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#2Aaron DeBono (Monash University)H-Index: 8
Last. Ben Capuano (Monash University)H-Index: 14
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The calcium-sensing receptor (CaSR) is a clinical target in the treatment of hyperparathyroidism and related diseases. However, clinical use of approved CaSR-targeting drugs such as cinacalcet ( 1 ) is limited due to adverse side effects including hypocalcaemia, nausea and vomiting, and in some instances, a lack of efficacy. The CaSR agonist and positive allosteric modulator (ago-PAM), AC265347 ( 2 ), is chemically distinct from clinically-approved CaSR PAMs. AC265347 potently suppressed parathy...
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#1Francesca Ferlenghi (University of Parma)H-Index: 6
#2Michele Mari (University of Urbino)H-Index: 12
Last. Fabiola Fanini (University of Urbino)H-Index: 1
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The N-(anilinoethyl)amide derivative UCM765, is an MT 2 -selective partial agonist with hypnotic, analgesic and anxiolytic properties in rodents, but suffers from low water solubility and modest metabolic stability. To overcome these limitations, different strategies were investigated, including modification of metabolically liable sites, introduction of hydrophilic substituents and design of more basic derivatives. Thermodynamic solubility, microsomal stability and lipophilicity of new compound...
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#1Kelvin K. H. Tong (University of Auckland)H-Index: 6
#2Muhammad Hanif (University of Auckland)H-Index: 50
Last. Hugh H. Harris (University of Adelaide)H-Index: 34
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We report investigations on the anticancer activity of organometallic [M II/III (η 6 - p -cymene/η 5 -pentamethylcyclopentadienyl)] (M = Ru, Os, Rh, and Ir) complexes of N -heterocyclic carbenes (NHCs) substituted with a triazolyl moiety. Depending on the precursors, the NHC ligands displayed either mono- or bidentate coordination via the NHC carbon atom or as N , C -donors. The metal complexes were investigated for their stability in aqueous solution, with the interpretation supported by densit...
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#1Ludvik Olai Espeland (University of Bergen)
#2Charis Georgiou (University of Bergen)
Last. Brenk R
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FabF (3-oxoacyl-[acyl-carrier-protein] synthase 2), which catalyses the rate limiting condensation reaction in the fatty acid synthesis II pathway, is an attractive target for new antibiotics. Here, we focus on FabF from P. aeruginosa ( Pa FabF) as antibiotics against this pathogen are urgently needed. To facilitate exploration of this target we have set up an experimental toolbox consisting of binding assays using bio-layer interferometry as well as saturation transfer difference (STD) and Wate...
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#1Mikhail Krasavin (SPbU: Saint Petersburg State University)H-Index: 24
#2Daniil Zhukovsky (SPbU: Saint Petersburg State University)H-Index: 5
Last. Marco Rotter (Goethe University Frankfurt)H-Index: 1
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Diversity-oriented synthesis (DOS) is a rich source for novel lead structures in Medicinal Chemistry. In this study, we present a DOS-compatible method for synthesis of compounds bearing a free thiol moiety. The procedure relies on Rh(II)-catalyzed coupling of dithiols to diazo building blocks. The synthetizes library was probed against metallo-β-lactamases (MBLs) NDM-1 and VIM-1. Biochemical and biological evaluation led to identification of novel potent MBL inhibitors with antibiotic adjuvant ...
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#1Parichita Chakraborty (UG: University of Groningen)H-Index: 2
#2Dorenda Oosterhuis (UG: University of Groningen)H-Index: 11
Last. Dirk-Jan Scheffers (UG: University of Groningen)H-Index: 21
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The rise of antimicrobial resistance has necessitated novel strategies to efficiently combat pathogenic bacteria. Metal-based compounds have been proven as a possible alternative to classical organic drugs. Here, we have assessed the antibacterial activity of seven gold complexes of different families. One compound, a cyclometalated Au(III) C^N complex, showed activity against Gram-positive bacteria, including multi-drug resistant clinical strains. The mechanism of action of this compound was st...
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#1Thomas Ackermann (LMU: Ludwig Maximilian University of Munich)H-Index: 5
#2Georg Höfner (LMU: Ludwig Maximilian University of Munich)H-Index: 21
Last. Klaus Theodor Wanner (LMU: Ludwig Maximilian University of Munich)H-Index: 11
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A straight-forward screening of a compound library comprising 2439 substances for the identification of new inhibitors for the neurotransmitter transporters GlyT1 and GlyT2 is described. Screening and full-scale competition experiments were performed using recently developed GlyT1 and GlyT2 MS Binding Assays. That way for both targets, GlyT1 and GlyT2, ligands were identified, which exhibited affinities (pKi values) in the low micromolar to sub-micromolar range. The majority of these binders exh...
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#1Nicholas Cedraro (Marche Polytechnic University)H-Index: 3
#2Rolando Cannalire (University of Perugia)H-Index: 11
Last. Stefano Sabatini (University of Perugia)H-Index: 25
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Antibiotic resistance breakers, such as efflux pump inhibitors (EPIs), represent a powerful alternative to the development of new antimicrobials. Recently, by using previously described EPIs, we developed pharmacophore models able to identify inhibitors of NorA, the most studied efflux pump of the Staphylococcus aureus. Herein, we reported a pharmacophore-based virtual screening of a library of new potential NorA EPIs generated by an in-silico scaffold hopping approach of the quinoline core. Aft...
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#1Natalia Milosevich (UVic: University of Victoria)H-Index: 5
#2Chelsea R. Wilson (UVic: University of Victoria)H-Index: 1
Last. Emily C. Dykhuizen (Purdue University)H-Index: 15
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Methyllysine reader proteins bind to methylated lysine residues and alter gene transcription by changing the compaction state of chromatin or by the recruitment of other multiprotein complexes. The polycomb paralog family of methyllysine readers bind to trimethylated lysine on the tail of histone 3 via a highly conserved aromatic cage located in their chromodomains. Each of the polycomb paralogs are implicated in several disease states. CBX6 and CBX8 are members of the polycomb paralog family wi...
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#1Shaymaa E. Kassab (Damanhour University)H-Index: 3
#2Samar Mowafy (UW: University of Washington)
hIDO1 is a heme-dioxygenase enzyme, over-expressed in the tumor micro-environment and implicated in the survival of cancer cells. Metabolism of tryptophan to N -formyl-kynurenine by hIDO1 leads to immune suppression to result in cancer cell immune escape. In this article, we discuss the discovery of selective hIDO1 inhibitors for therapeutic intervention, which was promoted to clinical trials and associated with the complex crystal structure of the enzyme with the respective inhibitor. The struc...
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