Results 181 to 190 of about 387,211 (278)

Chemoproteomic discovery of a brain‐penetrant, covalent NLRP3 inhibitor that binds a novel allosteric pocket

British Journal of Pharmacology, EarlyView.
NLRP3 is a promising inflammatory target, but existing inhibitors lack diversity and brain penetrance, and none are approved. Using chemoproteomics, we discovered a novel series that binds to Cys463 in a previously uncharacterized pocket. Compounds showed nanomolar potency, brain exposure, and in vivo suppression of IL‐1β, supporting neuroinflammatory ...
Donald C. Rogness, Evelyn P. Sievert, Vincent F. Vartabedian, Steffen M. Bernard, Erick Aitchison, William Tao, Mikaela Lindvall, Jing Qian, Christie L. Eissler, Brian E. Nordin, Benjamin D. Horning, Cian Kingston, Kelsey N. Lamb, Joshua C. Bell, Bingwen Lu, Jonathan Pollock, Jun Shi, Roli Khattri, David S. Weinstein, Matthew P. Patricelli, Brian N. Cook, Gabriel M. Simon   +21 more
wiley   +1 more source

Nonlinear energy consumption analysis of shallow-buried bias tunnel stability with improvement of failure mode. [PDF]

Sci Rep
Luo W, Liu S, Tao Z, Wang H, Gan X.
europepmc   +1 more source

Selective modulation of NaV channel gating counteracts aberrant hyperexcitability and rescues motor function and survival in a model of spinal muscular atrophy

British Journal of Pharmacology, EarlyView.
Background and Purpose Spinal muscular atrophy (SMA) is a motor neuron disease caused by SMN1 gene loss, leading to reduced survival motor neuron (SMN) protein and progressive motor neuron degeneration. Although SMN‐restoring therapies improve outcomes, residual disease burden and non‐curative efficacy underscore the need for complementary treatments ...
Fernanda C. Cardoso, Jessica A. I. Muller, Yougang Zhang, Jean Giacomotto   +3 more
wiley   +1 more source

The c‐Src inhibitor eCF506 diminishes opioid tolerance and reduces β‐arrestin2 recruitment

British Journal of Pharmacology, EarlyView.
Morphine activation of μ receptors causes tolerance through c‐Src activation and β‐arrestin2 recruitment. c‐Src inhibition or degradation reduces β‐arrestin2 recruitment, μ receptor endocytosis, while causing receptor upregulation, all likely contributing to reduced morphine tolerance.
Samuel Singleton, Fraser Nunn, Erika Lace, Álvaro Lorente‐Macías, Rachel Toth, Asier Unciti‐Broceta, Tim G. Hales   +6 more
wiley   +1 more source

Optimization of femtosecond laser spot coverage: analytical modeling of spatial frequencies, anisotropy, and saturation boundaries. [PDF]

Biomed Opt Express
Mosquera SA.
europepmc   +1 more source

Unraveling the active site cover of coproheme decarboxylase from Listeria monocytogenes

The FEBS Journal, EarlyView.
During heme biosynthesis in Gram‐positive bacteria, coproheme decarboxylase (ChdC) catalyzes the conversion of four‐propionate substrate coproheme to the two propionate product heme b. Its active site is universally covered by a flexible linking loop. This study identifies an important histidine residue, which stabilizes the loop in a ChdC homolog.
Nikolaus Falb, Dominik Hörtnagel, Chris Oostenbrink, Paul G. Furtmüller, Stefan Hofbauer   +4 more
wiley   +1 more source

Method for AFM investigation of lateral forces required for the surface detachment of neurites. [PDF]

Sci Rep
Braemer V, Paasche G.
europepmc   +1 more source

Directional information flow in human frataxin defines allosteric pathways connecting the hydrophobic core to the iron‐binding ridge

The FEBS Journal, EarlyView.
Human frataxin deficiency causes Friedreich's ataxia, yet how iron‐binding events are communicated across the protein is unclear. Using transfer entropy analysis of molecular dynamics simulations, we identify buried hydrophobic core leucines (LEU136, LEU140) as the source of directional signaling toward the iron‐binding acidic ridge.
Kevser Kübra Kırboğa, Ecir Uğur Küçüksille   +1 more
wiley   +1 more source

Emergence of form-independent direction selectivity in human V3A and MT. [PDF]

J Vis
Hong SW, Tong F.
europepmc   +1 more source

Three‐dimensional three‐interval thixotropy test (3D‐3ITT) protocol for cosmetic lotions: A proof‐of‐concept study linking thixotropy to sensory and emotional responses

International Journal of Cosmetic Science, EarlyView.
From rheology to emotion: 3D‐3ITT converts usage‐like shear histories into recovery maps and thixotropy index, TI3D. In a blinded half‐face study (N = 30), the higher‐ TI3D serum (S1s) improved absorption/clean feel and increased Relax and Comfort while lowering Anxiety relative to S2s.
Lihui Ye, Danning Zeng, Hua Sun, Yue Lv, Kaiwen Xiong, Jiaping Wang, Wenjia Zhou, Bin Zheng, Jean Yishi Chen, Guangwen He, Yuekui Sun   +10 more
wiley   +1 more source