Optimized psilocybin production in tryptophan catabolism‐repressed fungi
Here, we developed an in vivo psilocybin production chassis, based on repression of l‐tryptophan catabolism. By genome mining, we identified two aminotransferase ARO8/9 orthologs in Aspergillus nidulans involved in l‐tryptophan catabolism. Double deletion of the aminotransferase genes aroH1 and aroH2 resulted in a 10‐fold increased psilocybin ...
Slavica Janevska +12 more
wiley +1 more source
D1-like receptor activation improves PCP-induced cognitive deficits in animal models: Implications for mechanisms of improved cognitive function in schizophrenia [PDF]
YesPhencyclidine (PCP) produces cognitive deficits of relevance to schizophrenia in animal models. The aim was to investigate the efficacy of the D1-like receptor agonist, SKF-38393, to improve PCPinduced deficits in the novel object recognition (NOR ...
Abdul-Monim +84 more
core +1 more source
Neuroblastoma and its Target Therapies: A Medicinal Chemistry Review
Searching for a cure for neuroblastoma: This review highlights the urgent need to find a cure for high‐risk neuroblastoma. It provides an overview of the current treatment available and the drug discovery approach of seven drugs that reached clinical trial.
A. Gerges, U. Canning
wiley +1 more source
Novas metodologias sintéticas utilizando reator de micro-ondas fundamentadas nos princípios da química verde (azidas alílicas e reações de cicloadição) [PDF]
TCC (graduação) - Universidade Federal de Santa Catarina, Centro de Ciências Físicas e Matemáticas, Curso de Química.Este trabalho objetiva a preparação de compostos nitrogenados multifuncionais e de sistemas alílicos contendo o grupo azido, os quais são
Monteiro, Gustavo Claro
core
Ready access to 7,8-dihydroindolo[2,3-d][1]benzazepine-6(5H)-one scaffold and analogues via early-stage Fischer ring-closure reaction [PDF]
Irina Kuznetcova +4 more
openalex +1 more source
New Catalytic Routes to Benzofused Seven-Membered Azaheterocycles [PDF]
Benzazepines, benzodiazepines and benzoxazepines compose a privileged family of natural products and pharmaceuticals. Their remarkable biological activity made them useful drugs to treat a large variety of issues.
Velasco Rubio, Álvaro
core
We herein report the identification of UR‐NR435 (25), a SCH‐23390‐based fluorescent ligand bearing a 5‐TAMRA dye, as suitable for fluorescence microscopy at the D1R. Single‐digit nanomolar binding affinity could be determined in radioligand competition binding and molecular brightness studies at D1‐like receptors.
Niklas Rosier +11 more
wiley +1 more source
Q/R site interactions with the M3 helix in GluK2 kainate receptor channels revealed by thermodynamic mutant cycles [PDF]
RNA editing at the Q/R site near the apex of the pore loop of AMPA and kainate receptors controls a diverse array of channel properties, including ion selectivity and unitary conductance and susceptibility to inhibition by polyamines and cis-unsaturated ...
Boland +67 more
core +2 more sources
A suitable preparation of N-sulfonyl-1,2,3,4-tetrahydroisoquinolines and their ring homologs with a reusable Preyssler heteropolyacid as catalyst [PDF]
The preparation of N-sulfonyl-1,2,3,4-tetrahydroisoquinolines, N-sulfonyl-2,3,4,5-tetrahydro-1H-2-benzazepines and N-sulfonyl-1,2,3,4,5,6-hexahydrobenzazocine was catalyzed by a Preyssler heteropolyacid, H₁₄[NaP₅W₃₀O₁₁₀], (PA), supported on silica ...
Autino, Juan Carlos +3 more
core +1 more source
One-Pot Phosphate-Mediated Synthesis of Novel 1,3,5-Trisubstituted Pyridinium Salts: A New Family of S. aureus Inhibitors [PDF]
Polysubstituted pyridinium salts are valuable pharmacophores found in many biologically active molecules. Their synthesis typically involves the use of multistep procedures or harsh reaction conditions.
Edwards, M +4 more
core +1 more source

