Search Results - "Gambini, Luca"

Design, Synthesis, and Structural Characterization of Lysine Covalent BH3 Peptides Targeting Mcl‑1 by Gambini, Luca, Udompholkul, Parima, Baggio, Carlo, Muralidharan, Aruljothi, Kenjić, Nikola, Assar, Zahra, Perry, J. Jefferson P, Pellecchia, Maurizio

“…Modulating disease-relevant protein–protein interactions (PPIs) using pharmacological tools is a critical step toward the design of novel therapeutic…”
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Reduction of Circulating Cancer Cells and Metastases in Breast-Cancer Models by a Potent EphA2-Agonistic Peptide–Drug Conjugate by Salem, Ahmed F, Wang, Si, Billet, Sandrine, Chen, Jie-Fu, Udompholkul, Parima, Gambini, Luca, Baggio, Carlo, Tseng, Hsian-Rong, Posadas, Edwin M, Bhowmick, Neil A, Pellecchia, Maurizio

“…EphA2 overexpression has been associated with metastasis in multiple cancer types, including melanomas and ovarian, prostate, lung, and breast cancers. We have…”
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Potential Therapeutic Targeting of Coronavirus Spike Glycoprotein Priming by Barile, Elisa, Baggio, Carlo, Gambini, Luca, Shiryaev, Sergey A, Strongin, Alex Y, Pellecchia, Maurizio

“…Processing of certain viral proteins and bacterial toxins by host serine proteases is a frequent and critical step in virulence. The coronavirus spike…”
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Effective Tumor Targeting by EphA2-Agonist-Biotin-Streptavidin Conjugates by Udompholkul, Parima, Baggio, Carlo, Gambini, Luca, Sun, Yu, Zhao, Ming, Hoffman, Robert M, Pellecchia, Maurizio

“…We recently reported on a potent synthetic agent, 135H11, that selectively targets the receptor tyrosine kinase, EphA2. While 135H11 possesses a relatively…”
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NMR Fingerprints of the Drug-like Natural-Product Space Identify Iotrochotazine A: A Chemical Probe to Study Parkinson's Disease by Grkovic, Tanja, Pouwer, Rebecca H., Vial, Marie-Laure, Gambini, Luca, Noël, Alba, Hooper, John N. A., Wood, Stephen A., Mellick, George D., Quinn, Ronald J.

“…The NMR spectrum of a mixture of small molecules is a fingerprint of all of its components. Herein, we present an NMR fingerprint method that takes advantage…”
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Therapeutic Targeting of Pancreatic Cancer via EphA2 Dimeric Agonistic Agents by Salem, Ahmed F, Gambini, Luca, Udompholkul, Parima, Baggio, Carlo, Pellecchia, Maurizio

“…Recently, we reported on potent EphA2 targeting compounds and demonstrated that dimeric versions of such agents can exhibit remarkably increased agonistic…”
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Picomolar Inhibition of Plasmepsin V, an Essential Malaria Protease, Achieved Exploiting the Prime Region by Gambini, Luca, Rizzi, Luca, Pedretti, Alessandro, Taglialatela-Scafati, Orazio, Carucci, Mario, Pancotti, Andrea, Galli, Corinna, Read, Martin, Giurisato, Emanuele, Romeo, Sergio, Russo, Ilaria

“…Malaria is an infectious disease caused by Plasmodium parasites. It results in an annual death-toll of ~ 600,000. Resistance to all medications currently in…”
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Correction: Picomolar Inhibition of Plasmepsin V, an Essential Malaria Protease, Achieved Exploiting the Prime Region by Gambini, Luca, Rizzi, Luca, Pedretti, Alessandro, Taglialatela-Scafati, Orazio, Carucci, Mario, Pancotti, Andrea, Galli, Corinna, Read, Martin, Giurisato, Emanuele, Romeo, Sergio, Russo, Ilaria

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Targefrin: A Potent Agent Targeting the Ligand Binding Domain of EphA2 by Baggio, Carlo, Udompholkul, Parima, Gambini, Luca, Pellecchia, Maurizio

“…Overexpression of the receptor tyrosine kinase EphA2 is invariably associated with poor prognosis and development of aggressive metastatic cancers. Guided by…”
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Lysine Covalent Antagonists of Melanoma Inhibitors of Apoptosis Protein by Udompholkul, Parima, Baggio, Carlo, Gambini, Luca, Alboreggia, Giulia, Pellecchia, Maurizio

“…We have recently reported on Lys-covalent agents that, based on aryl-sulfonyl fluorides, were designed to target binding site Lys 311 in the X-linked inhibitor…”
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Covalent Inhibitors of Protein–Protein Interactions Targeting Lysine, Tyrosine, or Histidine Residues by Gambini, Luca, Baggio, Carlo, Udompholkul, Parima, Jossart, Jennifer, Salem, Ahmed F, Perry, J. Jefferson P, Pellecchia, Maurizio

“…We have recently reported a series of Lys-covalent agents targeting the BIR3 domain of the X-linked inhibitor of apoptosis protein (XIAP) using a…”
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Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy by Baggio, Carlo, Udompholkul, Parima, Gambini, Luca, Salem, Ahmed F, Jossart, Jennifer, Perry, J. Jefferson P, Pellecchia, Maurizio

“…We have recently investigated the reactivity of aryl-fluorosulfates as warheads to form covalent adducts with Lys, Tyr, and His residues. However, the rate of…”
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Design of Potent pan-IAP and Lys-Covalent XIAP Selective Inhibitors Using a Thermodynamics Driven Approach by Baggio, Carlo, Gambini, Luca, Udompholkul, Parima, Salem, Ahmed F, Aronson, Alexander, Dona, Ada, Troadec, Estelle, Pichiorri, Flavia, Pellecchia, Maurizio

“…Recently we reported that rapid determination of enthalpy of binding can be achieved for a large number of congeneric agents or in combinatorial libraries…”
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Stability and Cell Permeability of Sulfonyl Fluorides in the Design of Lys‐Covalent Antagonists of Protein‐Protein Interactions by Gambini, Luca, Udompholkul, Parima, Salem, Ahmed F., Baggio, Carlo, Pellecchia, Maurizio

“…Recently we reported on aryl‐fluorosulfates as possible stable and effective electrophiles for the design of lysine covalent, cell permeable antagonists of…”
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Human resistin protects against endotoxic shock by blocking LPS–TLR4 interaction by Jang, Jessica C., Li, Jiang, Gambini, Luca, Batugedara, Hashini M., Sati, Sandeep, Lazar, Mitchell A., Fan, Li, Pellecchia, Maurizio, Nair, Meera G.

“…Helminths trigger multiple immunomodulatory pathways that can protect from sepsis. Human resistin (hRetn) is an immune cell-derived protein that is highly…”
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Abstract 3911: Targeting the EphA2-ligand binding domain for the design of innovative cancer therapeutics by Udompholkul, Parima, Gambini, Luca, Salem, Ahmed F., Baggio, Carlo, Pellecchia, Maurizio

“…Abstract Eph receptors are the largest family of receptor tyrosine kinases, and are involved in regulating several cellular processes, including cell…”
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Aryl-fluorosulfate-based Lysine Covalent pan-Inhibitors of Apoptosis Proteins (IAP) Antagonists with Cellular Efficacy by Baggio, Carlo, Udompholkul, Parima, Gambini, Luca, Salem, Ahmed F., Jossart, Jennifer, Perry, J. Jefferson P., Pellecchia, Maurizio

“…We have recently investigated the reactivity of aryl-fluorosulfates as warheads to form covalent adducts with Lys, Tyr, and His residues. However, the rate of…”
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Structure-Based Design of Novel EphA2 Agonistic Agents with Nanomolar Affinity in Vitro and in Cell by Gambini, Luca, Salem, Ahmed F, Udompholkul, Parima, Tan, Xiao-Feng, Baggio, Carlo, Shah, Neh, Aronson, Alexander, Song, Jikui, Pellecchia, Maurizio

“…EphA2 overexpression is invariably associated with poor prognosis and development of aggressive metastatic cancers in pancreatic, prostate, lung, ovarian, and…”
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Theranostic Nanocages for Imaging and Photothermal Therapy of Prostate Cancer Cells by Active Targeting of Neuropeptide‑Y Receptor by Avvakumova, Svetlana, Galbiati, Elisabetta, Sironi, Laura, Locarno, Silvia A, Gambini, Luca, Macchi, Chiara, Pandolfi, Laura, Ruscica, Massimiliano, Magni, Paolo, Collini, Maddalena, Colombo, Miriam, Corsi, Fabio, Chirico, Giuseppe, Romeo, Sergio, Prosperi, Davide

“…Gold nanocages (AuNCs) have been shown to be a useful tool for harnessing imaging and hyperthermia therapy of cancer, thanks to their unique optical…”
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N‐locking stabilization of covalent helical peptides: Application to Bfl‐1 antagonists by Baggio, Carlo, Udompholkul, Parima, Gambini, Luca, Jossart, Jennifer, Salem, Ahmed F., Håkansson, Maria, Perry, J. Jefferson P., Pellecchia, Maurizio

“…Recently, it was reported that tetrapeptides cyclized via lactam bond between the amino terminus and a glutamic residue in position 4 (termed here N‐lock) can…”
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