Optimized Ring Closing Metathesis Reaction Conditions To Suppress Desallyl Side Products in the Solid-Phase Synthesis of Cyclic Peptides Involving Tyrosine(O …

SA Gisemba, JV Aldrich - The Journal of organic chemistry, 2019 - ACS Publications
We are exploring constraining aromatic residues in the kappa opioid receptor selective
antagonist arodyn (Ac [Phe1, 2, 3, Arg4, d-Ala8] dynorphin A (1-11)-NH2) by ring closing …

Anti-HIV screening for cell-penetrating peptides using chloroquine and identification of anti-HIV peptides derived from matrix proteins

T Mizuguchi, N Ohashi, W Nomura, M Komoriya… - Bioorganic & Medicinal …, 2015 - Elsevier
Previously, compounds which inhibit the HIV-1 replication cycle were found in overlapping
peptide libraries covering the whole sequence of an HIV-1 matrix (MA) protein constructed …

Potent leads based on CA-19L, an anti-HIV active HIV-1 capsid fragment

K Tsuji, R Wang, T Kobayakawa, KBA Owusu… - Bioorganic & Medicinal …, 2021 - Elsevier
Several anti-HIV-1 peptides have previously been found among overlapping fragment
peptide libraries that contain an octa-arginyl moiety and cover the whole sequence of an HIV …

The discovery of allyltyrosine based tripeptides as selective inhibitors of the HIV-1 integrase strand-transfer reaction

N Dalton, CP Gordon, TP Boyle… - Organic & …, 2016 - pubs.rsc.org
From library screening of synthetic antimicrobial peptides, an O-allyltyrosine-based
tripeptide was identified to possess inhibitory activity against HIV-1 integrase (IN) exhibiting …

The stapled AKAP disruptor peptide STAD-2 displays antimalarial activity through a PKA-independent mechanism

BR Flaherty, Y Wang, EC Trope, TG Ho… - PLoS …, 2015 - journals.plos.org
Drug resistance poses a significant threat to ongoing malaria control efforts. Coupled with
lack of a malaria vaccine, there is an urgent need for the development of new antimalarials …

[HTML][HTML] Development of Small-Molecule Anti-HIV-1 Agents Targeting HIV-1 Capsid Proteins

T Kobayakawa, M Yokoyama, K Tsuji… - Chemical and …, 2024 - jstage.jst.go.jp
The capsid of human immunodeficiency virus type 1 (HIV-1) forms a conical structure by
assembling oligomers of capsid (CA) proteins and is a virion shell that encapsulates viral …

Hybrids of small CD4 mimics and gp41-related peptides as dual-target HIV entry inhibitors

R Wang, K Tsuji, T Kobayakawa, Y Liu… - Bioorganic & Medicinal …, 2022 - Elsevier
Hybrid molecules containing small CD4 mimics and gp41-C-terminal heptad repeat (CHR)-
related peptides have been developed. A YIR-821 derivative was adopted as a CD4 mimic …

Efficient synthesis of a multi-substituted diphenylmethane skeleton as a steroid mimetic

T Misawa, K Tanaka, Y Demizu, M Kurihara - Bioorganic & Medicinal …, 2017 - Elsevier
Steroids are important components of cell membranes and are involved in several
physiological functions. A diphenylmethane (DPM) skeleton has recently been suggested to …

Influence of α-methylation in constructing stapled peptides with olefin metathesis

Q Zhang, X Shi, Y Jiang, Z Li - Tetrahedron, 2014 - Elsevier
Ring-closing metathesis is commonly utilized in peptide macro-cyclization. The influence of
α-methylation of the amino acids bearing the olefin moieties has never been systematically …

Anti-inflammatory macrolides to manage chronic neutrophilic inflammation

M Burnet, JH Guse, HJ Gutke, L Guillot, S Laufer… - 2014 - books.rsc.org
''Inflammation''broadly describes a tissue response to insult. It may be pathological, or it may
be healthy and regenerative. 1 Therapeutic approaches to inflammation have tended to …