Results 71 to 80 of about 84,342 (322)

Discovery of a Novel and Potent Kir4.1 Inhibitor as a Safe and Rapid‐Onset Antidepressant Agent in Mice

Advanced Science, EarlyView.
The preferred derivative JX3212 demonstrates strong inhibitory activity against Kir4.1 with favorable druggability and shows significant antidepressant efficacy in vivo. Abstract Major depressive disorder is a serious psychiatric disorder for which novel and fast‐acting antidepressants are required.
Sisi Wang, Xiaoyu Zhou, Mengdan Li, Chao Zhang, Haiyan Xu, Jingyi He, Li Zhan, Yueling Gu, Hao Gu, Tianyu Tu, Hanfang Liu, Taotao Lu, Yueming Zheng, Jian Li, Zhaobing Gao, Yixiang Xu   +15 more
wiley   +1 more source

Acid‐ and Nucleophile‐Gated Photoisomerization of Phosphaindirubin

Angewandte Chemie, EarlyView.
Triply gated isomerization: In polar solvents, a phosphorus‐containing indirubin photoswitch undergoes visible‐light‐driven Z→E isomerization only when protonated, and reverts thermally via nucleophile‐catalyzed back‐isomerization. This three‐way control by light, acid, and nucleophile enables reversible photoisomerization.
Jacob Jan van der Wal, Jorn D. Steen, Ann‐Kathrin Rückert, Roman Yu. Peshkov, Michiel F. Hilbers, P. Tim Prins, Wybren Jan Buma, Andreas Orthaber, Stefano Crespi   +8 more
wiley   +2 more sources

(2,4-Dichlorophenyl)(3-hydroxypiperidin-1-yl)methanone: crystal structure and Hirshfeld analysis

IUCrData, 2017
In the title compound, C12H13Cl2NO2, the piperidine ring adopts a chair conformation. The dihedral angle between the mean plane of the piperidine ring and the benzene ring is 58.5 (3)°.
U. Mohamooda Sumaya, D. Reuben Jonathan, Dravida Thendral Era, S. Gomathi, G. Usha   +4 more
doaj   +1 more source

Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s) [PDF]

, 2015
ACKNOWLEDGMENTS The work was supported by National Institutes of Health grants DA027113 and EY024717 to G.A.T. and DA09158 to A.M. A portion of this work was submitted in 2011 by A. Kulkarni in partial fulfillment of M.S.
Cascio, Maria G., Denovan-Wright, Eileen M., Janero, David R., Korde, Anisha, Kulkarni, Abhijit R., Kulkarni, Pushkar M., Laprairie, Robert B., Makriyannis, Alexandros, Pertwee, Roger G., Thakur, Ganesh A., Tichkule, Ritesh B., Zhou, Han, Zvonok, Nikolai   +12 more
core   +3 more sources

Ir(III) Complexes Convert Cold to Hot Tumors via Ferroptosis/Necroptosis‐Driven Immunogenic Cell Death and Photosensitized CD47 Downregulation

Advanced Science, EarlyView.
Red‐light‐activated Ir1 overcomes hypoxia tolerance and adapts to the immunosuppressive tumor microenvironment, converting immunologically cold tumors into inflamed hot microenvironments. This conversion is driven by synergistic induction of immunogenic cell death through coordinated ferroptosis‐necroptosis pathways and spatiotemporally controlled ...
Long‐Bo Yu, Peng Wang, Qing‐Hua Shen, Qi‐Xin Guan, Zhi‐Yuan Li, Ying‐Ying Han, Xin‐Yi Zhang, Qing‐Yuan Hu, Cai‐Ping Tan   +8 more
wiley   +1 more source

Macrocyclic Molecular Glues for the 14‐3‐3/ChREBP Interaction: Affinity and Cooperativity in an Inverse Relationship

Angewandte Chemie, EarlyView.
Macrocycles are effective molecular glues to stabilize the 14‐3‐3/ChREBP interaction. Linker length modulation uncovered an inverse correlation between the macrocycle binding affinity to 14‐3‐3 and its cooperativity in 14‐3‐3/ChREBP stabilization.
Marloes A. M. Pennings, Merel A. W. van den Bosch, Ansgar Oberheide, Carlo J. A. Verhoef, Christian Ottmann, Albert J. Markvoort, Galen P. Miley, Luc Brunsveld   +7 more
wiley   +2 more sources

Crystal structure of 3-methyl-2,6-bis(4-methyl-1,3-thiazol-5-yl)piperidin-4-one

Acta Crystallographica Section E, 2014
In the title compound, C14H17N3OS2, the central piperidinone ring adopts a chair conformation and the thiazole rings are inclined to its mean plane by 80.16 (12) and 67.15 (12)°.
A. Manimaran, K. Sethusankar, S. Ganesan, S. Ananthan   +3 more
doaj   +1 more source

Epoxysuccinyl peptide-derived cathepsin B inhibitors: Modulating membrane permeability by conjugation with the C-terminal heptapeptide segment of penetratin [PDF]

, 2002
Besides its physiological role in lysosomal protein breakdown, extralysosomal cathepsin B has recently been implicated in apoptotic cell death. Highly specific irreversible cathepsin B inhibitors that are readily cellpermeant should be useful tools to ...
Assfalg-Machleidt, Irmgard, Deluca, Dominga, Höhneke, Clara, Machleidt, Werner, Schaschke, Norbert, Sommerhoff, Christian P.   +5 more
core   +1 more source

Sodium piperidine-1-carbodithioate dihydrate [PDF]

Acta Crystallographica Section E Structure Reports Online, 2011
The asymmetric unit of the title compound, Na(+)·C(6)H(10)NS(2) (-)·2H(2)O, is composed of a sodium cation, a piperidine-dithio-carbamate anion which exhibits positional disorder, and two lattice water mol-ecules. The atoms of the piperidine ring are divided over two sites with occupancy factors of 0.554 (6) and 0.446 (6).
Ana C. Mafud, Maria Teresa P. Gambardella   +1 more
openaire   +3 more sources

Advanced Human Immune Cell‐Organoid Co‐Cultures for Functional Testing of Cancer Nanovaccines

Advanced Science, EarlyView.
Pancreatic ductal adenocarcinoma remains difficult to treat. We establish an organoid–immune co‐culture using patient‐derived organoids and matched T‐cells to assess cancer vaccines. A mesothelin‐targeted nanovaccine activates antigen‐specific T‐cells, increases IFN‐γ, and targets MSLN+ organoids.
Nathalia Ferreira, David Agorku, Andre Rosa, Julia Roosz, Lena Christ, Nicole Anderle, Ajinkya Kulkarni, Abir Hussein, Sana S. Sayedipour, Omar F. Luna, Tobias Legler, Philipp Ströbel, Fernando Albericio, Luis Cruz, Phillipp Beckhove, Peter Loskill, Frauke Alves, M. Andrea Markus, Fernanda Ramos‐Gomes   +18 more
wiley   +1 more source