Results 81 to 90 of about 16,181 (141)
Proteome‐Wide Profiling of Olaparib Interactors Using a Biotinylated Photoaffinity Probe
Novel interactors found for olaparib: Olaparib is an important anti‐cancer drug in BRCA‐mutated cancers. In this study, we identified novel interactors for olaparib using photoaffinity labeling. We designed a biotinylated photoaffinity probe and used it in a proteomic screening to discover a broad range of olaparib interactors, including previously ...
Femke L. A. M. van der Heijden+5 more
wiley +1 more source
Patient-derived mouse models of cancer need to be orthotopic in order to evaluate targeted anti-metastatic therapy. [PDF]
Patient-derived xenograft (PDX) mouse models of cancer are emerging as an important component of personalized precision cancer therapy. However, most models currently offered to patients have their tumors subcutaneously-transplanted in immunodeficient ...
Bouvet, Michael+10 more
core +2 more sources
Synthesis and Preliminary Evaluation of Tanshinone Mimic Conjugates for Mechanism of Action Studies
A small array of Tanshinone Mimics (TM) probes with a detection‐promoting moiety (either a photoaffinity probe ‐ PAP or biotin) has been synthesized for mechanism of action (MoA) studies on Human antigen R (HuR). Biological and biochemical assays were used to characterize the novel TM conjugates.
Giulia Assoni+5 more
wiley +1 more source
Given the essential role of protein‐protein interactions (PPIs) in cellular signalling pathways their selective modulation is of great therapeutic interest. Mimicry of secondary structural protein elements has emerged as a promising strategy, with various scaffolds reproducing recognition surfaces of α‐helical and β‐strand/sheet proteins.
James Luccarelli+4 more
wiley +1 more source
4-Iodo-N-(o-tolylsulfonyl)benzamide
The title compound, C14H12INO3S, crystallizes with two independent molecules (A and B) in the asymmetric unit. The dihedral angle between the two aryl rings is 83.1 (4)° in molecule A and 79.8 (4)° in molecule B.
S. Naveen+5 more
doaj +1 more source
para-Selective C-H amidation of simple arenes with nitriles [PDF]
A para-selective C-H amidation of simple arenes with nitriles has been developed. By increasing the amount of arenes, a further meta-selective C-H arylation of the produced amides occurred.
Allen+59 more
core +2 more sources
Energy Transfer Catalysis Enabled 2,2,2‐Trifluoroethoxy‐Amination of Olefins
A thioxanthone‐catalyzed 2,2,2‐trifluoroethoxyamination of olefins is developed using unprecedented, easily prepared, and bench‐stable oxime ethers via the generation of alkoxy and iminyl radicals. The controlled intermolecular addition of the alkoxy radical to an olefin, over possible competing side processes, is critical.
Floriane Doche+3 more
wiley +1 more source
Isoxazole derivatives (isoxazoles, isoxazolines, and isoxazolidines) are present in the structure of several natural products and/or pharmaceutically interesting compounds.
Konstantinos A. Ouzounthanasis+3 more
doaj +1 more source
2-Amino-N-(2-chloropyridin-3yl)benzamide
The title compound, C12H10ClN3O, is a condensation product of 3-amino-2-chloropyridine and ethyl 2-aminobenzoate in which the aromatic rings are almost coplanar [dihedral angle = 2.28 (9)°] and an intramolecular N—H...O hydrogen bond occurs.
Noura M. Riad+2 more
doaj +1 more source
1,2,6-thiadiazinones as novel narrow spectrum calcium/calmodulin-dependent protein kinase kinase 2 (CaMKK2) inhibitors [PDF]
We demonstrate for the first time that 4H-1,2,6-thiadiazin-4-one (TDZ) can function as a chemotype for the design of ATP-competitive kinase inhibitors. Using insights from a co-crystal structure of a 3,5-bis(arylamino)-4H-1,2,6-thiadiazin-4-one bound to ...
Asquith, Christopher R.M.+11 more
core +3 more sources