Search Results - "Cisneros, José A"

A Fluorescence Polarization Assay for Binding to Macrophage Migration Inhibitory Factor and Crystal Structures for Complexes of Two Potent Inhibitors by Cisneros, José A, Robertson, Michael J, Valhondo, Margarita, Jorgensen, William L

“…Human macrophage migration inhibitory factor (MIF) is both a keto–enol tautomerase and a cytokine associated with numerous inflammatory diseases and cancer…”
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Design, Synthesis, and Protein Crystallography of Biaryltriazoles as Potent Tautomerase Inhibitors of Macrophage Migration Inhibitory Factor by Dziedzic, Pawel, Cisneros, José A, Robertson, Michael J, Hare, Alissa A, Danford, Nadia E, Baxter, Richard H. G, Jorgensen, William L

“…Optimization is reported for biaryltriazoles as inhibitors of the tautomerase activity of human macrophage migration inhibitory factor (MIF), a proinflammatory…”
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Irregularities in enzyme assays: The case of macrophage migration inhibitory factor by Cisneros, José A., Robertson, Michael J., Valhondo, Margarita, Jorgensen, William L.

“…[Display omitted] Inhibitors of human macrophage migration inhibitory factor (MIF) previously reported in the literature have been reexamined by synthesis,…”
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Covalent Inhibition of Wild-Type HIV‑1 Reverse Transcriptase Using a Fluorosulfate Warhead by Ippolito, Joseph A, Niu, Haichan, Bertoletti, Nicole, Carter, Zachary J, Jin, Shengyan, Spasov, Krasimir A, Cisneros, José A, Valhondo, Margarita, Cutrona, Kara J, Anderson, Karen S, Jorgensen, William L

“…Covalent inhibitors of wild-type HIV-1 reverse transcriptase (CRTIs) are reported. Three compounds derived from catechol diether non-nucleoside inhibitors…”
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Crystal Structures of HIV‑1 Reverse Transcriptase with Picomolar Inhibitors Reveal Key Interactions for Drug Design by Frey, Kathleen M, Bollini, Mariela, Mislak, Andrea C, Cisneros, José A, Gallardo-Macias, Ricardo, Jorgensen, William L, Anderson, Karen S

“…X-ray crystal structures at 2.9 Å resolution are reported for two complexes of catechol diethers with HIV-1 reverse transcriptase. The results help elucidate…”
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Systematic Study of Effects of Structural Modifications on the Aqueous Solubility of Drug-like Molecules by Cisneros, José A, Robertson, Michael J, Mercado, Brandon Q, Jorgensen, William L

“…Aqueous solubilities and activities have been measured for 17 members of the quinolinyltriazole series of inhibitors of human macrophage migration inhibitory…”
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JAK2 JH2 Fluorescence Polarization Assay and Crystal Structures for Complexes with Three Small Molecules by Newton, Ana S, Deiana, Luca, Puleo, David E, Cisneros, José A, Cutrona, Kara J, Schlessinger, Joseph, Jorgensen, William L

“…A competitive fluorescence polarization (FP) assay is reported for determining binding affinities of probe molecules with the pseudokinase JAK2 JH2 allosteric…”
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Optimization of Pyrazoles as Phenol Surrogates to Yield Potent Inhibitors of Macrophage Migration Inhibitory Factor by Trivedi‐Parmar, Vinay, Robertson, Michael J., Cisneros, José A., Krimmer, Stefan G., Jorgensen, William L.

“…Macrophage migration inhibitory factor (MIF) is a proinflammatory cytokine that is implicated in the regulation of inflammation, cell proliferation, and…”
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Adding a Hydrogen Bond May Not Help: Naphthyridinone vs Quinoline Inhibitors of Macrophage Migration Inhibitory Factor by Dawson, Thomas K, Dziedzic, Pawel, Robertson, Michael J, Cisneros, José A, Krimmer, Stefan G, Newton, Ana S, Tirado-Rives, Julian, Jorgensen, William L

“…Coordination of the ammonium group of Lys32 in the active site of human macrophage migration inhibitory factor (MIF) using a 1,7-naphthyridin-8-one instead of…”
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Efficient ordering of the Hadamard basis for single pixel imaging by López-García, Lourdes, Cruz-Santos, William, García-Arellano, Anmi, Filio-Aguilar, Pedro, Cisneros-Martínez, José A, Ramos-García, Rubén

“…Single-pixel imaging is a technique that can reconstruct an image of a scene by projecting a series of spatial patterns on an object and capturing the…”
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The medicinal chemistry of agents targeting monoacylglycerol lipase by Viso, Alma, Cisneros, José A, Ortega-Gutiérrez, Silvia

“…Monoacylglycerol lipase (MAGL) has been recently proposed as the main enzymatic activity responsible for the in vivo hydrolysis of the most abundant…”
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Covalent inhibitors for eradication of drug-resistant HIV-1 reverse transcriptase: From design to protein crystallography by Chan, Albert H., Lee, Won-Gil, Spasov, Krasimir A., Cisneros, José A., Kudalkar, Shalley N., Petrova, Zaritza O., Buckingham, Amanda B., Anderson, Karen S., Jorgensen, William L.

“…Development of resistance remains a major challenge for drugs to treat HIV-1 infections, including those targeting the essential viral polymerase, HIV-1…”
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From in silico hit to long-acting late-stage preclinical candidate to combat HIV-1 infection by Kudalkar, Shalley N., Beloor, Jagadish, Quijano, Elias, Spasov, Krasimir A., Lee, Won-Gil, Cisneros, José A., Saltzman, W. Mark, Kumar, Priti, Jorgensen, William L., Anderson, Karen S.

“…The HIV-1 pandemic affecting over 37 million people worldwide continues, with nearly one-half of the infected population on highly active antiretroviral…”
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Alkylamine-tethered molecules recruit FBXO22 for targeted protein degradation by Kagiou, Chrysanthi, Cisneros, Jose A., Farnung, Jakob, Liwocha, Joanna, Offensperger, Fabian, Dong, Kevin, Yang, Ka, Tin, Gary, Horstmann, Christina S., Hinterndorfer, Matthias, Paulo, Joao A., Scholes, Natalie S., Sanchez Avila, Juan, Fellner, Michaela, Andersch, Florian, Hannich, J. Thomas, Zuber, Johannes, Kubicek, Stefan, Gygi, Steven P., Schulman, Brenda A., Winter, Georg E.

“…Targeted protein degradation (TPD) relies on small molecules to recruit proteins to E3 ligases to induce their ubiquitylation and degradation by the…”
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Structural and pharmacological evaluation of a novel non-nucleoside reverse transcriptase inhibitor as a promising long acting nanoformulation for treating HIV by Kudalkar, Shalley N., Ullah, Irfan, Bertoletti, Nicole, Mandl, Hanna K., Cisneros, José A., Beloor, Jagadish, Chan, Albert H., Quijano, Elias, Saltzman, W. Mark, Jorgensen, William L., Kumar, Priti, Anderson, Karen S.

“…Combination antiretroviral therapy (cART) has been proven effective in inhibiting human immunodeficiency virus type 1 (HIV-1) infection and has significantly…”
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Reply to Pandey et al.: Understanding the efficacy of a potential antiretroviral drug candidate in humanized mouse model of HIV infection by Kudalkar, Shalley N, Beloor, Jagadish, Quijano, Elias, Spasov, Krasimir A, Lee, Won-Gil, Cisneros, José A, Saltzman, W Mark, Kumar, Priti, Jorgensen, William L, Anderson, Karen S

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Extension into the entrance channel of HIV-1 reverse transcriptase—Crystallography and enhanced solubility by Bollini, Mariela, Frey, Kathleen M., Cisneros, José A., Spasov, Krasimir A., Das, Kalyan, Bauman, Joseph D., Arnold, Eddy, Anderson, Karen S., Jorgensen, William L.

“…Non-nucleoside inhibitors of HIV-1 reverse transcriptase (HIV-RT) are reported that feature extension into the entrance channel near Glu138. Complexes of the…”
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Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility by Bollini, Mariela, Cisneros, José A., Spasov, Krasimir A., Anderson, Karen S., Jorgensen, William L.

“…Non-nucleoside inhibitors of HIV-1 reverse transcriptase are reported that have ca. 100-fold greater solubility than the structurally related drugs etravirine…”
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Structure–Activity Relationship of a New Series of Reversible Dual Monoacylglycerol Lipase/Fatty Acid Amide Hydrolase Inhibitors by Cisneros, José A, Björklund, Emmelie, González-Gil, Inés, Hu, Yanling, Canales, Ángeles, Medrano, Francisco J, Romero, Antonio, Ortega-Gutiérrez, Silvia, Fowler, Christopher J, López-Rodríguez, María L

“…The two endocannabinoids, anandamide (AEA) and 2-arachidonoylglycerol (2-AG), play independent and nonredundant roles in the body. This makes the development…”
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Secondary Attack Rate of Hepatitis C Virus (HCV) by Cisneros-Rodríguez, José A., Moreno-Miceli, Miguel E. Manuel, Cano-Contreras, Ana D., De La Paz-Ibarra, Bertha R., Carrillo-Navarro, Jessica C., Sánchez Hernández, Judith A., Franco-Rico, José A.

“…The transmission routes of Hepatitis C Virus (HCV) are categorized as horizontal and vertical. The former includes sexual contact, parenteral exposure, and…”
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