule inhibitors of Sec61 by Lowe, Eric, Anderl, Janet L., Fan, Andrea R., Fang, Ying, Jiang, Jing, Johnson, Henry W., Kirk, Christopher J., McMinn, Dustin, Muchamuel, Tony, Rao, Meera, Sharp, Phillip P., Taunton, Jack, Wang, Jinhai, Whang, Jennifer A.

“…Abstract Secreted and membrane proteins play key roles in malignant transformation and tumor growth, including autocrine growth factor expression, receptor…”
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Novel assays for neurotoxicity, neural development and neuronal/glia interactionsvia multiplexed HCA of neurons and astrocytes by Fukada, Hitomi, Anderl, Janet L., Ball, Andrew J.

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High Content Analysis of betaIII-tubulin and synaptophysin enables sensitive detection ofneuronal differentiation and neurotoxicity in a variety of cellular models by Hata, Naoki, Kasuga, Takuro, Anderl, Janet L., Ball, Andrew J.

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Neurodegeneration Induced by Bortezomib Exposure in Vitro Occurs Via Proteasome Independent Mechanisms by Arastu-Kapur, Shirin, Ball, Andrew J., Anderl, Janet L., Bennett, Mark K, Kirk, Christopher J

“…Abstract 2859 Poster Board II-835 The dipeptide boronate proteasome inhibitor bortezomib (BTZ; Velcade®) is approved for the treatment of multiple myeloma and…”
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A Neuronal and Astrocyte Co-Culture Assay for High Content Analysis of Neurotoxicity by Anderl, Janet L, Redpath, Stella, Ball, Andrew J

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