Search Results - "Alboreggia, Giulia"
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Characterization of a Potent and Orally Bioavailable Lys-Covalent Inhibitor of Apoptosis Protein (IAP) Antagonist
Published in Journal of medicinal chemistry (22-06-2023)“…We have recently reported on the use of aryl-fluorosulfates in designing water- and plasma-stable agents that covalently target Lys, Tyr, or His residues in…”
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Conformational switch and multiple supramolecular structures of a newly identified self-assembling protein-mimetic peptide from Pseudomonas aeruginosa YeaZ protein
Published in Frontiers in chemistry (13-12-2022)“…Protein-mimetic peptides (PMPs) are shorter sequences of self-assembling proteins, that represent remarkable building blocks for the generation of bioinspired…”
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Targeted degradation of Pin1 by protein-destabilizing compounds
Published in Proceedings of the National Academy of Sciences - PNAS (19-11-2024)“…The concept of targeted protein degradation is at the forefront of modern drug discovery, which aims to eliminate disease-causing proteins using specific…”
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Lysine Covalent Antagonists of Melanoma Inhibitors of Apoptosis Protein
Published in Journal of medicinal chemistry (11-11-2021)“…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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Abstract 2460 Structure Studies of Suicide Inhibitors Bound to Human Pin1
Published in The Journal of biological chemistry (01-03-2024)Get full text
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Mixture-Based Screening of Focused Combinatorial Libraries by NMR: Application to the Antiapoptotic Protein hMcl‑1
Published in Journal of medicinal chemistry (27-07-2023)“…We report on an innovative ligand discovery strategy based on protein NMR-based screening of a combinatorial library of ∼125,000 compounds that was arranged in…”
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Covalent Targeting of Histidine Residues with Aryl Fluorosulfates: Application to Mcl-1 BH3 Mimetics
Published in Journal of medicinal chemistry (12-11-2024)“…Covalent drugs provide pharmacodynamic and pharmacokinetic advantages over reversible agents. However, covalent strategies have been developed mostly to target…”
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Histidine-Covalent Stapled Alpha-Helical Peptides Targeting hMcl‑1
Published in Journal of medicinal chemistry (23-05-2024)“…Several novel and effective cysteine targeting (Cys) covalent drugs are in clinical use. However, the target area containing a druggable Cys residue is…”
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