Search Results - "VOTTA, Bartholomew J."

The Immune Receptor NOD1 and Kinase RIP2 Interact with Bacterial Peptidoglycan on Early Endosomes to Promote Autophagy and Inflammatory Signaling by Irving, Aaron T., Mimuro, Hitomi, Kufer, Thomas A., Lo, Camden, Wheeler, Richard, Turner, Lorinda J., Thomas, Belinda J., Malosse, Christian, Gantier, Michael P., Casillas, Linda N., Votta, Bartholomew J., Bertin, John, Boneca, Ivo G., Sasakawa, Chihiro, Philpott, Dana J., Ferrero, Richard L., Kaparakis-Liaskos, Maria

“…The intracellular innate immune receptor NOD1 detects Gram-negative bacterial peptidoglycan (PG) to induce autophagy and inflammatory responses in host cells…”
Get full text

Extended pharmacodynamic responses observed upon PROTAC-mediated degradation of RIPK2 by Mares, Alina, Miah, Afjal H., Smith, Ian E. D., Rackham, Mark, Thawani, Aditya R., Cryan, Jenni, Haile, Pamela A., Votta, Bartholomew J., Beal, Allison M., Capriotti, Carol, Reilly, Michael A., Fisher, Don T., Zinn, Nico, Bantscheff, Marcus, MacDonald, Thomas T., Vossenkamper, Anna, Dace, Phoebe, Churcher, Ian, Benowitz, Andrew B., Watt, Gillian, Denyer, Jane, Scott-Stevens, Paul, Harling, John D.

“…Proteolysis-Targeting Chimeras (PROTACs) are heterobifunctional small-molecules that can promote the rapid and selective proteasome-mediated degradation of…”
Get full text

Systemic activation of the transient receptor potential vanilloid subtype 4 channel causes endothelial failure and circulatory collapse: Part 2 by Willette, Robert N, Bao, Weike, Nerurkar, Sandhya, Yue, Tian-Li, Doe, Chris P, Stankus, Gerald, Turner, Gregory H, Ju, Haisong, Thomas, Heath, Fishman, Cindy E, Sulpizio, Anthony, Behm, David J, Hoffman, Sandra, Lin, Zuojun, Lozinskaya, Irina, Casillas, Linda N, Lin, Min, Trout, Robert E Lee, Votta, Bartholomew J, Thorneloe, Kevin, Lashinger, Erin S R, Figueroa, David J, Marquis, Robert, Xu, Xiaoping

“…The transient receptor potential (TRP) vanilloid subtype 4 (V4) is a nonselective cation channel that exhibits polymodal activation and is expressed in the…”
Get more information

Randomized clinical study of safety, pharmacokinetics, and pharmacodynamics of RIPK1 inhibitor GSK2982772 in healthy volunteers by Weisel, Kathleen, Scott, Nicola E., Tompson, Debra J., Votta, Bartholomew J., Madhavan, Sujith, Povey, Kat, Wolstenholme, Allen, Simeoni, Monica, Rudo, Todd, Richards‐Peterson, Lauren, Sahota, Tarjinder, Wang, J. Gene, Lich, John, Finger, Joshua, Verticelli, Adeline, Reilly, Michael, Gough, Peter J., Harris, Philip A., Bertin, John, Wang, Mei‐Lun

“…GSK2982772 is a highly selective inhibitor of receptor‐interacting protein kinase 1 (RIPK1) being developed to treat chronic inflammatory diseases. This…”
Get full text

Inhibition of Receptor-Interacting Protein Kinase 1 in Chronic Plaque Psoriasis: A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study by Ludbrook, Valerie J., Budd, David C., Thorn, Katie, Tompson, Debra, Votta, Bartholomew J., Walker, Lucy, Lee, Amy, Chen, Xin, Peppercorn, Amanda, Loo, Wei Jing

“…Introduction Receptor-interacting protein kinase 1 (RIPK1), a key mediator of inflammation through necroptosis and proinflammatory cytokine production, may…”
Get full text

N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), a novel and potent transient receptor potential vanilloid 4 channel agonist induces urinary bladder contraction and hyperactivity: Part I by Thorneloe, Kevin S, Sulpizio, Anthony C, Lin, Zuojun, Figueroa, David J, Clouse, Angela K, McCafferty, Gerald P, Chendrimada, Tim P, Lashinger, Erin S R, Gordon, Earl, Evans, Louise, Misajet, Blake A, Demarini, Douglas J, Nation, Josephine H, Casillas, Linda N, Marquis, Robert W, Votta, Bartholomew J, Sheardown, Steven A, Xu, Xiaoping, Brooks, David P, Laping, Nicholas J, Westfall, Timothy D

“…The transient receptor potential (TRP) vanilloid 4 (TRPV4) member of the TRP superfamily has recently been implicated in numerous physiological processes. In…”
Get more information

Catalytic in vivo protein knockdown by small-molecule PROTACs by Bondeson, Daniel P, Mares, Alina, Smith, Ian E D, Ko, Eunhwa, Campos, Sebastien, Miah, Afjal H, Mulholland, Katie E, Routly, Natasha, Buckley, Dennis L, Gustafson, Jeffrey L, Zinn, Nico, Grandi, Paola, Shimamura, Satoko, Bergamini, Giovanna, Faelth-Savitski, Maria, Bantscheff, Marcus, Cox, Carly, Gordon, Deborah A, Willard, Ryan R, Flanagan, John J, Casillas, Linda N, Votta, Bartholomew J, den Besten, Willem, Famm, Kristoffer, Kruidenier, Laurens, Carter, Paul S, Harling, John D, Churcher, Ian, Crews, Craig M

“…The use of a high-affinity VHL ligand allows the development of chimeric molecules that promote the association of ERRα or RIPK2 with the VHL E3 ubiquitin…”
Get full text

Optimization of a Series of RIPK2 PROTACs by Miah, Afjal H, Smith, Ian E. D, Rackham, Mark, Mares, Alina, Thawani, Aditya R, Nagilla, Rakesh, Haile, Pamela A, Votta, Bartholomew J, Gordon, Laurie J, Watt, Gillian, Denyer, Jane, Fisher, Don T, Dace, Phoebe, Giffen, Paul, Goncalves, Andrea, Churcher, Ian, Scott-Stevens, Paul, Harling, John D

“…Receptor-interacting serine/threonine protein kinase 2 (RIPK2) is an important kinase of the innate immune system. Herein, we describe the optimization of a…”
Get full text

Inhibition of p38 MAP kinase as a therapeutic strategy by Lee, John C, Kumar, Sanjay, Griswold, Don E, Underwood, David C, Votta, Bartholomew J, Adams, Jerry L

“…Since the discovery of p38 MAP kinase in 1994, our understanding of its biology has progressed dramatically. The key advances include (1) identification of p38…”
Get full text

Voltage-gated K+ currents in mouse articular chondrocytes regulate membrane potential by Clark, Robert B., Hatano, Noriyuki, Kondo, Colleen, Belke, Darrell D., Brown, Barry S., Kumar, Sanjay, Votta, Bartholomew J., Giles, Wayne R.

“…Membrane currents and resting potential of isolated primary mouse articular chondrocytes maintained in monolayer cell culture for 1-9 days were recorded using…”
Get full text

Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2‑((4-(Benzo[d]­thiazol-5-ylamino)-6‑(tert-butylsulfonyl)­quinazolin-7-yl)oxy)ethyl Dihydrogen Phosphate, for the Treatment of Inflammatory Diseases by Haile, Pamela A, Casillas, Linda N, Votta, Bartholomew J, Wang, Gren Z, Charnley, Adam K, Dong, Xiaoyang, Bury, Michael J, Romano, Joseph J, Mehlmann, John F, King, Bryan W, Erhard, Karl F, Hanning, Charles R, Lipshutz, David B, Desai, Biva M, Capriotti, Carol A, Schaeffer, Michelle C, Berger, Scott B, Mahajan, Mukesh K, Reilly, Michael A, Nagilla, Rakesh, Rivera, Elizabeth J, Sun, Helen H, Kenna, John K, Beal, Allison M, Ouellette, Michael T, Kelly, Mike, Stemp, Gillian, Convery, Máire A, Vossenkämper, Anna, MacDonald, Thomas T, Gough, Peter J, Bertin, John, Marquis, Robert W

“…RIP2 kinase has been identified as a key signal transduction partner in the NOD2 pathway contributing to a variety of human pathologies, including…”
Get full text

Understanding Pharmacokinetic Disconnect in Preclinical Species for 4-Aminoquinolines: Consequences of Low Permeability and High P-glycoprotein Efflux Ratio on Rat and Dog Oral Pharmacokinetics by Mahajan, Mukesh K, Rivera, Elizabeth J, Sun, Helen H, Nagilla, Rakesh, DeMartino, Michael P, Haile, Pamela A, Casillas, Linda N, Marquis, Robert W, Votta, Bartholomew J, Bertin, John, Reilly, Michael A

“…Receptor Interacting Protein 2 (RIP2) kinase inhibitors have been reported for therapeutic opportunities in inflammatory bowel diseases such as Ulcerative…”
Get more information

Functional characterization of TRPV4 as an osmotically sensitive ion channel in porcine articular chondrocytes by Phan, Mimi N., Leddy, Holly A., Votta, Bartholomew J., Kumar, Sanjay, Levy, Dana S., Lipshutz, David B., Lee, Suk Hee, Liedtke, Wolfgang, Guilak, Farshid

“…Objective Transient receptor potential vanilloid 4 (TRPV4) is a Ca2+‐permeable channel that can be gated by tonicity (osmolarity) and mechanical stimuli…”
Get full text

A New Dimeric Dihydrochalcone and a New Prenylated Flavone from the Bud Covers of Artocarpus altilis:  Potent Inhibitors of Cathepsin K by PATIL, Ashok D., FREYER, Alan J., KILLMER, Lew, OFFEN, Priscilla, TAYLOR, Paul B., VOTTA, Bartholomew J., JOHNSON, Randall K.

“…A MeOH/CH(2)Cl(2) extract of the bud covers of Artocarpus altilis collected in Micronesia showed activity in a cathepsin K inhibition assay. In addition to the…”
Get full text

Chondroprotective role of the osmotically sensitive ion channel transient receptor potential vanilloid 4: Age‐ and sex‐dependent progression of osteoarthritis in Trpv4‐deficient mice by Clark, Andrea L., Votta, Bartholomew J., Kumar, Sanjay, Liedtke, Wolfgang, Guilak, Farshid

“…Objective Mechanical loading significantly influences the physiology and pathology of articular cartilage, although the mechanisms of mechanical signal…”
Get full text

Crystal structures of human RIP2 kinase catalytic domain complexed with ATP-competitive inhibitors: Foundations for understanding inhibitor selectivity by Charnley, Adam K., Convery, Máire A., Lakdawala Shah, Ami, Jones, Emma, Hardwicke, Philip, Bridges, Angela, Ouellette, Michael, Totoritis, Rachel, Schwartz, Benjamin, King, Bryan W., Wisnoski, David D., Kang, James, Eidam, Patrick M., Votta, Bartholomew J., Gough, Peter J., Marquis, Robert W., Bertin, John, Casillas, Linda

“…[Display omitted] Receptor interacting protein 2 (RIP2) is an intracellular kinase and key signaling partner for the pattern recognition receptors NOD1 and…”
Get full text

Discovery of Pyrazolocarboxamides as Potent and Selective Receptor Interacting Protein 2 (RIP2) Kinase Inhibitors by Haffner, Curt D, Charnley, Adam K, Aquino, Christopher J, Casillas, Linda, Convery, Máire A, Cox, Julie A, Elban, Mark A, Goodwin, Nicole C, Gough, Peter J, Haile, Pamela A, Hughes, Terry V, Knapp-Reed, Beth, Kreatsoulas, Constantine, Lakdawala, Ami S, Li, Huijie, Lian, Yiqian, Lipshutz, David, Mehlmann, John F, Ouellette, Michael, Romano, Joseph, Shewchuk, Lisa, Shu, Arthur, Votta, Bartholomew J, Zhou, Huiqiang, Bertin, John, Marquis, Robert W

“…Herein we report the discovery of pyrazolocarboxamides as novel, potent, and kinase selective inhibitors of receptor interacting protein 2 kinase (RIP2)…”
Get full text

Identification of Quinoline-Based RIP2 Kinase Inhibitors with an Improved Therapeutic Index to the hERG Ion Channel by Haile, Pamela A, Casillas, Linda N, Bury, Michael J, Mehlmann, John F, Singhaus, Robert, Charnley, Adam K, Hughes, Terry V, DeMartino, Michael P, Wang, Gren Z, Romano, Joseph J, Dong, Xiaoyang, Plotnikov, Nikolay V, Lakdawala, Ami S, Convery, Maire A, Votta, Bartholomew J, Lipshutz, David B, Desai, Biva M, Swift, Barbara, Capriotti, Carol A, Berger, Scott B, Mahajan, Mukesh K, Reilly, Michael A, Rivera, Elizabeth J, Sun, Helen H, Nagilla, Rakesh, LePage, Carol, Ouellette, Michael T, Totoritis, Rachel D, Donovan, Brian T, Brown, Barry S, Chaudhary, Khuram W, Gough, Peter J, Bertin, John, Marquis, Robert W

“…RIP2 kinase was recently identified as a therapeutic target for a variety of autoimmune diseases. We have reported previously a selective…”
Get full text

Correction to Identification of Quinoline-Based RIP2 Kinase Inhibitors with an Improved Therapeutic Index to the hERG Ion Channel by Haile, Pamela A., Casillas, Linda N., Bury, Michael J., Mehlmann, John F., Singhaus, Robert, Charnley, Adam K., Hughes, Terry V., DeMartino, Michael P., Wang, Gren Z., Romano, Joseph J., Dong, Xiaoyang, Plotnikov, Nikolay V., Lakdawala, Ami S., Duraiswami, Chaya, Convery, Maire A., Votta, Bartholomew J., Lipshutz, David B., Desai, Biva M., Swift, Barbara, Capriotti, Carol A., Berger, Scott B., Mahajan, Mukesh K., Reilly, Michael A., Rivera, Elizabeth J., Sun, Helen H., Nagilla, Rakesh, LePage, Carol, Ouellette, Michael T., Totoritis, Rachel D., Donovan, Brian T., Brown, Barry S., Chaudhary, Khuram W., Gough, Peter J., Bertin, John, Marquis, Robert W.

Get full text

Identification of an antibody‐based immunoassay for measuring direct target binding of RIPK1 inhibitors in cells and tissues by Finger, Joshua N., Brusq, Jean‐Marie, Campobasso, Nino, Cook, Michael N., Deutsch, Jennifer, Haag, Heather, Harris, Philip A., Jenkins, Earl L., Joglekar, Devika, Lich, John D., Maguire, Sean, Nagilla, Rakesh, Rivera, Elizabeth J., Sun, Helen, Votta, Bartholomew J., Bertin, John, Gough, Peter J.

“…Therapies that suppress RIPK1 kinase activity are emerging as promising therapeutic agents for the treatment of multiple inflammatory disorders. The ability to…”
Get full text