Results 61 to 70 of about 312,758 (261)

Targeted Degradation of Picornaviral 3C Protease via PROTACs Confers High Barrier to Viral Resistance and Broad‐Spectrum Antiviral Activity

open access: yesAdvanced Science, EarlyView.
This study reports D34 as the first PROTAC degrader that targets the 3C protease of picornaviruses. D34 effectively degrades EV71 3C protease via the ubiquitin‐proteasome pathway. More importantly, D34 exhibits a high resistance barrier and shows broad‐spectrum antiviral activity against multiple picornaviruses, highlighting its potential as a novel ...
Weilong Deng   +9 more
wiley   +1 more source

Beyond Simple Mimicry: Next‐Generation Geometric Architectures and Future Paradigms in Small‐Molecule and Macrocyclic Peptidomimetics

open access: yesAngewandte Chemie, EarlyView.
Peptide‐to‐Small Molecule Paradigm: Peptidomimetics have evolved from simple mimicry toward drug‐like scaffolds supported by increasing clinical successes. This Perspective highlights the geometric design principles—linear repetition, convergent fusion, and cyclization—defining the next‐generation peptidomimetic architectures capable of targeting ...
Jesang Lee   +5 more
wiley   +2 more sources

Programmable Nanobody‐Targeting Chimeras Enable Intracellular Viral Protein Degradation

open access: yesAdvanced Science, EarlyView.
Nab‐TAC enables targeted degradation of HBV surface antigen (HBsAg) in vivo. By fusing nanobody‐based recognition domains with programmable proteasome‐recruiting degradation signals, Nab‐TAC reduces HBsAg levels in a hydrodynamic HBV mouse model. ABSTRACT Chronic hepatitis B virus (HBV) infection remains a major global health challenge, largely because
Max Yu‐Chen Pan   +11 more
wiley   +1 more source

Direct Regioselective para‐Fluorination via I(I)/I(III) Catalysis

open access: yesAngewandte Chemie, EarlyView.
A direct, para‐selective fluorination by I(I)/I(III) catalysis is disclosed that does not require substrate pre‐functionalization. This strategy leverages the Leonard link inherent to phenylpropanoate and phenylpropanamides to promote a spirocyclization/para‐selective sequence. The C3‐side chain maps onto a range of common drug scaffolds and allows the
Christoph Roblick   +5 more
wiley   +2 more sources

S100A9 tetramers, which are ligands of CD85j, increase the ability of MVAHIV-primed NK cells to control HIV infection

open access: yesFrontiers in Immunology, 2015
Natural Killer (NK) cells are the major antiviral effector population of the innate immune system. We previously found that S100A9 is a novel ligand of the receptor CD85j and that S100A9 tetramers enhance the anti-HIV activity of NK cells. Also, we found
Uriel eMoreno-Nieves1   +5 more
doaj   +1 more source

METTL7A Downregulation Drives SLC1A5‐Mediated Glutamine Competition to Promote Tumor Proliferation and Suppress CD8+ T Cell Immunity in Gastric Cancer

open access: yesAdvanced Science, EarlyView.
GC cells enhance glutamine accumulation by upregulating SLC1A5 expression. This upregulation not only boosts GC cell proliferation, but also outcompetes CD8+ T cells for glutamine and suppresses their antitumor immunity. Mechanistically, METTL7A deficiency in GC induces SLC1A5 overexpression via an m6A‐dependent pathway and N‐glycosylation ...
Mingjun Sun   +16 more
wiley   +1 more source

Stress Hyperglycemia Drives CD4+ T Cell PANoptosis and Postoperative Organ Injury via Monocyte‐Derived Succinate

open access: yesAdvanced Science, EarlyView.
High glucose is linked to reduced succinate dehydrogenase activity in CD14+ monocytes, accompanied by succinate accumulation and extracellular release. Extracellular succinate exacerbates mitochondrial ROS production and mtDNA release in CD4+ T cells. Cytosolic mtDNA then activates Z‐DNA binding protein 1 (ZBP1) and engages ZBP1‐associated inflammatory
Shuai Zhao   +11 more
wiley   +1 more source

TRIM28‐Derived Peptide Exerts Anti‐Tumor Roles by Stabilizing Tumor Suppressive BRD7 Protein in Multiple Cancers

open access: yesAdvanced Science, EarlyView.
An α‐helical peptide, TAB12, designed to mimic the TRIM28 binding interface, competitively disrupts the TRIM28‐BRD7 interaction, thereby blocking ubiquitin‐mediated degradation of the tumor suppressor BRD7. This stabilization unleashes potent anti‐tumor effects across multiple tumor types with a favorable safety profile, offering a feasible strategy ...
Qingqing Wei   +10 more
wiley   +1 more source

Structure-Activity Relationships of Synthetic Coumarins as HIV-1 Inhibitors

open access: yesBioinorganic Chemistry and Applications, 2006
HIV/AIDS pandemics is a serious threat to health and development of mankind, and searching for effective anti-HIV agents remains actual. Considerable progress has been made in recent years in the field of drug development against HIV.
I. Kostova   +3 more
doaj   +2 more sources

Canonical Antibodies Adopt Distinct Binding Modes to Recognize Viral Glycan Shields

open access: yesAdvanced Science, EarlyView.
Canonical Y‐shaped antibodies recognize viral glycan shields through adaptive Fab assembly states shaped by glycan organization and somatic hypermutation. Structural analyses ofbroadly neutralizing antibodies VRC35 and VRC36 across glycoproteins of HIV‐1, influenza, SARS‐CoV‐2, and Lassa viruses reveal distinct Fab assembly states, spanning monovalent,
Jiaxuan Cheng   +71 more
wiley   +1 more source

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