Search Results - "Kurkin, Alexander V"

Stress promotes RNA G-quadruplex folding in human cells by Kharel, Prakash, Fay, Marta, Manasova, Ekaterina V., Anderson, Paul J., Kurkin, Alexander V., Guo, Junjie U., Ivanov, Pavel

“…Guanine (G)-rich nucleic acids can fold into G-quadruplex (G4) structures under permissive conditions. Although many RNAs contain sequences that fold into RNA…”
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Discovery of the 4-aminopiperidine-based compound EM127 for the site-specific covalent inhibition of SMYD3 by Parenti, Marco Daniele, Naldi, Marina, Manoni, Elisabetta, Fabini, Edoardo, Cederfelt, Daniela, Talibov, Vladimir O., Gressani, Valeria, Guven, Ummu, Grossi, Valentina, Fasano, Candida, Sanese, Paola, De Marco, Katia, Shtil, Alexander A., Kurkin, Alexander V., Altieri, Andrea, Danielson, U. Helena, Caretti, Giuseppina, Simone, Cristiano, Varchi, Greta, Bartolini, Manuela, Del Rio, Alberto

“…Recent findings support the hypothesis that inhibition of SMYD3 methyltransferase may be a therapeutic avenue for some of the deadliest cancer types. Herein,…”
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Antiviral Activity and Crystal Structures of HIV-1 gp120 Antagonists by Curreli, Francesca, Kwon, Young D, Nicolau, Isabella, Burgos, Giancarla, Altieri, Andrea, Kurkin, Alexander V, Verardi, Raffaello, Kwong, Peter D, Debnath, Asim K

“…As part of our effort to discover drugs that target HIV-1 entry, we report the antiviral activity and crystal structures of two novel inhibitors in a complex…”
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Design and Characterization of Novel Small Molecule Activators of Excitatory Amino Acid Transporter 2 by Das, Sanjay, Trubnikov, Artem V., Novoselov, Anton M., Kurkin, Alexander V., Beld, Joris, Altieri, Andrea, Kortagere, Sandhya

“…Excitotoxicity in the brain is a causal factor in several neurological and neurodegenerative disorders. Excitatory amino acid transporter 2 (EAAT2), an…”
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Comparative Pharmacokinetics of a Dual Inhibitor of HIV-1, NBD-14189, in Rats and Dogs with a Proof-of-Concept Evaluation of Antiviral Potency in SCID-hu Mouse Model by Stoddart, Cheryl A, Curreli, Francesca, Horrigan, Stephen, Altieri, Andrea, Kurkin, Alexander V, Debnath, Asim K

“…We earlier reported substantial progress in designing gp120 antagonists. Notably, we discovered that NBD-14189 is not only the most active gp120 antagonist but…”
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In Vitro and In Vivo Pharmacological Characterization of a Novel TRPM8 Inhibitor Chemotype Identified by Small-Scale Preclinical Screening by Iraci, Nunzio, Ostacolo, Carmine, Medina-Peris, Alicia, Ciaglia, Tania, Novoselov, Anton M, Altieri, Andrea, Cabañero, David, Fernandez-Carvajal, Asia, Campiglia, Pietro, Gomez-Monterrey, Isabel, Bertamino, Alessia, Kurkin, Alexander V

“…Transient receptor potential melastatin type 8 (TRPM8) is a target for the treatment of different physio-pathological processes. While TRPM8 antagonists are…”
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Generation, optimization and characterization of novel anti-prion compounds by Altieri, Andrea, Spiridonov, Evgeny A., Sivtzev, Semen I., Ishibashi, Daisuke, Biggi, Silvia, Nishida, Noriyuki, Biasini, Emiliano, Kurkin, Alexander V.

“…[Display omitted] Prions are misfolded proteins involved in neurodegenerative diseases of high interest in veterinary and public health. In this work, we…”
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Oxidative Dearomatization of 4,5,6,7-Tetrahydro-1H-indoles Obtained by Metal- and Solvent-Free Thermal 5-endo-dig Cyclization: The Route to Erythrina and Lycorine Alkaloids by Andreev, Ivan A., Ratmanova, Nina K., Novoselov, Anton M., Belov, Dmitry S., Seregina, Irina F., Kurkin, Alexander V.

“…A facile one‐pot approach based on a thermally induced metal‐ and solvent‐free 5‐endo‐dig cyclization reaction of the amino propargylic alcohols in combination…”
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Design, synthesis and evaluation of small molecule CD4-mimics as entry inhibitors possessing broad spectrum anti-HIV-1 activity by Curreli, Francesca, Belov, Dmitry S, Ramesh, Ranjith R, Patel, Naisargi, Altieri, Andrea, Kurkin, Alexander V, Debnath, Asim K

“…Since our first discovery of a CD4-mimic, NBD-556, which targets the Phe43 cavity of HIV-1 gp120, we and other groups made considerable progress in designing…”
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Structure-Based Identification and Biological Characterization of New NAPRT Inhibitors by Franco, Jorge, Piacente, Francesco, Walter, Melanie, Fratta, Simone, Ghanem, Moustafa, Benzi, Andrea, Caffa, Irene, Kurkin, Alexander V., Altieri, Andrea, Herr, Patrick, Martínez-Bailén, Macarena, Robina, Inmaculada, Bruzzone, Santina, Nencioni, Alessio, Del Rio, Alberto

“…NAPRT, the rate-limiting enzyme of the Preiss–Handler NAD biosynthetic pathway, has emerged as a key biomarker for the clinical success of NAMPT inhibitors in…”
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Synthesis of Substituted Pyrrole Derivatives Based on 8-Azaspiro[5.6]dodec-10-ene Scaffold by Iusupov, Ildar R, Tafeenko, Victor A, Altieri, Andrea, Kurkin, Alexander V

“…This work describes the synthesis of spirocyclic compounds based on 8-azaspiro[5.6]dodec-10-ene. Diastereomerically pure pyrrole derivatives were prepared from…”
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Synthesis of Bicyclic Proline Derivatives by the Aza-Cope-Mannich Reaction: Formal Synthesis of (±)-Acetylaranotin by Belov, Dmitry S., Ratmanova, Nina K., Andreev, Ivan A., Kurkin, Alexander V.

“…Herein we suggest an approach to oxygenated bicyclic amino acids based on an aza‐Cope–Mannich rearrangement. Seven distinct amino acid scaffolds analogous to…”
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(1RS,2RS,6RS)-2-(6-Amino-9H-purin-9-yl)-8-azaspiro[5.6]dodec-10-en-1-ol Dihydrochloride by Iusupov, Ildar R., Lyssenko, Konstantin A., Altieri, Andrea, Kurkin, Alexander V.

“…The title compound (1RS,2RS,6RS)-2-(6-Amino-9H-purin-9-yl)-8-azaspiro[5.6]dodec-10-en-1-ol dihydrochloride was synthesized for the first time in two steps, the…”
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Discovery of Highly Potent Fusion Inhibitors with Potential Pan-Coronavirus Activity That Effectively Inhibit Major COVID-19 Variants of Concern (VOCs) in Pseudovirus-Based Assays by Curreli, Francesca, Ahmed, Shahad, Victor, Sofia M B, Drelich, Aleksandra, Panda, Siva S, Altieri, Andrea, Kurkin, Alexander V, Tseng, Chien-Te K, Hillyer, Christopher D, Debnath, Asim K

“…We report the discovery of several highly potent small molecules with low-nM potency against severe acute respiratory syndrome coronavirus (SARS-CoV; lowest…”
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Highly Stereoselective and Scalable Synthesis of trans-Fused Octahydrocyclohepta[b]pyrrol-4(1H)‑ones via the Aza-Cope–Mannich Rearrangement in Racemic and Enantiopure Forms by Belov, Dmitry S, Lukyanenko, Evgeny R, Kurkin, Alexander V, Yurovskaya, Marina A

“…We have developed an efficient and stereoselective route to trans-fused octahydrocyclohepta[b]pyrrol-4(1H)-ones. The key features of our synthesis include the…”
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The Antioxidant Cofactor Alpha-Lipoic Acid May Control Endogenous Formaldehyde Metabolism in Mammals by Shindyapina, Anastasia V, Komarova, Tatiana V, Sheshukova, Ekaterina V, Ershova, Natalia M, Tashlitsky, Vadim N, Kurkin, Alexander V, Yusupov, Ildar R, Mkrtchyan, Garik V, Shagidulin, Murat Y, Dorokhov, Yuri L

“…The healthy human body contains small amounts of metabolic formaldehyde (FA) that mainly results from methanol oxidation by pectin methylesterase, which is…”
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A Small‐Molecule Inhibitor of Prion Replication and Mutant Prion Protein Toxicity by Massignan, Tania, Sangiovanni, Valeria, Biggi, Silvia, Stincardini, Claudia, Elezgarai, Saioa R., Maietta, Giulia, Andreev, Ivan A., Ratmanova, Nina K., Belov, Dmitry S., Lukyanenko, Evgeny R., Belov, Grigory M., Barreca, Maria Letizia, Altieri, Andrea, Kurkin, Alexander V., Biasini, Emiliano

“…Into the fold: Prion diseases are neurodegenerative disorders characterized by the accumulation in the brain of a self‐replicating, misfolded isoform (PrPSc)…”
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Synthesis, Antiviral Potency, in Vitro ADMET, and X‑ray Structure of Potent CD4 Mimics as Entry Inhibitors That Target the Phe43 Cavity of HIV‑1 gp120 by Curreli, Francesca, Kwon, Young Do, Belov, Dmitry S, Ramesh, Ranjith R, Kurkin, Alexander V, Altieri, Andrea, Kwong, Peter D, Debnath, Asim K

“…In our attempt to optimize the lead HIV-1 entry antagonist, NBD-11021, we present in this study the rational design and synthesis of 60 new analogues and…”
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Preclinical Optimization of gp120 Entry Antagonists as anti-HIV‑1 Agents with Improved Cytotoxicity and ADME Properties through Rational Design, Synthesis, and Antiviral Evaluation by Curreli, Francesca, Ahmed, Shahad, Benedict Victor, Sofia M, Iusupov, Ildar R, Belov, Dmitry S, Markov, Pavel O, Kurkin, Alexander V, Altieri, Andrea, Debnath, Asim K

“…We previously reported a milestone in the optimization of NBD-11021, an HIV-1 gp120 antagonist, by developing a new and novel analogue, NBD-14189 (Ref1), which…”
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Design and Synthesis of Fsp3‐Enriched Spirocyclic‐Based Biological Screening Compound Arrays via DOS Strategies and Their NNMT Inhibition Profiling by Iusupov, Ildar R., Lukyanenko, Evgeny R., Altieri, Andrea, Kurkin, Alexander V.

“…Medicinal chemists are keen to explore tridimensional compounds, especially when it comes to small molecules. It has already been stressed that the majority of…”
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