Search Results - "Grimster, Neil P."

Covalent PROTACs: the best of both worlds? by Grimster, Neil P

“…Covalent PROTACs combine the cutting edge research areas of targeted covalent inhibitors (TCIs) and proteolysis targeting chimeras (PROTACs). This nascent…”
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Toward the Molecular Mechanism(s) by Which EGCG Treatment Remodels Mature Amyloid Fibrils by Palhano, Fernando L, Lee, Jiyong, Grimster, Neil P, Kelly, Jeffery W

“…Protein misfolding and/or aggregation has been implicated as the cause of several human diseases, such as Alzheimer’s and Parkinson’s diseases and familial…”
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Cu(II)-Catalyzed Direct and Site-Selective Arylation of Indoles Under Mild Conditions by Phipps, Robert J, Grimster, Neil P, Gaunt, Matthew J

“…We have developed a new site-selective Cu(II)-catalyzed C−H bond functionalization process that can selectively arylate indoles at either the C3 or C2 position…”
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Inhibition of Mcl-1 through covalent modification of a noncatalytic lysine side chain by Akçay, Gizem, Belmonte, Matthew A, Aquila, Brian, Chuaqui, Claudio, Hird, Alexander W, Lamb, Michelle L, Rawlins, Philip B, Su, Nancy, Tentarelli, Sharon, Grimster, Neil P, Su, Qibin

“…The use of an aryl boronic acid carbonyl warhead to target a noncatalytic lysine side chain enables the development of covalent inhibitors against the…”
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Palladium-Catalyzed Intermolecular Alkenylation of Indoles by Solvent-Controlled Regioselective CH Functionalization by Grimster, Neil P., Gauntlett, Carolyn, Godfrey, Christopher R. A., Gaunt, Matthew J.

“…Either the C2‐ or the C3‐substituted product can be obtained with the same palladium(II) catalyst in an oxidative intermolecular alkenylation of indoles. A…”
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Mild Aerobic Oxidative Palladium (II) Catalyzed C−H Bond Functionalization:  Regioselective and Switchable C−H Alkenylation and Annulation of Pyrroles by Beck, Elizabeth M, Grimster, Neil P, Hatley, Richard, Gaunt, Matthew J

“…A palladium catalyzed C−H bond functionalization system that operates under ambient and aerobic conditions can be used to alkenylate pyrroles with control of…”
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The Design of Covalent-Based Inhibitors by Ward, Richard A, Grimster, Neil

“…Annual Report on Medicinal Chemistry series, highlights new advances in the field with this new volume presenting interesting chapters. Each chapter is written…”
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Beyond cysteine: recent developments in the area of targeted covalent inhibition by Mukherjee, Herschel, Grimster, Neil P

“…Over the past decade targeted covalent inhibitors have undergone a renaissance due to the clinical validation and regulatory approval of several small molecule…”
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Selective Janus kinase 1 inhibition resolves inflammation and restores hair growth offering a viable treatment option for alopecia areata by Mattsson, Johan, Israelsson, Elisabeth, Björhall, Karin, Yrlid, Linda Fahlén, Thörn, Kristoffer, Thorén, Anna, Toledo, Emelie Andersén, Jinton, Lisa, Öberg, Lisa, Wingren, Cecilia, Tapani, Sofia, Jackson, Sonya G., Skogberg, Gabriel, Lundqvist, Anders J., Hendrickx, Ramon, Cavallin, Anders, Österlund, Torben, Grimster, Neil P., Nilsson, Magnus, Åstrand, Annika

“…Background Janus Kinase (JAK) inhibition has recently demonstrated therapeutic efficacy in both restoring hair growth and resolving inflammation in Alopecia…”
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Catalytic Asymmetric Transannulation of NH-1,2,3-Triazoles with Olefins by Kwok, Sen Wai, Zhang, Li, Grimster, Neil P., Fokin, Valery V.

“…A convenient one‐pot asymmetric synthesis of 2,3‐dihydropyrroles from in situ generated triflated triazoles and olefins is described that further expands the…”
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Aromatic Sulfonyl Fluorides Covalently Kinetically Stabilize Transthyretin to Prevent Amyloidogenesis while Affording a Fluorescent Conjugate by Grimster, Neil P, Connelly, Stephen, Baranczak, Aleksandra, Dong, Jiajia, Krasnova, Larissa B, Sharpless, K. Barry, Powers, Evan T, Wilson, Ian A, Kelly, Jeffery W

“…Molecules that bind selectively to a given protein and then undergo a rapid chemoselective reaction to form a covalent conjugate have utility in drug…”
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Discovery and optimization of covalent Bcl-xL antagonists by Mukherjee, Herschel, Su, Nancy, Belmonte, Matthew A., Hargreaves, David, Patel, Joe, Tentarelli, Sharon, Aquila, Brian, Grimster, Neil P.

“…Over the last ten years, targeted covalent inhibition has become a key discipline within medicinal chemistry research, most notably in the development of…”
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Discovery of the Potent and Selective Inhaled Janus Kinase 1 Inhibitor AZD4604 and Its Preclinical Characterization by Nilsson, Magnus, Berggren, Kristina, Berglund, Susanne, Cerboni, Silvia, Collins, Mia, Dahl, Göran, Elmqvist, David, Grimster, Neil P., Hendrickx, Ramon, Johansson, Johan R., Kettle, Jason G., Lepistö, Matti, Rhedin, Magdalena, Smailagic, Amir, Su, Qibin, Wennberg, Tiiu, Wu, Allan, Österlund, Torben, Naessens, Thomas, Mitra, Suman

“…JAK-STAT cytokines are critical in regulating immunity. Persistent activation of JAK-STAT signaling pathways by cytokines drives chronic inflammatory diseases…”
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Discovery of (2R)‑N‑[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]‑1H‑indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a Potent and Selective Janus Kinase 1 Inhibitor by Su, Qibin, Banks, Erica, Bebernitz, Geraldine, Bell, Kirsten, Borenstein, Cassandra F, Chen, Huawei, Chuaqui, Claudio E, Deng, Nanhua, Ferguson, Andrew D, Kawatkar, Sameer, Grimster, Neil P, Ruston, Linette, Lyne, Paul D, Read, Jon A, Peng, Xianyou, Pei, Xiaohui, Fawell, Stephen, Tang, Zhanlei, Throner, Scott, Vasbinder, Melissa M, Wang, Haoyu, Winter-Holt, Jon, Woessner, Richard, Wu, Allan, Yang, Wenzhan, Zinda, Michael, Kettle, Jason G

“…JAK1, JAK2, JAK3, and TYK2 belong to the JAK (Janus kinase) family. They play critical roles in cytokine signaling. Constitutive activation of JAK/STAT…”
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Accelerated Discovery of Carbamate Cbl‑b Inhibitors Using Generative AI Models and Structure-Based Drug Design by Quinn, Taylor R., Giblin, Kathryn A., Thomson, Clare, Boerth, Jeffrey A., Bommakanti, Gayathri, Braybrooke, Erin, Chan, Christina, Chinn, Alex J., Code, Erin, Cui, Caifeng, Fan, Yukai, Grimster, Neil P., Kohara, Keishi, Lamb, Michelle L., Ma, Lina, Mfuh, Adelphe M., Robb, Graeme R., Robbins, Kevin J., Schimpl, Marianne, Tang, Haoran, Ware, Jamie, Wrigley, Gail L., Xue, Lin, Zhang, Yun, Zhu, Huimin, Hughes, Samantha J.

“…Casitas B-lymphoma proto-oncogene-b (Cbl-b) is a RING finger E3 ligase that has an important role in effector T cell function, acting as a negative regulator…”
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Discovery, Optimization, and Biological Evaluation of Arylpyridones as Cbl‑b Inhibitors by Mfuh, Adelphe M., Boerth, Jeffrey A., Bommakanti, Gayathri, Chan, Christina, Chinn, Alex J., Code, Erin, Fricke, Patrick J., Giblin, Kathryn A., Gohlke, Andrea, Hansel, Catherine, Hariparsad, Niresh, Hughes, Samantha J., Jin, Meizhong, Kantae, Vasudev, Kavanagh, Stefan L., Lamb, Michelle L., Lane, Jordan, Moore, Rachel, Puri, Taranee, Quinn, Taylor R., Reddy, Iswarya, Robb, Graeme R., Robbins, Kevin J., Gancedo Rodrigo, Miguel, Schimpl, Marianne, Singh, Baljinder, Singh, Meha, Tang, Haoran, Thomson, Clare, Walsh, Jarrod J., Ware, Jamie, Watson, Iain D. G., Ye, Min-Wei, Wrigley, Gail L., Zhang, Andrew X., Zhang, Yun, Grimster, Neil P.

“…Casitas B-lymphoma proto-oncogene-b (Cbl-b), a member of the Cbl family of RING finger E3 ubiquitin ligases, has been demonstrated to play a central role in…”
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Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 1 by Kettle, Jason G, Åstrand, Annika, Catley, Matthew, Grimster, Neil P, Nilsson, Magnus, Su, Qibin, Woessner, Richard

“…Janus kinases (JAKs) are a family of four enzymes; JAK1, JAK2, JAK3 and tyrosine kinase 2 (TYK2) that are critical in cytokine signalling and are strongly…”
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Optimization of a series of novel, potent and selective Macrocyclic SYK inhibitors by Grimster, Neil P., Gingipalli, Lakshmaiah, Balazs, Amber, Barlaam, Bernard, Boiko, Scott, Boyd, Scott, Dry, Hannah, Goldberg, Frederick W., Ikeda, Tim, Johnson, Tony, Kawatkar, Sameer, Kemmitt, Paul, Lamont, Scott, Lorthioir, Olivier, Mfuh, Adelphe, Patel, Joe, Pike, Andy, Read, Jon, Romero, Romulo, Sarkar, Ujjal, Sha, Li, Simpson, Iain, Song, Kun, Su, Qibin, Wang, Haixia, Watson, David, Wu, Allan, Zehnder, Troy E., Zheng, XiaoLan, Li, Shaolu, Dong, Zhiqiang, Yang, Dejian, Song, Yanwei, Wang, Peng, Liu, Xuemei, Dowling, James E., Edmondson, Scott D.

“…[Display omitted] Spleen tyrosine kinase (SYK) is a non-receptor cytoplasmic kinase. Due to its pivotal role in B cell receptor and Fc-receptor signalling,…”
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Generation of Candidate Ligands for Nicotinic Acetylcholine Receptors via in situ Click Chemistry with a Soluble Acetylcholine Binding Protein Template by Grimster, Neil P., Stump, Bernhard, Fotsing, Joseph R., Weide, Timo, Talley, Todd T., Yamauchi, John G., Nemecz, Ákos, Kim, Choel, Ho, Kwok-Yiu, Sharpless, K. Barry, Taylor, Palmer, Fokin, Valery V.

“…Nicotinic acetylcholine receptors (nAChRs), which are responsible for mediating key physiological functions, are ubiquitous in the central and peripheral…”
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Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors by Grimster, Neil P, Anderson, Erica, Alimzhanov, Marat, Bebernitz, Geraldine, Bell, Kirsten, Chuaqui, Claudio, Deegan, Tracy, Ferguson, Andrew D, Gero, Thomas, Harsch, Andreas, Huszar, Dennis, Kawatkar, Aarti, Kettle, Jason G, Lyne, Paul, Read, Jon A, Rivard Costa, Caroline, Ruston, Linette, Schroeder, Patricia, Shi, Jie, Su, Qibin, Throner, Scott, Toader, Dorin, Vasbinder, Melissa, Woessner, Richard, Wang, Haixia, Wu, Allan, Ye, Minwei, Zheng, Weijia, Zinda, Michael

“…Janus kinases (JAKs) have been demonstrated to be critical in cytokine signaling and have thus been implicated in both cancer and inflammatory diseases. The…”
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