Search Results - "Lipford, J. Russell"

Prospecting for molecular glues by den Besten, Willem, Lipford, J. Russell

“…Two recent studies identified CDK12 inhibitors that bind to CDK12–cyclin K complexes and act as molecular glues to stabilize an interaction with the ubiquitin…”
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Diverse alterations associated with resistance to KRAS(G12C) inhibition by Zhao, Yulei, Murciano-Goroff, Yonina R., Xue, Jenny Y., Ang, Agnes, Lucas, Jessica, Mai, Trang T., Da Cruz Paula, Arnaud F., Saiki, Anne Y., Mohn, Deanna, Achanta, Pragathi, Sisk, Ann E., Arora, Kanika S., Roy, Rohan S., Kim, Dongsung, Li, Chuanchuan, Lim, Lee P., Li, Mark, Bahr, Amber, Loomis, Brian R., de Stanchina, Elisa, Reis-Filho, Jorge S., Weigelt, Britta, Berger, Michael, Riely, Gregory, Arbour, Kathryn C., Lipford, J. Russell, Li, Bob T., Lito, Piro

“…Inactive state-selective KRAS(G12C) inhibitors 1 – 8 demonstrate a 30–40% response rate and result in approximately 6-month median progression-free survival in…”
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A “Click Chemistry Platform” for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation by Wurz, Ryan P, Dellamaggiore, Ken, Dou, Hannah, Javier, Noelle, Lo, Mei-Chu, McCarter, John D, Mohl, Dane, Sastri, Christine, Lipford, J. Russell, Cee, Victor J

“…Proteolysis targeting chimeras (PROTACs) are bispecific molecules containing a target protein binder and an ubiquitin ligase binder connected by a linker. By…”
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A putative stimulatory role for activator turnover in gene expression by Smith, Geoffrey T, Lipford, J. Russell, Chi, Yong, Deshaies, Raymond J

“…The ubiquitin-proteasome system (UPS) promotes the destruction of target proteins by attaching to them a ubiquitin chain that is recognized by the 26S…”
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A nanoparticle vaccine that targets neoantigen peptides to lymphoid tissues elicits robust antitumor T cell responses by Arbelaez, Carlos A., Estrada, Juan, Gessner, Melissa A., Glaus, Charles, Morales, Agnieszka B., Mohn, Deanna, Phee, Hyewon, Lipford, J. Russell, Johnston, James A.

“…Cancer vaccines using synthetic long peptides (SLP) targeting tumor antigens have been tested in the clinic but the outcomes have been unimpressive, perhaps…”
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Discovery of 1H‑Pyrazol-3(2H)‑ones as Potent and Selective Inhibitors of Protein Kinase R‑like Endoplasmic Reticulum Kinase (PERK) by Smith, Adrian L, Andrews, Kristin L, Beckmann, Holger, Bellon, Steven F, Beltran, Pedro J, Booker, Shon, Chen, Hao, Chung, Young-Ah, D’Angelo, Noel D, Dao, Jennifer, Dellamaggiore, Kenneth R, Jaeckel, Peter, Kendall, Richard, Labitzke, Katja, Long, Alexander M, Materna-Reichelt, Silvia, Mitchell, Petia, Norman, Mark H, Powers, David, Rose, Mark, Shaffer, Paul L, Wu, Michelle M, Lipford, J. Russell

“…The structure-based design and optimization of a novel series of selective PERK inhibitors are described resulting in the identification of 44 as a potent,…”
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Diverse roles for ubiquitin-dependent proteolysis in transcriptional activation by Lipford, J. Russell, Deshaies, Raymond J

“…A growing literature points to a fundamental role for the ubiquitin-proteasome degradation system (UPS) in transcription. Four recent publications add…”
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KRASG12C Inhibition with Sotorasib in Advanced Solid Tumors by Hong, David S, Fakih, Marwan G, Strickler, John H, Desai, Jayesh, Durm, Gregory A, Shapiro, Geoffrey I, Falchook, Gerald S, Price, Timothy J, Sacher, Adrian, Denlinger, Crystal S, Bang, Yung-Jue, Dy, Grace K, Krauss, John C, Kuboki, Yasutoshi, Kuo, James C, Coveler, Andrew L, Park, Keunchil, Kim, Tae Won, Barlesi, Fabrice, Munster, Pamela N, Ramalingam, Suresh S, Burns, Timothy F, Meric-Bernstam, Funda, Henary, Haby, Ngang, Jude, Ngarmchamnanrith, Gataree, Kim, June, Houk, Brett E, Canon, Jude, Lipford, J. Russell, Friberg, Gregory, Lito, Piro, Govindan, Ramaswamy, Li, Bob T

“…Activating mutations in RAS , the most commonly mutated oncogene in human cancer, result in stimulating growth of cells. Sotorasib inhibits the G12C mutant…”
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The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity by Canon, Jude, Rex, Karen, Saiki, Anne Y., Mohr, Christopher, Cooke, Keegan, Bagal, Dhanashri, Gaida, Kevin, Holt, Tyler, Knutson, Charles G., Koppada, Neelima, Lanman, Brian A., Werner, Jonathan, Rapaport, Aaron S., San Miguel, Tisha, Ortiz, Roberto, Osgood, Tao, Sun, Ji-Rong, Zhu, Xiaochun, McCarter, John D., Volak, Laurie P., Houk, Brett E., Fakih, Marwan G., O’Neil, Bert H., Price, Timothy J., Falchook, Gerald S., Desai, Jayesh, Kuo, James, Govindan, Ramaswamy, Hong, David S., Ouyang, Wenjun, Henary, Haby, Arvedson, Tara, Cee, Victor J., Lipford, J. Russell

“…KRAS is the most frequently mutated oncogene in cancer and encodes a key signalling protein in tumours 1 , 2 . The KRAS(G12C) mutant has a cysteine residue…”
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Analysis of Polyubiquitin Conjugates Reveals That the Rpn10 Substrate Receptor Contributes to the Turnover of Multiple Proteasome Targets by Mayor, Thibault, Lipford, J Russell, Graumann, Johannes, Smith, Geoffrey T, Deshaies, Raymond J

“…The polyubiquitin receptor Rpn10 targets ubiquitylated Sic1 to the 26S proteasome for degradation. In contrast, turnover of at least one ubiquitin-proteasome…”
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Mutant-selective AKT inhibition through lysine targeting and neo-zinc chelation by Craven, Gregory B., Chu, Hang, Sun, Jessica D., Carelli, Jordan D., Coyne, Brittany, Chen, Hao, Chen, Ying, Ma, Xiaolei, Das, Subhamoy, Kong, Wayne, Zajdlik, Adam D., Yang, Kin S., Reisberg, Solomon H., Thompson, Peter A., Lipford, J. Russell, Taunton, Jack

“…Somatic alterations in the oncogenic kinase AKT1 have been identified in a broad spectrum of solid tumours. The most common AKT1 alteration replaces Glu17 with…”
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Mercapturate pathway metabolites of sotorasib, a covalent inhibitor of KRASG12C, are associated with renal toxicity in the Sprague Dawley rat by Werner, Jonathan A., Davies, Rhian, Wahlstrom, Jan, Dahal, Upendra P., Jiang, Min, Stauber, Jonathan, David, Benjamin, Siska, William, Thomas, Barbara, Ishida, Katsu, Humphreys, W. Griffith, Lipford, J. Russell, Monticello, Thomas M.

“…Sotorasib is a first-in class KRASG12C covalent inhibitor in clinical development for the treatment of tumors with the KRAS p.G12C mutation. In the nonclinical…”
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Discovery of (R)‑8-(6-Methyl-4-oxo-1,4,5,6-tetrahydro­pyrrolo[3,4‑b]­pyrrol-2-yl)-3-(1-methylcyclopropyl)-2-((1-methylcyclopropyl)­amino)­quinazolin-4(3H)‑one, a Potent and Selective Pim-1/2 Kinase Inhibitor for Hematological Malignancies by Wang, Hui-Ling, Andrews, Kristin L, Booker, Shon K, Canon, Jude, Cee, Victor J, Chavez, Frank, Chen, Yuping, Eastwood, Heather, Guerrero, Nadia, Herberich, Brad, Hickman, Dean, Lanman, Brian A, Laszlo, Jimmy, Lee, Matthew R, Lipford, J. Russell, Mattson, Bethany, Mohr, Christopher, Nguyen, Yen, Norman, Mark H, Pettus, Liping H, Powers, David, Reed, Anthony B, Rex, Karen, Sastri, Christine, Tamayo, Nuria, Wang, Paul, Winston, Jeffrey T, Wu, Bin, Wu, Qiong, Wu, Tian, Wurz, Ryan P, Xu, Yang, Zhou, Yihong, Tasker, Andrew S

“…Pim kinases are a family of constitutively active serine/threonine kinases that are partially redundant and regulate multiple pathways important for cell…”
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Unfolded Protein Response in Cancer: IRE1α Inhibition by Selective Kinase Ligands Does Not Impair Tumor Cell Viability by Harrington, Paul E, Biswas, Kaustav, Malwitz, David, Tasker, Andrew S, Mohr, Christopher, Andrews, Kristin L, Dellamaggiore, Ken, Kendall, Richard, Beckmann, Holger, Jaeckel, Peter, Materna-Reichelt, Silvia, Allen, Jennifer R, Lipford, J. Russell

“…The kinase/endonuclease inositol requiring enzyme 1 (IRE1α), one of the sensors of unfolded protein accumulation in the endoplasmic reticulum that triggers the…”
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Discovery and Optimization of Quinazolinone-pyrrolopyrrolones as Potent and Orally Bioavailable Pan-Pim Kinase Inhibitors by Pettus, Liping H, Andrews, Kristin L, Booker, Shon K, Chen, Jie, Cee, Victor J, Chavez, Frank, Chen, Yuping, Eastwood, Heather, Guerrero, Nadia, Herberich, Bradley, Hickman, Dean, Lanman, Brian A, Laszlo, Jimmy, Lee, Matthew R, Lipford, J. Russell, Mattson, Bethany, Mohr, Christopher, Nguyen, Yen, Norman, Mark H, Powers, David, Reed, Anthony B, Rex, Karen, Sastri, Christine, Tamayo, Nuria, Wang, Paul, Winston, Jeffrey T, Wu, Bin, Wu, Tian, Wurz, Ryan P, Xu, Yang, Zhou, Yihong, Tasker, Andrew S, Wang, Hui-Ling

“…The high expression of proviral insertion site of Moloney murine leukemia virus kinases (Pim-1, -2, and -3) in cancers, particularly the hematopoietic…”
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KRAS G12C Inhibition with Sotorasib in Advanced Solid Tumors by Hong, David S, Fakih, Marwan G, Strickler, John H, Desai, Jayesh, Durm, Gregory A, Shapiro, Geoffrey I, Falchook, Gerald S, Price, Timothy J, Sacher, Adrian, Denlinger, Crystal S, Bang, Yung-Jue, Dy, Grace K, Krauss, John C, Kuboki, Yasutoshi, Kuo, James C, Coveler, Andrew L, Park, Keunchil, Kim, Tae Won, Barlesi, Fabrice, Munster, Pamela N, Ramalingam, Suresh S, Burns, Timothy F, Meric-Bernstam, Funda, Henary, Haby, Ngang, Jude, Ngarmchamnanrith, Gataree, Kim, June, Houk, Brett E, Canon, Jude, Lipford, J Russell, Friberg, Gregory, Lito, Piro, Govindan, Ramaswamy, Li, Bob T

“…No therapies for targeting mutations in cancer have been approved. The p.G12C mutation occurs in 13% of non-small-cell lung cancers (NSCLCs) and in 1 to 3% of…”
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The discovery of novel 3-(pyrazin-2-yl)-1H-indazoles as potent pan-Pim kinase inhibitors by Wang, Hui-Ling, Cee, Victor J., Chavez, Frank, Lanman, Brian A., Reed, Anthony B., Wu, Bin, Guerrero, Nadia, Lipford, J. Russell, Sastri, Christine, Winston, Jeff, Andrews, Kristin L., Huang, Xin, Lee, Matthew R., Mohr, Christopher, Xu, Yang, Zhou, Yihong, Tasker, Andrew S.

“…[Display omitted] The three Pim kinases are a small family of serine/threonine kinases regulating several signaling pathways that are fundamental to…”
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Quantitative measurement of the requirement of diverse protein degradation pathways in MHC class I peptide presentation by Mamrosh, Jennifer L, Sherman, David J, Cohen, Joseph R, Johnston, James A, Joubert, Marisa K, Li, Jing, Lipford, J Russell, Lomenick, Brett, Moradian, Annie, Prabhu, Siddharth, Sweredoski, Michael J, Vander Lugt, Bryan, Verma, Rati, Deshaies, Raymond J

“…Peptides from degradation of intracellular proteins are continuously displayed by major histocompatibility complex (MHC) class I. To better understand origins…”
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Discovery of imidazopyridazines as potent Pim-1/2 kinase inhibitors by Wurz, Ryan P., Sastri, Christine, D’Amico, Derin C., Herberich, Brad, Jackson, Claire L.M., Pettus, Liping H., Tasker, Andrew S., Wu, Bin, Guerrero, Nadia, Lipford, J. Russell, Winston, Jeffrey T., Yang, Yajing, Wang, Paul, Nguyen, Yen, Andrews, Kristin L., Huang, Xin, Lee, Matthew R., Mohr, Christopher, Zhang, J.D., Reid, Darren L., Xu, Yang, Zhou, Yihong, Wang, Hui-Ling

“…[Display omitted] High levels of Pim expression have been implicated in several hematopoietic and solid tumor cancers, suggesting that inhibition of Pim…”
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Discovery of 5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-amines as potent PIM inhibitors by Wu, Bin, Wang, Hui-Ling, Cee, Victor J., Lanman, Brian A., Nixey, Thomas, Pettus, Liping, Reed, Anthony B., Wurz, Ryan P., Guerrero, Nadia, Sastri, Christine, Winston, Jeff, Lipford, J. Russell, Lee, Matthew R., Mohr, Christopher, Andrews, Kristin L., Tasker, Andrew S.

“…[Display omitted] PIM kinases are a family of Ser/Thr kinases that are implicated in tumorigenesis. The discovery of a new class of PIM inhibitors,…”
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