An effective conjugation strategy for designing short peptide-based HIV-1 fusion inhibitors

G Liang, H Wang, H Chong, S Cheng… - Organic & …, 2016 - pubs.rsc.org
Lengthy peptides corresponding to the C-terminal heptad repeat (C-peptides) of human
immunodeficiency virus type 1 (HIV-1) gp41 are potent inhibitors against virus–cell fusion …

Pharmaceutical implications of helix length control in helix-mediated protein–protein interactions

LG Milroy, L Brunsveld - Future Medicinal Chemistry, 2013 - Taylor & Francis
The most abundant protein secondary structure in nature–the α-helix–is frequently found at
protein interfaces, making it an important lead structure for the design of small-molecule …

Bivalent HIV-1 fusion inhibitors based on peptidomimetics

T Kobayakawa, K Ebihara, K Tsuji, T Kawada… - Bioorganic & Medicinal …, 2020 - Elsevier
Membrane fusion is a valid target for inhibition of HIV-1 replication. A 34-mer fragment
peptide (C34), which is contained in the HIV-1 envelope protein gp41, has significant anti …

Metathesis‐Based Stapling of a Pyridine–Acetylene–Phenol Oligomer Having Alkenyl Side Chains after Intermolecular Templation by Native Saccharides

H Abe, C Sato, Y Ohishi… - European Journal of …, 2018 - Wiley Online Library
A nonameric (pyridine–acetylene–phenol–acetylene) 4–pyridine oligomer formed a helical
structure by intermolecular templation with a hexose such as d‐glucose associated by the …

Macrocyclic α-helical peptide drug discovery

TK Sawyer, V Guerlavais, K Darlak, E Feyfant - 2014 - books.rsc.org
Macrocyclization of peptides has inspired both basic research and drug discovery focused
on Nature's three dimensional (3D) molecular recognition underlying intracellular protein …

[HTML][HTML] HIV-1 Integrase-targeted short peptides derived from a viral protein r sequence

XZ Zhao, M Métifiot, E Kiselev, JJ Kessl, K Maddali… - Molecules, 2018 - mdpi.com
HIV-1 integrase (IN) inhibitors represent a new class of highly effective anti-AIDS
therapeutics. Current FDA-approved IN strand transfer inhibitors (INSTIs) share a common …

Effects of alkyl side chains and terminal hydrophilicity on vitamin D receptor (VDR) agonistic activity based on the diphenylpentane skeleton

T Misawa, M Yorioka, Y Demizu… - Bioorganic & Medicinal …, 2015 - Elsevier
Vitamin D receptor (VDR) is a family of nuclear receptors (NR) that regulates physiological
effects such as the immune system, calcium homeostasis, and cell proliferation. We …

All Hydrocarbon Stapled Peptides as Allosteric Modulators of Protein-Protein Interactions

GN Bendzunas - 2021 - search.proquest.com
The ubiquity and variety of protein-protein interactions (PPI) mediating the human protein
interactome make them an attractive yet daunting target for investigation and therapeutic …

[PDF][PDF] Small-Molecule Anti-HIV-1 Agents Based on HIV-1 Capsid Proteins. Biomolecules 2021, 11, 208

T Kobayakawa, M Yokoyama, K Tsuji, M Fujino… - 2021 - pdfs.semanticscholar.org
The capsid of human immunodeficiency virus type 1 (HIV-1) is a shell that encloses viral
RNA and is highly conserved among many strains of the virus. It forms a conical structure by …

Inhibition of talin-induced integrin activation by a double-hit stapled peptide

T Gao, E Cho, P Zhang, J Wu - Structure, 2023 - cell.com
Integrins are ubiquitously expressed cell-adhesion proteins. Activation of integrins is
triggered by talin through an inside-out signaling pathway, which can be driven by RAP1 …