Search Results - "Bryant, Clifford"

K2P2.1 (TREK-1)–activator complexes reveal a cryptic selectivity filter binding site by Lolicato, Marco, Arrigoni, Cristina, Mori, Takahiro, Sekioka, Yoko, Bryant, Clifford, Clark, Kimberly A., Minor, Daniel L.

“…Crystal structures of an activated two-pore potassium channel reveal a cryptic binding pocket that binds small-molecule activators that restrict the mobility…”
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Predicting binding to p-glycoprotein by flexible receptor docking by Dolghih, Elena, Bryant, Clifford, Renslo, Adam R, Jacobson, Matthew P

“…P-glycoprotein (P-gp) is an ATP-dependent transport protein that is selectively expressed at entry points of xenobiotics where, acting as an efflux pump, it…”
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Different 2-Aminothiazole Therapeutics Produce Distinct Patterns of Scrapie Prion Neuropathology in Mouse Brains by Giles, Kurt, Berry, David B, Condello, Carlo, Hawley, Ronald C, Gallardo-Godoy, Alejandra, Bryant, Clifford, Oehler, Abby, Elepano, Manuel, Bhardwaj, Sumita, Patel, Smita, Silber, B Michael, Guan, Shenheng, DeArmond, Stephen J, Renslo, Adam R, Prusiner, Stanley B

“…Because no drug exists that halts or even slows any neurodegenerative disease, developing effective therapeutics for any prion disorder is urgent. We recently…”
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Pyrvinium Pamoate and Structural Analogs Are Early Macrofilaricide Leads by Gunderson, Emma L, Bryant, Clifford, Bulman, Christina A, Fischer, Chelsea, Luo, Mona, Vogel, Ian, Lim, Kee-Chong, Jawahar, Shabnam, Tricoche, Nancy, Voronin, Denis, Corbo, Christopher, Ayiseh, Rene B, Manfo, Faustin P T, Mbah, Glory E, Cho-Ngwa, Fidelis, Beerntsen, Brenda, Renslo, Adam R, Lustigman, Sara, Sakanari, Judy A

“…Onchocerciasis and lymphatic filariasis are neglected tropical diseases caused by infection with filarial worms. Annual or biannual mass drug administration…”
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Chemical-biological characterization of a cruzain inhibitor reveals a second target and a mammalian off-target by Choy, Jonathan W, Bryant, Clifford, Calvet, Claudia M, Doyle, Patricia S, Gunatilleke, Shamila S, Leung, Siegfried S F, Ang, Kenny K H, Chen, Steven, Gut, Jiri, Oses-Prieto, Juan A, Johnston, Jonathan B, Arkin, Michelle R, Burlingame, Alma L, Taunton, Jack, Jacobson, Matthew P, McKerrow, James M, Podust, Larissa M, Renslo, Adam R

“…Inhibition of the Trypanosoma cruzi cysteine protease cruzain has been proposed as a therapeutic approach for the treatment of Chagas' disease. Among the…”
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Cartilage thickness measurements from optical coherence tomography by Rogowska, Jadwiga, Bryant, Clifford M, Brezinski, Mark E

“…We describe a new semiautomatic image processing method for detecting the cartilage boundaries in optical coherence tomography (OCT). In particular, we focus…”
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Engaging a Non-catalytic Cysteine Residue Drives Potent and Selective Inhibition of Caspase‑6 by Van Horn, Kurt S., Wang, Dongju, Medina-Cleghorn, Daniel, Lee, Peter S., Bryant, Clifford, Altobelli, Chad, Jaishankar, Priyadarshini, Leung, Kevin K., Ng, Raymond A., Ambrose, Andrew J., Tang, Yinyan, Arkin, Michelle R., Renslo, Adam R.

“…Caspases are a family of cysteine-dependent proteases with important cellular functions in inflammation and apoptosis, while also implicated in human diseases…”
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Protein and Chemical Determinants of BL-1249 Action and Selectivity for K 2P Channels by Pope, Lianne, Arrigoni, Cristina, Lou, Hubing, Bryant, Clifford, Gallardo-Godoy, Alejandra, Renslo, Adam R, Minor, Jr, Daniel L

“…K potassium channels generate leak currents that stabilize the resting membrane potential of excitable cells. Various K channels are implicated in pain,…”
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Development of covalent chemogenetic K 2P channel activators by Deal, Parker E, Lee, Haerim, Mondal, Abhisek, Lolicato, Marco, Mendonça, Philipe Ribeiro Furtado de, Black, Holly, Jang, Seil, El-Hilali, Xochina, Bryant, Clifford, Isacoff, Ehud Y, Renslo, Adam R, Minor, Jr, Daniel L

“…K potassium channels regulate excitability by affecting cellular resting membrane potential in the brain, cardiovascular system, immune cells, and sensory…”
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Protein and Chemical Determinants of BL-1249 Action and Selectivity for K2P Channels by Pope, Lianne, Arrigoni, Cristina, Lou, Hubing, Bryant, Clifford, Gallardo-Godoy, Alejandra, Renslo, Adam R, Minor, Daniel L

“…K2P potassium channels generate leak currents that stabilize the resting membrane potential of excitable cells. Various K2P channels are implicated in pain,…”
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K2P2.1 (TREK-1)-Activator Complexes Reveal a Cryptic Selectivity Filter Binding Site by Lolicato, Marco, Arrigoni, Cristina, Mori, Takahiro, Sekioka, Yoko, Bryant, Clifford, Clark, Kimberly A., Minor, Daniel L.

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K^sub 2P^2.1 (TREK-1)–activator complexes reveal a cryptic selectivity filter binding site by Lolicato, Marco, Arrigoni, Cristina, Mori, Takahiro, Sekioka, Yoko, Bryant, Clifford, Clark, Kimberly A, Minor, Daniel L

“…Polymodal thermo- and mechanosensitive two-pore domain potassium (K2P) channels of the TREK1 subfamily generate 'leak' currents that regulate neuronal…”
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K.sub.2P2.1 -activator complexes reveal a cryptic selectivity filter binding site by Lolicato, Marco, Arrigoni, Cristina, Mori, Takahiro, Sekioka, Yoko, Bryant, Clifford, Clark, Kimberly A, Minor, Daniel L., Jr

“…Crystal structures of an activated two-pore potassium channel reveal a cryptic binding pocket that binds small-molecule activators that restrict the mobility…”
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Hsp90 Inhibitors as New Leads To Target Parasitic Diarrheal Diseases by DEBNATH, Anjan, SHAHINAS, Dea, REED, Sharon L, MCKERROW, James H, BRYANT, Clifford, HIRATA, Ken, MIYAMOTO, Yukiko, HWANG, Grace, GUT, Jiri, RENSLO, Adam R, PILLAI, Dylan R, ECKMANN, Lars

“…Entamoeba histolytica and Giardia lamblia are anaerobic protozoan parasites that cause amebiasis and giardiasis, two of the most common diarrheal diseases…”
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Divergent Modes of Enzyme Inhibition in a Homologous Structure−Activity Series by Ferreira, Rafaela S, Bryant, Clifford, Ang, Kenny K. H, McKerrow, James H, Shoichet, Brian K, Renslo, Adam R

“…A docking screen identified reversible, noncovalent inhibitors (e.g., 1) of the parasite cysteine protease cruzain. Chemical optimization of 1 led to a series…”
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Biaryl amides and hydrazones as therapeutics for prion disease in transgenic mice by Lu, Duo, Giles, Kurt, Li, Zhe, Rao, Satish, Dolghih, Elena, Gever, Joel R, Geva, Michal, Elepano, Manuel L, Oehler, Abby, Bryant, Clifford, Renslo, Adam R, Jacobson, Matthew P, Dearmond, Stephen J, Silber, B Michael, Prusiner, Stanley B

“…The only small-molecule compound demonstrated to substantially extend survival in prion-infected mice is a biaryl hydrazone termed "Compd B"…”
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Tetrafluorophenoxymethyl ketone cruzain inhibitors with improved pharmacokinetic properties as therapeutic leads for Chagas’ disease by Neitz, R. Jeffrey, Bryant, Clifford, Chen, Steven, Gut, Jiri, Hugo Caselli, Estefania, Ponce, Servando, Chowdhury, Somenath, Xu, Haichao, Arkin, Michelle R., Ellman, Jonathan A., Renslo, Adam R.

“…[Display omitted] Inhibition of the cysteine protease cruzain from Trypanosoma cruzi has been studied pre-clinically as a new chemotherapeutic approach to…”
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Lead identification to clinical candidate selection: drugs for Chagas disease by Neitz, R Jeffrey, Chen, Steven, Supek, Frantisek, Yeh, Vince, Kellar, Danielle, Gut, Jiri, Bryant, Clifford, Gallardo-Godoy, Alejandra, Molteni, Valentina, Roach, Steven L, Khare, Shilpi, Stinson, Monique, Chatterjee, Arnab K, Robertson, Stephanie, Renslo, Adam R, Arkin, Michelle, Glynne, Richard, McKerrow, James, Siqueira-Neto, Jair L

“…Chagas disease affects 8 million people worldwide and remains a main cause of death due to heart failure in Latin America. The number of cases in the United…”
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Predicting Binding to P-Glycoprotein by Flexible Receptor Docking: e1002083 by Dolghih, Elena, Bryant, Clifford, Renslo, Adam R, Jacobson, Matthew P

“…P-glycoprotein (P-gp) is an ATP-dependent transport protein that is selectively expressed at entry points of xenobiotics where, acting as an efflux pump, it…”
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Novel non-peptidic vinylsulfones targeting the S2 and S3 subsites of parasite cysteine proteases by Bryant, Clifford, Kerr, Iain D., Debnath, Moumita, Ang, Kenny K.H., Ratnam, Joseline, Ferreira, Rafaela S., Jaishankar, Priyadarshini, Zhao, DongMei, Arkin, Michelle R., McKerrow, James H., Brinen, Linda S., Renslo, Adam R.

“…We describe here the identification of non-peptidic vinylsulfones that inhibit parasite cysteine proteases in vitro and inhibit the growth of Trypanosoma…”
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