Results 111 to 120 of about 259,085 (245)

The Natural Product Corramycin Acts as a DNA Gyrase Poison and Overcomes Fluoroquinolone Resistance in Mycobacterium tuberculosis

Advanced Science, EarlyView.
Corramycin, a myxobacterial natural product antibiotic, exhibits potent bactericidal activity against multidrug‐resistant Mycobacterium tuberculosis. The compound hijacks bacterial transporters such as BacA and OppABCD to enter the cell and inhibits DNA synthesis through a previously unrecognized mode of DNA gyrase poisoning, locking the enzyme in an ...
Franziska Fries, Jennifer Herrmann, Michael Dal Molin, Yaëlle Wormser, Timo Risch, Yunsheng Gao, Gareth Prosser, Francesca Gubellini, Ariel Mechaly, Joshua B. Wallach, Anthony Castro, Arka Banerjee, Sari Rasheed, Alexander Horn, Mathias Müsken, Michael Kurz, Lindsay Sonnenkalb, Viola Dreyer, Stefan Niemann, Sönke Andres, Dirk Schnappinger, Uli Kazmaier, Norbert Reiling, Rolf Müller, Jan Rybniker, Stéphanie Petrella   +25 more
wiley   +1 more source

A Novel Pak1 Activator Ameliorates ER Stress for HFpEF Therapy

Advanced Science, EarlyView.
Chronic metabolic stress is a major contributor to HFpEF progression. Under prolonged metabolic stress, Pak1 activity becomes impaired, contributing to disrupted ER proteostasis, cardiomyocyte apoptosis, fibrosis, and diastolic dysfunction. Mechanistically, Pak1 overexpression activates the ERK1/2–MNK1–eIF4E signaling axis, promotes translational ...
Honglin Xu, Hongyuan Zhang, Tayyiba Azam, Susanne S. Hille, Yingjuan Liu, Min Zi, Jiaqing Lang, He Yu, Yujia Cao, Bernard D. Keavney, Tamer M. A. Mohamed, Jessica M. Miller, Riham R. E. Abouleisa, Ming Xu, Elizabeth J. Cartwright, Oliver J. Müller, Ming Lei, Xin Wang   +17 more
wiley   +1 more source

Serine proteases and protease‐activated receptor 2 mediate the proinflammatory and algesic actions of diverse stimulants [PDF]

, 2014
Background and purposeAlthough serine proteases and agonists of protease-activated receptor 2 (PAR2) cause inflammation and pain, the spectrum of proteases that are activated by proinflammatory and algesic stimuli and their contribution to inflammatory ...
Cottrell, GS, Bunnett, NW, Kirkwood, K, Cattaruzza, F, Murphy, JE, Knecht, W, Bogyo, M, Amadesi, S, Lyo, V, Carlsson, JF   +9 more
core   +1 more source

Repurposing a Small Molecule Plant Hormone as a Tunable ON‐Switch for CAR‐T Cell Immunotherapy

Advanced Science, EarlyView.
By engineering a receptor system integrating the plant auxin receptor AFB1 with its co‐receptor IAA7, we enable ligand‐dependent interactions triggered by the plant hormone auxins. This design allows rapid, reversible, and dose‐dependent T cell activation, resulting in potent cytotoxicity against B‐cell lymphoma in vitro and in vivo.
Hongxiang Zeng, Lei Zheng, Rongkun Tao, Sirui Zheng, Yanke Zhong, Yongxia Niu, Peng Zhang, Xiang Ma, Chen Yang, Min Zhang, Fuyu Duan, Jing Yang, Xuan Wei, Xiang Zhou, Zhenbiao Yang, Zhaoxi Sun, Qizhou Lian   +16 more
wiley   +1 more source

Serine proteases in bone disease

, 2009
Serine proteases are active in many physiological and pathological processes within bone tissue. Although essential to adequate maintenance of bone and cartilage, their inappropriate expression can lead to exacerbation of tissue destruction and ...
Timson, David J., Bouteldja, Nadia, Bouteldja, N., Timson, D.J., David Timson, Nadia Bouteldja   +5 more
core   +1 more source

VlPAG/DRN Microglia Drive Neuropathic Pain‐Induced Depression via a Defined Neuroimmune Axis

Advanced Science, EarlyView.
Peripheral nerve injury (SNI) induces neuropathic pain, activates midbrain microglia, and triggers an NLRP3–IL‐1β–dependent inflammatory cascade. IL‐1β signals through IL‐1R1 on vlPAG/DRN VGLUT2+ neurons (vlPAG/DRNGlu), inducing hyperexcitability and driving the vlPAG/DRNGlu→BNSTGABA circuit to produce the affective component of neuropathic pain ...
Jing Yang, Bing‐Jie Tang, Jia‐Yi Li, Shu‐Lan Xie, Shumin Duan, Junping Chen, Shengmei Zhu, Zhen‐Zhong Xu   +7 more
wiley   +1 more source

Serine proteases at the cutting edge of IBD: Focus on gastrointestinal inflammation

, 2020
International audienceSerine proteases have been long recognized to coordinate many physiological processes and play key roles in regulating the inflammatory response.
Mkaouar, Héla, Jablaoui, Amin, Akermi, Nizar, Maguin, Emmanuelle, Rhimi, Moez, Kriaa, Aicha   +5 more
core   +1 more source

Nucleoside‐Modified mRNA Encoding Alpha‐Galactosidase A Ameliorates Fabry Disease Phenotypes in Human IPSC‐Derived Cardiomyocytes

Advanced Science, EarlyView.
Human iPSC‐derived Fabry cardiomyocytes exhibited broad transcriptional dysregulation, apoptosis, mitochondrial dysfunction, impaired reactive oxygen species handling, altered contractility, and abnormal calcium transient decay, potentially mediated by phospholamban hyperphosphorylation.
Malte Juchem, Lea Oehlsen, Sedef Ersoy, Jia Li Ye, Natalie Weber, Elisa Mohr, Wilson Agyapong, Junqing Liu, Maximilian Fuchs, Ke Xiao, Christopher Jahn, Reto Eggenschwiler, Tobias Cantz, Julia Beimdiek, Falk F. R. Buettner, Theresia Kraft, Jan Hegermann, Ivonne J. Knorr, Lisa Ernst, Linda Feldbrügge, Resa Puffert, Kevin Schmidt, Christian Bär, Jeannine Hoepfner, Thomas Thum   +24 more
wiley   +1 more source

Selective Modulation of OTUB1 Noncanonical Function via a bioPhosTAC Strategy

Advanced Science, EarlyView.
This work positions the versatile performance of the peptide‐based bioPhosTAC platform for dissecting phosphorylation‐dependent biology and expanding the scope of induced‐proximity technologies. We demonstrated that selective manipulation of a tyrosine phosphorylation site is sufficient to propagate coordinated cellular consequences.
Seung Un Seo, Seon Min Woo, Minhyeong Choi, Soeun Rhee, Simmyung Yook, Donghyuk Shin, Kwang‐Su Park, Taeg Kyu Kwon   +7 more
wiley   +1 more source

Membrane-Anchored Serine Proteases in Vertebrate Cell and Developmental Biology

, 2011
Analysis of vertebrate genome sequences at the turn of the millennium revealed that a vastly larger repertoire of enzymes execute proteolytic cleavage reactions within the pericellular and extracellular environments than was anticipated from biochemical
Thomas H. Bugge, Roman Szabo
core   +1 more source