Results 71 to 80 of about 1,152,447 (302)

Structural insights into an engineered feruloyl esterase with improved MHET degrading properties

open access: yesFEBS Letters, EarlyView.
A feruloyl esterase was engineered to mimic key features of MHETase, enhancing the degradation of PET oligomers. Structural and computational analysis reveal how a point mutation stabilizes the active site and reshapes the binding cleft, expading substrate scope.
Panagiota Karampa   +5 more
wiley   +1 more source

Compensatory effects in the PI3K/PTEN/AKT signaling network following receptor tyrosine kinase inhibition [PDF]

open access: yes, 2011
Overcoming de novo and acquired resistance to anticancer drugs that target signaling networks is a formidable challenge for drug design and effective cancer therapy.
Bown, James L.   +5 more
core   +4 more sources

Effect of amaranth proteins on the RAS system: In vitro, in vivo and ex vivo assays [PDF]

open access: yes, 2020
The aim of this work was to analyse the hypotensive effect of amaranthprotein/peptides on spontaneously hypertensive rats (SHR). The mechanism of action of these peptides was studied in vivo and ex vivo.
Aphalo, Paula   +4 more
core   +2 more sources

Gut microbiome and aging—A dynamic interplay of microbes, metabolites, and the immune system

open access: yesFEBS Letters, EarlyView.
Age‐dependent shifts in microbial communities engender shifts in microbial metabolite profiles. These in turn drive shifts in barrier surface permeability of the gut and brain and induce immune activation. When paired with preexisting age‐related chronic inflammation this increases the risk of neuroinflammation and neurodegenerative diseases.
Aaron Mehl, Eran Blacher
wiley   +1 more source

2-Oxoesters: A Novel Class of Potent and Selective Inhibitors of Cytosolic Group IVA Phospholipase A2. [PDF]

open access: yes, 2017
Cytosolic phospholipase A2 (GIVA cPLA2) is the only PLA2 that exhibits a marked preference for hydrolysis of arachidonic acid containing phospholipid substrates releasing free arachidonic acid and lysophospholipids and giving rise to the generation of ...
Barbayianni, Efrosini   +10 more
core   +1 more source

A methionine‐lined active site governs carbocation stabilization and product specificity in a bacterial terpene synthase

open access: yesFEBS Letters, EarlyView.
This study reveals a unique active site enriched in methionine residues and demonstrates that these residues play a critical role by stabilizing carbocation intermediates through novel sulfur–cation interactions. Structure‐guided mutagenesis further revealed variants with significantly altered product profiles, enhancing pseudopterosin formation. These
Marion Ringel   +13 more
wiley   +1 more source

Molecular Logic as a Means to Assess Therapeutic Antidotes

open access: yesFrontiers in Chemistry, 2019
An emerging direction in the area of molecular logic and computation is developing molecular-scale devices that can operate in complex biological environments, such as within living cells, which are beyond the reach of conventional electronic devices ...
Linor Unger-Angel   +2 more
doaj   +1 more source

The structural basis for the selectivity of sulfonamido dicarbaboranes toward cancer-associated carbonic anhydrase IX

open access: yesJournal of Enzyme Inhibition and Medicinal Chemistry, 2020
Human carbonic anhydrase IX (CA IX), a protein specifically expressed on the surface of solid tumour cells, represents a validated target both for anticancer therapy and diagnostics.
Michael Kugler   +10 more
doaj   +1 more source

Angiotensin-Converting Enzyme Inhibitor / Angiotensin II Receptor Blocker in COVID-19: a Double-edged Sword or a Myth

open access: yesNepalese Medical Journal, 2020
Angiotensin-converting enzyme-2 receptor has been unearthed as a prime site of entry of Severe Acute Respiratory Syndrome Coronavirus 2 owing to its strong affinity towards spike protein of Severe Acute Respiratory Syndrome Coronavirus 2, resulting in ...
Kunal Bikram Shaha   +5 more
doaj   +1 more source

Valosin‐containing protein counteracts ATP‐driven dissolution of FUS condensates through its ATPase activity in vitro

open access: yesFEBS Letters, EarlyView.
Biomolecular condensates formed by fused in sarcoma (FUS) are dissolved by high ATP concentrations yet persist in cells. Using a reconstituted system, we demonstrate that valosin‐containing protein (VCP), an AAA+ ATPase, counteracts ATP‐driven dissolution of FUS condensates through its D2 ATPase activity.
Hitomi Kimura   +2 more
wiley   +1 more source

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