Results 11 to 20 of about 1,053 (147)

Synthesis of Low-Molecular-Weight Fucoidan Analogue and Its Inhibitory Activities against Heparanase and SARS-CoV-2 Infection. [PDF]

Angew Chem Int Ed Engl
The purpose‐designed low‐molecular‐weight fucoidan analogue exhibited anti‐heparanase activity even in the cell‐based assay. In addition, the analogue inhibited the binding between SARS‐CoV‐2 spike protein (SARS‐CoV‐2‐S) and heparin and between SARS‐CoV‐2‐S and angiotensin‐converting enzyme 2 (ACE2).
Sugimoto A, Koike T, Kuboki Y, Komaba S, Kosono S, Aswathy M, Anzai I, Watanabe T, Toshima K, Takahashi D.   +9 more
europepmc   +3 more sources

ROS-Triggered Microgels for Programmable Drug Release in Volumetric Muscle Loss Repair. [PDF]

Adv Healthc Mater
Reduced graphene oxide‐incorporated hyaluronic acid microgels are developed as ROS‐responsive, injectable platforms for curcumin delivery in volumetric muscle loss. The microgels exhibit strong antioxidative activity, high drug‐loading capacity, and ROS‐triggered release.
Lee S, Choe G, Kim J, Park J, Kok JYE, Lee JY.   +5 more
europepmc   +2 more sources

2‐Carboranylquinazoline: The Path to an ABCG2 Inhibitor

ChemMedChem, Volume 18, Issue 11, June 1, 2023., 2023
Better 2 than 4: The efflux transporter ABCG2 is highly associated with drug resistance in cancer cells. Introduction of a carborane moiety at position 2 of a quinazolin‐4‐amine scaffold gave N‐phenyl‐2‐carboranylquinazolin‐4‐amine which, compared to its N‐carboranyl regioisomer, provided enhanced inhibitory activity and the ability to reverse ...
Philipp Stockmann, Lydia Kuhnert, Lisa Zörner, Walther Honscha, Evamarie Hey‐Hawkins   +4 more
wiley   +1 more source

How Single Site Mutations Can Help Understanding Structure Formation of Amyloid β1−40

Macromolecular Bioscience, Volume 23, Issue 5, May 2023., 2023
The contact between phenylalanine 19 and leucine 34 in Aβ molecules is highly conserved suggesting a particular significance for Aβ misfolding and, in turn, for its neurotoxicity. Point mutations in Aβ peptides at the contact F19−L34 help understanding this importance.
Benedikt Schwarze, Daniel Huster
wiley   +1 more source

Graphene‐Based Materials in Dental Applications: Antibacterial, Biocompatible, and Bone Regenerative Properties

International Journal of Biomaterials, Volume 2023, Issue 1, 2023., 2023
Graphene‐based materials have been shown to have advantageous properties in biomedical and dental applications due to their high mechanical, physiochemical, antibacterial, and stem cell differentiating properties. Although graphene‐based materials have displayed appropriate biocompatible properties when used in implant materials for orthopedic ...
A. G. Williams, E. Moore, A. Thomas, J. A. Johnson, Alexander Seifalian   +4 more
wiley   +1 more source

Endoplasmic reticulum oxidoreductin 1‐alpha deficiency and activation of protein translation synergistically impair breast tumour resilience

British Journal of Pharmacology, Volume 179, Issue 23, Page 5180-5195, December 2022., 2022
Background and Purpose Endoplasmic reticulum (ER) stress triggers an adaptive response in tumours which fosters cell survival and resilience to stress. Activation of the ER stress response, through its PERK branch, promotes phosphorylation of the α‐subunit of the translation initiation factor eIF2, thereby repressing general protein translation and ...
Ersilia Varone, Alessandra Decio, Maria Chiara Barbera, Marco Bolis, Laura Di Rito, Federica Pisati, Raffaella Giavazzi, Ester Zito   +7 more
wiley   +1 more source

FOXM1 Inhibition Enhances the Therapeutic Outcome of Lung Cancer Immunotherapy by Modulating PD‐L1 Expression and Cell Proliferation

Advanced Science, Volume 9, Issue 29, October 14, 2022., 2022
In this study, the authors show that FOXM1 selectively regulates PD‐L1 expression by binding directly to the PD‐L1 promoter. The FOXM1 inhibitor significantly lowers PD‐L1 levels and tumor growth in vitro and in vivo without any side effects on vital normal tissues.
Hamadi Madhi, Jeon‐Soo Lee, Young Eun Choi, Yan Li, Myoung Hee Kim, Yongdoo Choi, Sung‐Ho Goh   +6 more
wiley   +1 more source

Development of a potent small‐molecule degrader against oncogenic BRAFV600E protein that evades paradoxical MAPK activation

Cancer Science, Volume 113, Issue 8, Page 2828-2838, August 2022., 2022
In this study, we developed chimeric compounds, proteolysis targeting chimeras (PROTACs), that target BRAF V600E protein for degradation. CRBN(BRAF)‐24, the most effective chimera, selectively degraded BRAF V600E in a ubiquitin‐proteasome system (UPS)‐dependent manner and inhibited the proliferation of BRAF V600E‐driven cancer cells.
Nobumichi Ohoka, Masanori Suzuki, Takuya Uchida, Yoshinori Tsukumo, Masayuki Yoshida, Takao Inoue, Hitoshi Ohki, Mikihiko Naito   +7 more
wiley   +1 more source

Baseline and time‐updated factors in preclinical development of anionic dendrimers as successful anti‐HIV‐1 vaginal microbicides

WIREs Nanomedicine and Nanobiotechnology, Volume 14, Issue 3, May/June 2022., 2022
Key preclinical steps in the development of a vaginal microbicide against HIV‐1 infection to lead to clinical trials. Abstract Although a wide variety of topical microbicides provide promising in vitro and in vivo efficacy, most of them failed to prevent sexual transmission of human immunodeficiency virus type 1 (HIV‐1) in human clinical trials.
Ignacio Rodríguez‐Izquierdo, Daniel Sepúlveda‐Crespo, Jose María Lasso, Salvador Resino, Ma Ángeles Muñoz‐Fernández   +4 more
wiley   +1 more source

Identification of natural compounds tubercidin and lycorine HCl against small‐cell lung cancer and BCAT1 as a therapeutic target

Journal of Cellular and Molecular Medicine, Volume 26, Issue 9, Page 2557-2565, May 2022., 2022
Abstract Although small‐cell lung cancer (SCLC) accounts for a small fraction of lung cancer cases (~15%), the prognosis of patients with SCLC is poor with an average overall survival period of a few months without treatment. Current treatments include standard chemotherapy, which has minimal efficacy and a newly developed immunotherapy that thus far ...
Jungang Chen, Lindsey Barrett, Zhen Lin, Samantha Kendrick, Shengyu Mu, Lu Dai, Zhiqiang Qin   +6 more
wiley   +1 more source