Live-Cell Raman Imaging Elucidates Intracellular Distribution of Macrocyclic Peptides Designed as HIV Protease Inhibitors. [PDF]
Nawa Y +8 more
europepmc +1 more source
Kinetic Fingerprints as Mechanistic and Clinical Roadmaps Across KIT Activation States
Kinetic profiling of 172 compounds across KIT conformations—including D816V—reveals kinetic fingerprints that predict efficacy, selectivity, resistance, and inhibitors’ ability to stabilize key regulatory elements. Far from a secondary metric, binding kinetics provide mechanistic insights beyond affinity, offering a powerful framework for rational drug
Ana Corrionero +7 more
wiley +1 more source
Asymmetric Synthesis of the HIV Protease Inhibitor TMC-126, a PMX Antimalarial Protease Inhibitor, and a Putative COVID-19 Inhibitor Using a Highly Stereoselective Glycolate Aldol Addition Reaction Pathway. [PDF]
Affram KA +9 more
europepmc +1 more source
The protease from type I human immunodeficiency virus (HIV-1 ) is a critical drug target against which many therapeutically useful inhibitors have been developed; however, the set of viral strains in the population has been shifting to become more drug ...
ALEXANDER L. PERRYMAN;LIN, JUNG-HSIN;J. ANDREW MCCAMMON +1 more
core
What's new? TRIM25 is known for its role in antiviral immunity and association with poor prognosis in various cancers. This study reveals an association between high TRIM25 expression and Merkel cell polyomavirus positivity in Merkel cell carcinoma.
Klaus W. Fagerstedt +6 more
wiley +1 more source
Drug Repurposing: Conversion of the Peripherally Restricted HIV Protease Inhibitor Amprenavir to Potent, Selective, and CNS-Penetrant Agonists for the Cannabinoid Receptor 2. [PDF]
Haymer DH +15 more
europepmc +1 more source
This study evaluated 1433 human immunodeficiency virus (HIV)-infected patients starting highly active antiretroviral therapy (HAART), 409 (28%) of whom had prior nucleoside experience and achieved an HIV load of
Klauke, S +11 more
core
HIV‐1 establishes immediate latency in T cells expressing the viral Nef protein
Nef is a viral protein often omitted from HIV‐1 reporter viruses. Consequently, its role in viral latency is unclear. We developed three novel dual reporter HIV‐1 derivatives that express Nef and allow for detection of latent and productive infection. Using these reporters, we show that Nef does not affect the establishment of immediate viral latency ...
Cindy Lam, Ivan Sadowski
wiley +1 more source
Computational Simulation of HIV Protease Inhibitors to the Main Protease (Mpro) of SARS-CoV-2: Implications for COVID-19 Drugs Design. [PDF]
Yu W +14 more
europepmc +1 more source
Strategies for Loading and Releasing Peptide Therapeutics in Biodegradable Carriers
A biodegradable carrier‐based peptide delivery system is a powerful treatment platform for diverse diseases, owing to its superior therapeutic efficacy and low toxicity. This review examines the conventional peptide‐loaded carrier fabrication process and its current limitations.
Wookyoung Jang, Ki Wan Bong
wiley +1 more source

