Results 221 to 230 of about 26,717 (273)

Development of a GC-376 Based Peptidomimetic PROTAC as a Degrader of 3-Chymotrypsin-like Protease of SARS-CoV-2.

ACS Medicinal Chemistry Letters
We have applied a proteolysis targeting chimera (PROTAC) technology to obtain a peptidomimetic molecule able to trigger the degradation of SARS-CoV-2 3-chymotrypsin-like protease (3CLPro).
Deborah Grifagni, E. Lenci, Alessia De Santis, Andrea Orsetti, C. G. Barracchia, Filomena Tedesco, Raffaele Bellini Puglielli, Francesca Lucarelli, Angela Lauriola, M. Assfalg, F. Cantini, V. Calderone, Daniele Guardavaccaro, A. Trabocchi, M. D'Onofrio, S. Ciofi‐Baffoni   +15 more
semanticscholar   +1 more source

Formylated polyamines as peptidomimetics

Bioorganic & Medicinal Chemistry Letters, 2012
A new construct for imitating a natural peptide ligand using a modified retro-inverso sequence is described. It is demonstrated through the synthesis of a peptidomimetic derived from the endogenous sequence of leucine enkephalin. The product was active at 400 nM and selective for μ-opioid receptors.
Sacha, Javor, Aaron, Janowsky, Robert, Johnson, Katherine, Wolfrum, Mitra, Tadayoni-Rebek, Julius, Rebek   +5 more
openaire   +2 more sources

Aminimides as Peptidomimetics

2003
Highly selective and specific protein-protein and peptide-protein interactions are elicited by a large number of natural specific biological responses. The mimicry of these natural interactions has been an important and useful strategy for the development of metabolically stable drugs capable of being administered orally (1-4).
B S, Fulton, A P, Kaplan, J C, Hogan, S L, Gallion   +3 more
openaire   +2 more sources

Novel peptidomimetic hematoregulatory compounds

Bioorganic & Medicinal Chemistry Letters, 2000
The activity of a novel series of peptidomimetic hematoregulatory compounds, designed based on a pharmacophore model inferred from the structure activity relationships of a peptide SK&F 107647 (1), is reported. These compounds induce a hematopoietic synergistic factor (HSF) which in turn modulates host defense.
D A, Heerding, M, Abruzzese, D, Alberts, J, Burgess, J F, Callahan, W F, Huffman, A G, King, S, LoCastro, P, DeMarsh, L M, Pelus, J S, Takata, P K, Bhatnagar   +11 more
openaire   +2 more sources

Minimalist and universal peptidomimetics

Chemical Society Reviews, 2011
Many "new generation" peptidomimetics are designed to present amino acid side chains only; they do not have structural features that resemble peptide main chains. These types of molecules have frequently been presented in the literature as mimics of specific secondary structures.
Eunhwa, Ko, Jing, Liu, Kevin, Burgess
openaire   +2 more sources

Peptidomimetics in cancer chemotherapy

Clinical and Translational Oncology, 2007
A summary of the current status of the application of peptidomimetics in cancer therapeutics as an alternative to peptide drugs is provided. Only compounds that are used in therapy or at least under clinical trials are discussed, using inhibitors of farnesyltransferase, proteasome and matrix metalloproteinases as examples.
C, Avendaño, J C, Menéndez
openaire   +2 more sources

Steroid Receptor Coactivator Peptidomimetics

2003
Publisher Summary This chapter focuses on the methods that are useful for designing and synthesizing a series of coactivator peptidomimetics (axXXbxcx) of the L1XXL2L3 sequence to identify specific inhibitors of particular hormone receptor (NR)–coactivator interactions.
Timothy R, Geistlinger, R Kiplin, Guy
openaire   +2 more sources

Peptidomimetics derived from natural products

Medicinal Research Reviews, 1993
Although much has been written in recent years about rational drug design, no drug has been designed de novo, that is, without using a natural substrate or inhibitor or screening lead as a starting point. Instead, as we have seen, medicinal chemists continue to depend upon serendipitous discovery of novel biological activities and novel chemical ...
R A, Wiley, D H, Rich
openaire   +2 more sources

Benzodiazepine peptidomimetic inhibitors of farnesyltransferase

Bioorganic & Medicinal Chemistry, 1994
A structural survey of protein Zn2+ binding geometries was instigated based upon the functional requirement of Ras farnesyltransferase for Zn2+. The Cys-X-X-Cys motif found in Zn(2+)-binding proteins such as aspartate transcarbamylase was used as a template to devise a bidentate-coordination model for Cys-A1-A2-X peptide inhibitors.
James C. Marsters, Robert S. McDowell, Mark E. Reynolds, David A. Oare, Todd C. Somers, Mark S. Stanley, Thomas E. Rawson, Martin E. Struble, Daniel J. Burdick, Kathryn S. Chan, Charles M. Duarte, Kenneth J. Paris, Jeff Y.K. Tom, Dairian T. Wan, Yingchun Xue, John P. Bumier   +15 more
openaire   +2 more sources

Oxetanyl Amino Acids for Peptidomimetics

Organic Letters, 2017
Peptides are important in the drug discovery process. In analogy to nonpeptidic small-molecule counterparts, they can sometimes suffer from disadvantages such as their low bioavailability and poor metabolic stability. Herein, we report the synthesis of new oxetanyl dipeptides and their incorporation into Leu-enkephalin analogues as proof-of-principle ...
Guido P. Möller, Steffen Müller, Bernd T. Wolfstädter, Susanne Wolfrum, Dirk Schepmann, Bernhard Wünsch, Erick M. Carreira   +6 more
openaire   +2 more sources