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Peptides in BioNMR Research
Get PDFHeteronuclear NMR in combination with isotope labelling is used to study folding of polypeptides induced by metals in the case of metallothioneins, binding of the peptidic allosteric modulator ?-TIA to the human G-protein coupled ?1b adrenergic receptor, the development
of therapeutic drugs that interfere with the biosynthesis of the outer membrane of Gram-negative bacteria, and a system in which protein assembly is induced upon peptide addition. NMR in these cases is used to derive precise structural data and to study the dynamics
Development of the Commercial Manufacturing Process for Ipatasertib
Get PDFIpatasertib is a potent small molecule Akt kinase inhibitor currently tested in Phase III clinical trials for the treatment of metastatic castration-resistant prostate cancer and triple negative metastatic breast cancer. In this paper an overview of the development achievements towards the commercial manufacturing process is given. The convergent synthesis consists of ten steps with eight isolated intermediates and utilizes a wide range of chemical techniques and technologies to build-up this complex drug. All three stereocenters are introduced using enzyme or metal catalysis
Towards the Development of Orally Available Peptide Therapeutics
Get PDFPeptides have a number of attractive properties that make them an interesting modality for drug development, including their ability to bind challenging targets, their high target specificity, and their non-toxic metabolic products. However, a major limitation of peptides as drugs is
their typically poor oral availability, hindering their convenient and flexible application as pills. Of the more than 60 approved peptide drugs, the large majority is not orally applicable. The oral delivery of peptides is hampered by their metabolic instability and/or limited intestinal
uptake. In this article, we review the barriers peptides need to overcome after their oral administration to reach disease targets, we highlight two recent successes of pharma companies in developing orally applicable peptide drugs, and we discuss efforts of our laboratory towards the generation
of bioavailable cyclic peptides
Peptide Dendrimers: From Enzyme Models to Antimicrobials and Transfection Reagents
Get PDFAiming at studying cooperativity effects between amino acids in easily accessible protein models, we have explored the chemistry of peptide dendrimers, which we obtain as pure products by solid-phase peptide synthesis using a branching diamino acid such as lysine at every second or
third position in a peptide sequence, followed by reverse-phase HPLC purification. This article reviews discoveries driven by combinatorial library synthesis and screening, including enantioselective esterase and aldolase enzyme models, cobalamin binding and peroxidase dendrimers, glycopeptide
dendrimer biofilm inhibitors and their X-ray crystal structures as complexes with lectins, antimicrobial peptide dendrimers active against multidrug resistant Gram-negative bacteria, and transfection reagents for siRNA and CRISPR-Cas9 plasmid DNA. Latest developments include cheminformatics
and artificial intelligence for exploring the peptide chemical space, and the principle of stereorandomization to understand the role of peptide chirality in activity
Fundamental Research in Chemistry and the SCS: Past, Present, Future: Perspectives on Chemistry and Society on the Occasion of the 75th Anniversary of CHIMIA
No full textDigital Light 3D Printing of Biodegradable Elastomers for Personalized Devices: Polymer and Colloid Highlights
No full textFantastic Molecular Glues and Where to Find them: Medicinal Chemistry and Chemical Biology Highlights
No full textSurface Chemistry of Perovskite Oxynitride Photocatalysts: A Computational Perspective
Get PDFPerovskite oxynitrides are an established class of photocatalyst materials for water splitting. Previous computational studies have primarily focused on their bulk properties and have drawn relevant conclusions on their light absorption and charge transport properties. The actual catalytic
conversions, however, occur on their surfaces and a detailed knowledge of the atomic-scale structure and processes on oxynitride surfaces is indispensable to further improve these materials. In this contribution, we summarize recent progress made in the understanding of perovskite oxynitride
surfaces, highlight key processes that set these materials apart from their pure oxide counterparts and discuss challenges and possible future directions for research on oxynitrides