Results 11 to 20 of about 9,059 (164)
Frontiers in Chemistry, 2021 Allosteric modulators (AMs) of G-protein coupled receptors (GPCRs) are desirable drug targets because they can produce fewer on-target side effects, improved selectivity, and better biological specificity (e.g., biased signaling or probe dependence) than
Keith M. Olson +4 more
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Brilacidin Demonstrates Inhibition of SARS-CoV-2 in Cell Culture
Viruses, 2021 Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2), the newly emergent causative agent of coronavirus disease-19 (COVID-19), has resulted in more than two million deaths worldwide since it was first detected in 2019.
Allison Bakovic +7 more
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Beilstein Journal of Organic Chemistry, 2023 Peptidomimetics with a substituted imidazo[1,2-a]pyridine fragment were synthesized by a tandem of Groebke–Blackburn–Bienaymé and Ugi reactions. The target products contain substituted imidazo[1,2-a]pyridine and peptidomimetic moieties as pharmacophores ...
Oleksandr V. Kolomiiets +5 more
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QSAR Modelling of Peptidomimetic Derivatives towards HKU4-CoV 3CLpro Inhibitors against MERS-CoV
Chemistry, 2021 In this paper, we report the relationship between the anti-MERS-CoV activities of the HKU4 derived peptides for some peptidomimetic compounds and various descriptors using the quantitative structure activity relationships (QSAR) methods.
Imad Hammoudan +4 more
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1,2,3-Triazoles as Biomimetics in Peptide Science
Molecules, 2021 Natural peptides are an important class of chemical mediators, essential for most vital processes. What limits the potential of the use of peptides as drugs is their low bioavailability and enzymatic degradation in vivo.
Naima Agouram +2 more
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Pharmaceuticals, 2023 Vascular endothelial growth factor receptor 2 (VEGFR2) mediates VEGFA signaling mainly through the PI3K/AKT/mTOR and PLCγ/ERK1/2 pathways. Here we unveil a peptidomimetic (VGB3) based on the interaction between VEGFB and VEGFR1 that unexpectedly binds ...
Mohadeseh Namjoo +8 more
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Discovery of novel spike/ACE2 inhibitory macrocycles using in silico reinforcement learning
Frontiers in Drug Discovery, 2022 Introduction: The COVID-19 pandemic has cast a heavy toll in human lives and global economics. COVID-19 is caused by the SARS-CoV-2 virus, which infects cells via its spike protein binding human ACE2.Methods: To discover potential inhibitory ...
Lev Shapira +9 more
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Molecules, 2021 Peptoids (oligo N-substituted glycines) are peptide analogues, which can be designed to mimic host antimicrobial peptides, with the advantage that they are resistant to proteolytic degradation.
Jamie Toole +5 more
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Molecules, 2014 Our previous studies showed that alteration of dipeptides Y-Fca-Ala-OMe (III) into Y-Ala-Fca-OMe (IV) (Y = Ac, Boc; Fca = 1'-aminoferrocene-1-carboxylic acid) significantly influenced their conformational space.
Monika Kovačević +6 more
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In Search of Small Molecules That Selectively Inhibit MBOAT4
Molecules, 2021 Ghrelin is a 28-residue peptide hormone produced by stomach P/D1 cells located in oxyntic glands of the fundus mucosa. Post-translational octanoylation of its Ser-3 residue, catalyzed by MBOAT4 (aka ghrelin O-acyl transferase (GOAT)), is essential for ...
Emily S. Murzinski +7 more
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