Results 61 to 70 of about 645,880 (357)

Small-Molecule Positive Allosteric Modulators of the β2-Adrenoceptor Isolated from DNA-Encoded Libraries

Molecular Pharmacology, 2018
Conventional drug discovery efforts at the β2-adrenoceptor (β2AR) have led to the development of ligands that bind almost exclusively to the receptor’s hormone-binding orthosteric site.
Seungkirl Ahn, Biswaranjan Pani, Alem W. Kahsai, E. K. Olsen, Gitte Husemoen, Mikkel Vestergaard, Lei Jin, Shuai Zhao, L. Wingler, Paula K. Rambarat, Rishabh K. Simhal, Thomas T Xu, Lillian D. Sun, Paul J. Shim, D. Staus, Li-Yin Huang, T. Franch, Xin Chen, R. Lefkowitz   +18 more
semanticscholar   +1 more source

Multiple ETS family transcription factors bind mutant p53 via distinct interaction regions

FEBS Letters, EarlyView.
Mutant p53 gain‐of‐function is thought to be mediated by interaction with other transcription factors. We identify multiple ETS transcription factors that can bind mutant p53 and found that this interaction can be promoted by a PXXPP motif. ETS proteins that strongly bound mutant p53 were upregulated in ovarian cancer compared to ETS proteins that ...
Stephanie A. Metcalf, Nicholas F. Downing, Kaitlyn M. Mills, Samuel C. Metcalfe, Alexander E. Kritzer, Lindsey D. Mayo, Peter C. Hollenhorst   +6 more
wiley   +1 more source

Phenylalanine‐Based DNA‐Encoded Chemical Libraries for the Discovery of Potent and Selective Small Organic Ligands Against Markers of Cancer and Immune Cells

Advanced Science
DNA‐encoded chemical libraries (DELs) are powerful tools for drug discovery, enabling the high‐throughput screening of vast libraries of small molecules against target proteins of pharmaceutical interest.
Francesca Migliorini, Andrea Ciamarone, Sheila Dakhel Plaza, Tony Georgiev, Marta Mascellani, Emanuela Sabato, Giulio Vistoli, Ilaria Biancofiore, Nicholas Favalli, Emanuele Puca, Sebastian Oehler, Dario Neri, Samuele Cazzamalli   +12 more
doaj   +1 more source

DNA display II. Genetic manipulation of combinatorial chemistry libraries for small-molecule evolution.

PLoS Biology, 2004
Biological in vitro selection techniques, such as RNA aptamer methods and mRNA display, have proven to be powerful approaches for engineering molecules with novel functions.
David R Halpin, Pehr B Harbury
doaj   +1 more source

Exhaustive Search of Ligand Binding Pathways via Volume-based Metadynamics

, 2019
Determining the complete set of ligands' binding/unbinding pathways is important for drug discovery and to rationally interpret mutation data. Here we have developed a metadynamics-based technique that addressed this issue and allows estimating ...
Capelli, Riccardo, Carloni, Paolo, Parrinello, Michele   +2 more
core   +1 more source

Single-domain antibodies and their formatting to combat viral infections [PDF]

, 2018
Since their discovery in the 1990s, single-domain antibodies (VHHs), also known as NanobodiesA (R), have changed the landscape of affinity reagents. The outstanding solubility, stability, and specificity of VHHs, as well as their small size, ease of ...
Ballegeer, Marlies, De Vlieger, Dorien, Rossey, Iebe, Saelens, Xavier, Schepens, Bert   +4 more
core   +2 more sources

Cell wall target fragment discovery using a low‐cost, minimal fragment library

FEBS Letters, EarlyView.
LoCoFrag100 is a fragment library made up of 100 different compounds. Similarity between the fragments is minimized and 10 different fragments are mixed into a single cocktail, which is soaked to protein crystals. These crystals are analysed by X‐ray crystallography, revealing the binding modes of the bound fragment ligands.
Kaizhou Yan, Mathew Stanley, Olawale Raimi, Andrew T. Ferenbach, Helge C Dorfmueller, Daan M. F. van Aalten   +5 more
wiley   +1 more source

Temperature-related intensity change (TRIC)-based high-throughput screening enables the discovery of small molecule CD28 binders

SLAS Discovery
CD28 is a pivotal costimulatory receptor involved in T cell activation and immune regulation, positioning it as a key therapeutic target for inflammatory diseases, including inflammatory bowel disease (IBD).
Laura Calvo-Barreiro, Saurabh Upadhyay, Moustafa T. Gabr   +2 more
doaj   +1 more source

Nanopipettes as Monitoring Probes for the Single Living Cell: State of the Art and Future Directions in Molecular Biology. [PDF]

, 2018
Examining the behavior of a single cell within its natural environment is valuable for understanding both the biological processes that control the function of cells and how injury or disease lead to pathological change of their function.
Bulbul, Gonca, Chaves, Gepoliano, Olivier, Joseph, Ozel, Rifat Emrah, Pourmand, Nader   +4 more
core   +2 more sources

Inhibiting stearoyl‐CoA desaturase suppresses bone metastatic prostate cancer by modulating cellular stress, mTOR signaling, and DNA damage response

FEBS Letters, EarlyView.
Bone metastasis in prostate cancer (PCa) patients is a clinical hurdle due to the poor understanding of the supportive bone microenvironment. Here, we identify stearoyl‐CoA desaturase (SCD) as a tumor‐promoting enzyme and potential therapeutic target in bone metastatic PCa.
Alexis Wilson, Mackenzie K Herroon, Shane Mecca, Laimar C Garmo, Jacob Lindquist, Shrila Rajendran, Steve M. Patrick, Izabela Podgorski   +7 more
wiley   +1 more source