Search Results - "VERNER, Erik"

Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy by Honigberg, Lee A, Smith, Ashley M, Sirisawad, Mint, Verner, Erik, Loury, David, Chang, Betty, Li, Shyr, Pan, Zhengying, Thamm, Douglas H, Miller, Richard A, Buggy, Joseph J

“…Activation of the B-cell antigen receptor (BCR) signaling pathway contributes to the initiation and maintenance of B-cell malignancies and autoimmune diseases…”
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Isoform-specific histone deacetylase inhibitors: The next step? by Balasubramanian, Sriram, Verner, Erik, Buggy, Joseph J

“…Abstract Histone deacetylases (HDACs) have emerged as attractive drug targets, particularly for neoplastic indications. This large family is divided into four…”
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Discovery of Reversible Covalent Bruton’s Tyrosine Kinase Inhibitors PRN473 and PRN1008 (Rilzabrutinib) by Owens, Timothy D, Brameld, Ken A, Verner, Erik J, Ton, Tony, Li, Xiaoyan, Zhu, Jiang, Masjedizadeh, Mohammad R, Bradshaw, J. Michael, Hill, Ronald J, Tam, Danny, Bisconte, Angelina, Kim, Eun Ok, Francesco, Michelle, Xing, Yan, Shu, Jin, Karr, Dane, LaStant, Jacob, Finkle, David, Loewenstein, Natalie, Haberstock-Debic, Helena, Taylor, Michael J, Nunn, Philip, Langrish, Claire L, Goldstein, David M

“…Bruton’s tyrosine kinase (BTK), a Tec family tyrosine kinase, is critical in immune pathways as an essential intracellular signaling element, participating in…”
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CRA-024781: a novel synthetic inhibitor of histone deacetylase enzymes with antitumor activity in vitro and in vivo by Buggy, Joseph J, Cao, Z Alexander, Bass, Kathryn E, Verner, Erik, Balasubramanian, Sriram, Liu, Liang, Schultz, Brian E, Young, Peter R, Dalrymple, Stacie A

“…CRA-024781 is a novel, broad spectrum hydroxamic acid–based inhibitor of histone deacetylase (HDAC) that shows antitumor activity in vitro and in vivo…”
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Development of Serine Protease Inhibitors Displaying a Multicentered Short (<2.3 Å) Hydrogen Bond Binding Mode:  Inhibitors of Urokinase-Type Plasminogen Activator and Factor Xa by Verner, Erik, Katz, Bradley A, Spencer, Jeffrey R, Allen, Darin, Hataye, Jason, Hruzewicz, Witold, Hui, Hon C, Kolesnikov, Aleksandr, Li, Yong, Luong, Christine, Martelli, Arnold, Radika, Kesavan, Rai, Roopa, She, Miles, Shrader, William, Sprengeler, Paul A, Trapp, Sean, Wang, Jing, Young, Wendy B, Mackman, Richard L

“…Novel scaffolds that bind to serine proteases through a unique network of short hydrogen bonds to the catalytic Ser195 have been developed. The resulting…”
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CRA-026440: a potent, broad-spectrum, hydroxamic histone deacetylase inhibitor with antiproliferative and antiangiogenic activity in vitro and in vivo by Cao, Z Alexander, Bass, Kathryn E, Balasubramanian, Sriram, Liu, Liang, Schultz, Brian, Verner, Erik, Dai, Yuqin, Molina, Rafael A, Davis, Jack R, Misialek, Shawn, Sendzik, Martin, Orr, Christine J, Leung, Ling, Callan, Ondine, Young, Peter, Dalrymple, Stacie A, Buggy, Joseph J

“…CRA-026440 is a novel, broad-spectrum, hydroxamic acid–based inhibitor of histone deacetylase (HDAC) that shows antitumor and antiangiogenic activities in…”
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Prolonged and tunable residence time using reversible covalent kinase inhibitors by Bradshaw, J Michael, McFarland, Jesse M, Paavilainen, Ville O, Bisconte, Angelina, Tam, Danny, Phan, Vernon T, Romanov, Sergei, Finkle, David, Shu, Jin, Patel, Vaishali, Ton, Tony, Li, Xiaoyan, Loughhead, David G, Nunn, Philip A, Karr, Dane E, Gerritsen, Mary E, Funk, Jens Oliver, Owens, Timothy D, Verner, Erik, Brameld, Ken A, Hill, Ronald J, Goldstein, David M, Taunton, Jack

“…Structural changes in the capping groups of inverted cyanoacrylamide-based kinase inhibitors resulted in alterations in residence time, with some compounds…”
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Discovery of the Irreversible Covalent FGFR Inhibitor 8‑(3-(4-Acryloyl­piperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)­pyrido[2,3‑d]­pyrimidin-7(8H)‑one (PRN1371) for the Treatment of Solid Tumors by Brameld, Ken A, Owens, Timothy D, Verner, Erik, Venetsanakos, Eleni, Bradshaw, J. Michael, Phan, Vernon T, Tam, Danny, Leung, Kwan, Shu, Jin, LaStant, Jacob, Loughhead, David G, Ton, Tony, Karr, Dane E, Gerritsen, Mary E, Goldstein, David M, Funk, Jens Oliver

“…Aberrant signaling of the FGF/FGFR pathway occurs frequently in cancers and is an oncogenic driver in many solid tumors. Clinical validation of FGFR as a…”
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ITK Inhibitor Induces Dose-Dependent Th1 Skewing in Normal T Cells and Is Active in Refractory T Cell Lymphomas by Song, Yuqin, Ding, Ning, Yoon, Dok Hyun, Reneau, John C., Wilcox, Ryan A., Kim, Won Seog, Kim, Youn H., Khodadoust, Michael S., Feldman, Tatyana A., Yannakou, Costas K., Giri, Pratyush, Brammer, Jonathan E, Hsu, Lih-Yun, Yuan, Hongwei, Verner, Erik, Mahabhashyam, Suresh, Miller, Richard A.

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Preliminary Clinical Data from a Phase 1 Trial with CPI-818, a Selective ITK Inhibitor That Preferentially Blocks the Growth of T Lymphoma Cells by Ng, Patrick P., Mobasher, Mehrdad, Yeung, Kitman S., Hotson, Andrew N., Hill, Craig M., Madriaga, Antonett, Dao-Pick, Trang P., Verner, Erik, Radeski, Dejan, Khodadoust, Michael S., Kim, Youn H., Miller, Richard A., Buggy, Joseph J., Janc, James W.

“…Introduction ITK is a tyrosine kinase critical to T cell receptor (TCR) signaling. Overexpression of this gene has been reported in cutaneous T-cell lymphoma…”
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Abstract 1313: CPI-818: A selective inhibitor of interleukin-2-inducible T-cell kinase (ITK) that inhibits T-cell receptor signaling, promotes Th1 skewing, and achieves objective tumor responses when administered to dogs with T cell lymphomas by Janc, James W., Hill, Craig M., Ng, Patrick P., Hoston, Andrew N., Madriaga, Antonett, Dao-Pick, Trang P., Yeung, Kitman S., Hudson, Ryan, Beausoleil, Anne-Marie, Bradley, Erin, Verner, Erik, Thamm, Douglas H., Miller, Richard A., Buggy, Joseph J.

“…Abstract Background: ITK is a non-receptor tyrosine kinase that modifies T cell receptor (TCR) signaling. Mice deficient in ITK, but not resting lymphocyte…”
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Targeting Interleukin-2-inducible T-cell Kinase (ITK) and Resting Lymphocyte Kinase (RLK) Using a Novel Covalent Inhibitor PRN694 by Zhong, Yiming, Dong, Shuai, Strattan, Ethan, Ren, Li, Butchar, Jonathan P., Thornton, Kelsey, Mishra, Anjali, Porcu, Pierluigi, Bradshaw, J. Michael, Bisconte, Angelina, Owens, Timothy D., Verner, Erik, Brameld, Ken A., Funk, Jens Oliver, Hill, Ronald J., Johnson, Amy J., Dubovsky, Jason A.

“…Interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK or TXK) are essential mediators of intracellular signaling in both normal and…”
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The Irreversible Covalent Fibroblast Growth Factor Receptor Inhibitor PRN1371 Exhibits Sustained Inhibition of FGFR after Drug Clearance by Venetsanakos, Eleni, Brameld, Ken A, Phan, Vernon T, Verner, Erik, Owens, Timothy D, Xing, Yan, Tam, Danny, LaStant, Jacob, Leung, Kwan, Karr, Dane E, Hill, Ronald J, Gerritsen, Mary E, Goldstein, David M, Funk, Jens Oliver, Bradshaw, J Michael

“…An increasing number of cancers are known to harbor mutations, translocations, or amplifications in the fibroblast growth factor receptor (FGFR) family of…”
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Abstract 1813: Selective ITK blockade induces antitumor responses and enhances efficacy to immune checkpoint inhibitors in preclinical models by Hsu, Lih-Yun, Pawar, Rahul D., Li, Dan, Ghosh, Poorva, Nguyen, Kevin, Williams, Carlene, Song, Yuqin, Ding, Ning, Verner, Erik, Miller, Richard A.

“…Abstract Interleukin 2 inducible T cell kinase (ITK) plays a role in both T cell receptor (TCR) signaling and T helper cell differentiation. ITK-/- mice…”
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Structural Snapshots of Human HDAC8 Provide Insights into the Class I Histone Deacetylases by Somoza, John R, Skene, Robert J, Katz, Bradley A, Mol, Clifford, Ho, Joseph D, Jennings, Andy J, Luong, Christine, Arvai, Andrew, Buggy, Joseph J, Chi, Ellen, Tang, Jie, Sang, Bi-Ching, Verner, Erik, Wynands, Robert, Leahy, Ellen M, Dougan, Douglas R, Snell, Gyorgy, Navre, Marc, Knuth, Mark W, Swanson, Ronald V, McRee, Duncan E, Tari, Leslie W

“…Modulation of the acetylation state of histones plays a pivotal role in the regulation of gene expression. Histone deacetylases (HDACs) catalyze the removal of…”
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Efficacy in collagen induced arthritis models with a selective, reversible covalent Bruton’s tyrosine kinase inhibitor PRN473 is driven by durable target occupancy rather than extended plasma exposure (THER5P.904) by Bisconte, Angelina, Hill, Ronald, Bradshaw, Michael, Verner, Erik, Finkle, David, Brameld, Ken, Funk, Jens, Goldstein, David, Nunn, Phil

“…Abstract Bruton’s Tyrosine Kinase (BTK) is an essential signaling element downstream of the B-cell receptor (BCR). Inhibition of BTK activity in B cells…”
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Inversion of configuration in the displacement of lithium by hydrogen during a transannular 1,4-hydrogen transfer accompanying a [1,2]-Wittig rearrangement by Verner, Erik J, Cohen, Theodore

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Stereochemical analysis of totally stereoselective competing [1,2]- and 2,3]-Wittig rearrangements. Inversion at the lithium-bearing carbon atom by Verner, Erik J, Cohen, Theodore

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Targeting Interleukin-2-Inducible T-Cell Kinase (ITK) and Resting Lymphocyte Kinase (RLK) Using a Novel Covalent Inhibitor PRN694 by Zhong, Yiming, Dong, Shuai, Thornton, Kelsey, Mishra, Anjali, Porcu, Pierluigi, Bradshaw, Michael, Bisconte, Angelina, Owens, Timothy, Verner, Erik, Brameld, Ken, Funk, Jens Oliver, Hill, Ronald, Johnson, Amy J., Dubovsky, Jason A

“…▪ IL2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) are two members of the Tec family of non-receptor tyrosine kinases which are essential…”
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Abstract 5434: Development and biological characterization of novel, potent and stable isoform-specific inhibitors of histone deacetylase-8 (HDAC8) by Balasubramanian, Sriram, Sirisawad, Mint, Verner, Erik, Mani, Chitra, Jejurkar, Purvi, Buggy, Joseph J.

“…Abstract Histone deacetylase (HDAC) inhibitors have shown promise for the treatment of hematological and solid tumors. The current clinical candidates all…”
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