Poor oral bioavailability, low metabolic stability towards proteolysis and rapid excretion via both liver and kidneys displayed by innumerable peptides of potential therapeutic value has generated an intensive search for peptidomimics (1-2). A possible approach of such nonpeptidal peptidomimics is to replace the peptide by a scaffold that distributes in the space the peptidal side chains of amino acids essential for biological activity and mimics the bioactive conformation of the peptide.
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http://dx.doi.org/10.1385/0-89603-517-4:227 | DOI Listing |
Angew Chem Int Ed Engl
December 2023
School of Chemistry, Indian Institute of Science Education and Research Thiruvananthapuram Thiruvananthapuram, Kerala, 695551, India.
There is much demand for crystalline covalent helical polymers. Inspired by the helical structure of collagen, we synthesized a covalent helical polymer wherein the repeating dipeptide Gly-Pro units are connected by triazole linkages. We synthesized an azide and alkyne-modified dipeptide monomer made up of the repeating amino acid sequence of collagen.
View Article and Find Full Text PDFACS Macro Lett
April 2020
Department of Pure & Applied Chemistry, University of Strathclyde, 295 Cathedral Street, Glasgow G1 1XL, U.K.
Peptoids are biofunctional -substituted glycine peptidomimics. Their self-assembly is of fundamental interest because they demonstrate alternatives to conventional peptide structures based on backbone chirality and beta-sheet hydrogen bonding. The search for self-assembling, water-soluble "minimal" sequences, be they peptide or peptidomimic, is a further challenge.
View Article and Find Full Text PDFBr J Pharmacol
April 2019
Novartis Pharmaceuticals Corporation, Fort Worth, TX, 76134, USA.
In contrast to the availability of potent and selective antagonists of several prostaglandin receptor types (including DP , DP , EP and TP receptors), there has been a paucity of well-characterized, selective FP receptor antagonists. The earliest ones included dimethyl amide and dimethyl amine derivatives of PGF , but these have failed to gain prominence. The fluorinated PGF analogues, AL-8810 and AL-3138, were subsequently discovered as competitive and non-competitive FP receptor antagonists respectively.
View Article and Find Full Text PDFPLoS One
April 2016
Council of Scientific and Industrial Research-Central Leather Research Institute, Chemical Laboratory, Adyar, Chennai, 600 020, India.
ACS Chem Neurosci
June 2013
Department of Physiology, University of Texas Southwestern Medical Center at Dallas, Dallas, Texas 75390, United States.
Alzheimer's disease (AD) is the most common form of dementia and currently affects 5.4 million Americans. A number of anti-Aβ (beta amyloid) therapeutic agents have been developed for AD, but so far all of them failed in clinic.
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