Search Results - "Mark A. Jarosinski"
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Structural principles of insulin formulation and analog design: A century of innovation
Published in Molecular metabolism (Germany) (01-10-2021)“…The discovery of insulin in 1921 and its near-immediate clinical use initiated a century of innovation. Advances extended across a broad front, from the…”
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Peptide Model of the Mutant Proinsulin Syndrome. I. Design and Clinical Correlation
Published in Frontiers in endocrinology (Lausanne) (01-03-2022)“…The mutant proinsulin syndrome is a monogenic cause of diabetes mellitus due to toxic misfolding of insulin's biosynthetic precursor. Also designated (MIDY),…”
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‘Smart’ insulin-delivery technologies and intrinsic glucose-responsive insulin analogues
Published in Diabetologia (01-05-2021)“…Insulin replacement therapy for diabetes mellitus seeks to minimise excursions in blood glucose concentration above or below the therapeutic range (hyper- or…”
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New Horizons: Next-Generation Insulin Analogues: Structural Principles and Clinical Goals
Published in The journal of clinical endocrinology and metabolism (24-03-2022)“…Design of "first-generation" insulin analogues over the past 3 decades has provided pharmaceutical formulations with tailored pharmacokinetic (PK) and…”
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Insertion of a synthetic switch into insulin provides metabolite-dependent regulation of hormone–receptor activation
Published in Proceedings of the National Academy of Sciences - PNAS (27-07-2021)“…Insulin-signaling requires conformational change: whereas the free hormone and its receptor each adopt autoinhibited conformations, their binding leads to…”
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Proteinase-activated receptor-2 mediates hyperresponsiveness in isolated guinea pig bronchi
Published in Biochemical pharmacology (01-08-2003)“…The mast cell serine protease tryptase has been implicated as a critical mediator of airway hyperresponsiveness in vitro and in vivo. We have previously…”
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β-Secretase Cleavage of Alzheimer's Amyloid Precursor Protein by the Transmembrane Aspartic Protease BACE
Published in Science (American Association for the Advancement of Science) (22-10-1999)“…Cerebral deposition of amyloid β peptide (Aβ) is an early and critical feature of Alzheimer's disease. Aβ generation depends on proteolytic cleavage of the…”
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Structure of a human DNA repair protein UBA domain that interacts with HIV-1 Vpr
Published in Nature structural biology (01-12-1998)“…The HIV-1 protein Vpr is critical for a number of viral functions including a unique ability to arrest T-cells at a G2/M checkpoint and induce subsequent…”
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Synthesis, chemical reactivity, and antitumor evaluation of congeners of carmethizole hydrochloride, an experimental acylated vinylogous carbinolamine tumor inhibitor
Published in Journal of medicinal chemistry (12-11-1993)“…A series of analogues of 4,5-bis(((N-methylcarbamoyl)oxy)methyl)-1-methyl-2-(methylthio)-im idazole (1, carmethizole) were synthesized. The chemical…”
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Lanthionine macrocyclization by in situ activation of serine
Published in The journal of peptide research (01-06-1998)“…The present report details a straightforward, solid‐phase approach to cyclolanthionine peptides. After stepwise assembly of the linear sequence and…”
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Synthesis of 3-pyrrolines by an intramolecular Wittig reaction
Published in Journal of organic chemistry (01-10-1991)Get full text
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Parkinson's Disease-associated α-Synuclein Is More Fibrillogenic than β- and γ-Synuclein and Cannot Cross-seed Its Homologs
Published in The Journal of biological chemistry (03-11-2000)“…Parkinson's disease (PD) is a neurodegenerative disorder that is pathologically characterized by the presence of intracytoplasmic Lewy bodies. Recently, two…”
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Enhanced resolution in MAS NMR for combinatorial chemistry
Published in Tetrahedron letters (24-02-1997)“…We have demonstrated the ability to obtain high resolution NMR spectra from samples on resin using J-resolved 2D NMR. Projection of the non-tilted spectrum…”
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Design of a new peptidomimetic agonist for the melanocortin receptors based on the solution structure of the peptide ligand, Ac-Nle-cyclo[Asp-Pro-DPhe-Arg-Trp-Lys]-NH(2)
Published in Bioorganic & medicinal chemistry letters (21-07-2003)“…The solution structure of a potent melanocortin receptor agonist, Ac-Nle-cyclo[Asp-Pro-DPhe-Arg-Trp-Lys]-NH(2) (1) was calculated using distance restraints…”
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Design of a new peptidomimetic agonist for the melanocortin receptors based on the solution structure of the peptide ligand, Ac-Nle-cyclo[Asp-Pro- dPhe-Arg-Trp-Lys]-NH 2
Published in Bioorganic & medicinal chemistry letters (2003)“…The solution structure of a potent melanocortin receptor agonist, Ac-Nle-cyclo[Asp-Pro- dPhe-Arg-Trp-Lys]-NH 2 ( 1) was calculated using distance restraints…”
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Parkinson's Disease-associated α-Synuclein Is More Fibrillogenic than β- and γ-Synuclein and Cannot Cross-seed Its Homologs
Published in The Journal of biological chemistry (03-11-2000)“…Parkinson's disease (PD) is a neurodegenerative disorder that is pathologically characterized by the presence of intracytoplasmic Lewy bodies. Recently, two…”
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[Beta]-Secretase Cleavage of Alzheimer's Amyloid Precursor Protein by the Transmembrane Aspartic Protease BACE
Published in Science (American Association for the Advancement of Science) (22-10-1999)“…Cerebral deposition of amyloid [Beta] peptide (A[Beta]) is an early and critical feature of Alzheimer's disease. A[Beta] generation depends on proteolytic…”
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