Pretubulysin derived probes as novel tools for monitoring the microtubule network via activity-based protein profiling and fluorescence microscopy [PDF]
, 2012 Microtubules (mt) are highly dynamic polymers composed of alpha- and beta-tubulin monomers that are present in all dividing and non-dividing cells. A broad variety of natural products exists that are known to interfere with the microtubule network, by ...
Burkhart, Jens L. +7 more
core +1 more source
EBioMedicine, 2017 Therapeutic approaches to fight Alzheimer's disease include anti-Amyloidβ (Aβ) antibodies and secretase inhibitors. However, the blood-brain barrier (BBB) limits the brain exposure of biologics and the chemical space for small molecules to be BBB ...
Nadine Ruderisch +18 more
doaj +1 more source
Tetrahydrobenzo[h][1,6]naphthyridine-6-chlorotacrine hybrids as a new family of anti-Alzheimer agents targeting beta-amyloid, tau, and cholinesterase pathologies [PDF]
, 2014 Optimization of an essentially inactive 3,4-dihydro-2H-pyrano[3,2-c]quinoline carboxylic ester derivative as acetylcholinesterase (AChE) peripheral anionic site (PAS)-binding motif by double O → NH bioisosteric replacement, combined with molecular ...
Clos, Victòria +9 more
core +2 more sources
Optimization of a class of tryptophan dendrimers that inhibit HIV replication leads to a selective, specific, and low-nanomolar inhibitor of clinical isolates of enterovirus A71 [PDF]
, 2016 Tryptophan dendrimers that inhibit HIV replication by binding to the HIV envelope glycoproteins gp120 and gp41 have unexpectedly also proven to be potent, specific, and selective inhibitors of the replication of the unrelated enterovirus A71.
Camarasa Rius, María José +10 more
core +1 more source
Ribosome-Inactivating Proteins: From Plant Defense to Tumor Attack
Toxins, 2010 Ribosome-inactivating proteins (RIPs) are EC3.2.32.22 N-glycosidases that recognize a universally conserved stem-loop structure in 23S/25S/28S rRNA, depurinating a single adenine (A4324 in rat) and irreversibly blocking protein translation, leading ...
Maria Serena Fabbrini +3 more
doaj +1 more source
Journal of Translational Autoimmunity, 2021 Increased interferon-α (IFN-α) production is a critical component in the pathophysiology of systemic lupus erythematosus (SLE) and other rheumatic autoimmune diseases.
Fanny Duguet +13 more
doaj +1 more source
Potent inhibitors active against HIV reverse transcriptase with K101P, a mutation conferring rilpivirine resistance [PDF]
, 2015 Catechol diether compounds have nanomolar antiviral and enzymatic activity against HIV with reverse transcriptase (RT) variants containing K101P, a mutation that confers high-level resistance to FDA-approved non-nucleoside inhibitors efavirenz and ...
Anderson, Karen S. +9 more
core +2 more sources
Neurobiology of Disease, 2021 A growing body of evidence suggests that aggregated α-synuclein, the major constituent of Lewy bodies, plays a key role in the pathogenesis of Parkinson's disease and related α-synucleinopathies.
Eva Nordström +21 more
doaj +1 more source
A time-resolved fluorescence immunoassay for the measurement of testosterone in saliva: Monitoring of testosterone replacement therapy with testosterone buciclate [PDF]
, 1998 Monitoring of testosterone replacement therapy requires a reliable method for testosterone measurement. Determination of salivary testosterone, which reflects the hormone's biologically active plasma fraction, is a superior technique for this purpose ...
Bals-Pratsch M +13 more
core +1 more source
Potent single-domain antibodies that arrest respiratory syncytial virus fusion protein in its prefusion state [PDF]
, 2017 Human respiratory syncytial virus (RSV) is the main cause of lower respiratory tract infections in young children. The RSV fusion protein (F) is highly conserved and is the only viral membrane protein that is essential for infection.
Chen, Man +13 more
core +2 more sources