Results 131 to 140 of about 754,901 (303)

Reconstructing enzyme evolution by protein engineering

FEBS Letters, EarlyView.
Natural enzyme evolution can be retraced by protein engineering methods such as directed evolution, rational design, and ancestral sequence reconstruction. These approaches reveal how enzymes emerged from ligand‐binding scaffolds, developed varying substrate preferences, formed oligomeric complexes, adapted to environmental changes, and evolved novel ...
Lukas Drexler, Markus R. Busch, Reinhard Sterner   +2 more
wiley   +1 more source

Drug discovery by dynamic combinatorial libraries

, 2002
Dynamic combinatorial chemistry is a recently introduced supramolecular approach that uses self-assembly processes to generate libraries of chemical compounds.
Ramström, Olof,, Olof Ramström, Lehn, J. M., Jean-Marie Lehn   +3 more
core   +1 more source

Synergistic Effect of Combination Treatment of Brexpiprazole and Nalmefene on Ethanol Intake in Rats

Neuropsychopharmacology Reports
Aims Reduction of alcohol consumption is one of treatment goals to reduce harm among individuals with alcohol use disorder (AUD), a major worldwide health problem, for which nalmefene, an opioid receptor modulator, is used.
Naoki Amada, Mai Nakamura, Yuta Ohgi, Yusuke Kakumoto, Mikio Suzuki, Takashi Futamura, Kenji Maeda   +6 more
doaj   +1 more source

The role of miR‐335‐5p in the redifferentiation of BRAF p.V600E thyroid cancers

Molecular Oncology, EarlyView.
The BRAF p.V600E mutation promotes thyroid cancer dedifferentiation and radioiodine resistance. Using a network approach, we identified miR‐335‐5p as a key regulator of BRAF‐mutated thyroid tumors. Restoring miR‐335‐5p increased thyroid‐specific gene expression and iodine uptake in cells and organoids.
Valeria Pecce, Simone Bini, Marialuisa Sponziello, Giorgio Grani, Giulia Fiscon, Paola Paci, Lorenzo Farina, Rosa Falcone, Valentina Maggisano, Sebastiano Filetti, Cosimo Durante, Antonella Verrienti   +11 more
wiley   +1 more source

Optimisation-based modelling for explainable lead discovery in malaria [PDF]

Background: The search for new antimalarial treatments is urgent due to growing resistance to existing therapies. The Open Source Malaria (OSM) project offers a promising starting point, having extensively screened various compounds for their ...
Li, Yutong, Furnham, Nicholas, Tsoka, Sophia, Cardoso-Silva, Jonathan, Papageorgiou, Lazaros G, Kelly, John M, Delves, Michael J   +6 more
core  

A high-throughput quality control method for assessing the serial dilution performance of dose–response plates with acoustic ejection mass spectrometry

SLAS Technology
This study aimed to develop a streamlined method for evaluating the dilution ratio of drug dose–response plates created by automated liquid handlers in the early stages of drug discovery.
Mary Ashley Rimmer, Nathaniel R Twarog, Yong Li, Anang A Shelat, Zoran Rankovic, Lei Yang   +5 more
doaj   +1 more source

TRAIL‐PEG‐Apt‐PLGA nanosystem as an aptamer‐targeted drug delivery system potential for triple‐negative breast cancer therapy using in vivo mouse model

Molecular Oncology, EarlyView.
Aptamers are used both therapeutically and as targeting agents in cancer treatment. We developed an aptamer‐targeted PLGA–TRAIL nanosystem that exhibited superior therapeutic efficacy in NOD/SCID breast cancer models. This nanosystem represents a novel biotechnological drug candidate for suppressing resistance development in breast cancer.
Gulen Melike Demirbolat, Aslihan Kucuk, Omer Erdogan, Samed Ozer, Bensu Kozan, Tugba Cuceli, Erkan Gumus, Evrim Cevik, Ozge Cevik   +8 more
wiley   +1 more source

Tumour–host interactions in Drosophila: mechanisms in the tumour micro‐ and macroenvironment

Molecular Oncology, EarlyView.
This review examines how tumour–host crosstalk takes place at multiple levels of biological organisation, from local cell competition and immune crosstalk to organism‐wide metabolic and physiological collapse. Here, we integrate findings from Drosophila melanogaster studies that reveal conserved mechanisms through which tumours hijack host systems to ...
José Teles‐Reis, Tor Erik Rusten
wiley   +1 more source

Circular RNA expression landscapes in myelodysplastic neoplasms: Associations with mutational signatures and disease progression

Molecular Oncology, EarlyView.
In this explorative study, the abundance of circular RNA molecules in bone marrow stem cells was found to be elevated in patients with high‐risk myelodysplastic neoplasms, and to be associated with an increased risk of progression to acute myeloid leukemia.
Eileen Wedge, Morten Tulstrup, Gabriele Todisco, Pedro Moura, Christophe Côme, Jakob Werner Hansen, Jakob Schmidt Jespersen, Balthasar Schlotmann, Maria Creignou, Mette Dahl, Claudia Schöllkopf, Klas Raaschou‐Jensen, Krister Wennerberg, Bo Porse, Joachim Weischenfeldt, Eva Hellström‐Lindberg, Lasse Sommer Kristensen, Kirsten Grønbæk   +17 more
wiley   +1 more source

Predictive performance of front-loaded experimentation strategies in pharmaceutical discovery: a Bayesian perspective [PDF]

, 2004
Experimentation is a significant innovation process activity and its design is fundamental to the learning and knowledge build-up process. Front-loaded experimentation is known as a strategy seeking to improve innovation process performance; by ...
van Dyck, Walter
core