Results 111 to 120 of about 358,313 (362)

Inhibition of Serine Proteases by Arylboronic Acids [PDF]

Proceedings of the National Academy of Sciences, 1971
Arylboronic acids were found to be strong competitive inhibitors of subtilisin and chymotrypsin. The binding constants are strongly pH dependent and give a Hammett-type plot with a slope of -0.885. The pH dependence, the Hammett plot, and nmr model-system studies indicate that inhibition is due to electron-pair donation by the active site histidine to ...
Manfred Philipp, Myron L. Bender
openaire   +3 more sources

Bilirubin Targeting WNK1 to Alleviate NLRP3‐Mediated Neuroinflammation

Advanced Science, EarlyView.
At physiological concentrations, bilirubin binds to the kinase domain of WNK1, thereby augmenting its activity and facilitating the phosphorylation of downstream SPAK/OSR1. This phosphorylation inhibits KCC2 activity, leading to elevate intracellular chloride levels in neurons.
Linfei Mao, Jiayu Lu, Quanjun Yang, Zhenqi Liu, Cuiping Wu, Bingbing Ke, Kaiyan Su, Haolin Yuan, Yaqi Cui, Yao Wang, Richard Salvi, Guang Yang, Shankai Yin, Feng Liu, Chunyan Li   +14 more
wiley   +1 more source

Enterohemorrhagic E. coli (EHEC)—Secreted Serine Protease EspP Stimulates Electrogenic Ion Transport in Human Colonoid Monolayers

Toxins, 2018
One of the characteristic manifestations of Shiga-toxin-producing Escherichia coli (E. coli) infection in humans, including EHEC and Enteroaggregative E. coli O104:H4, is watery diarrhea. However, neither Shiga toxin nor numerous components of the type-3
C. Ming Tse, Julie G. In, Jianyi Yin, Mark Donowitz, Michele Doucet, Jennifer Foulke-Abel, Fernando Ruiz-Perez, James P. Nataro, Nicholas C. Zachos, James B. Kaper, Olga Kovbasnjuk   +10 more
doaj   +1 more source

Dysregulation of protease and protease inhibitors in a mouse model of human pelvic organ prolapse. [PDF]

PLoS ONE, 2013
Mice deficient for the fibulin-5 gene (Fbln5(-/-)) develop pelvic organ prolapse (POP) due to compromised elastic fibers and upregulation of matrix metalloprotease (MMP)-9.
Madhusudhan Budatha, Simone Silva, Teodoro Ignacio Montoya, Ayako Suzuki, Sheena Shah-Simpson, Cecilia Karin Wieslander, Masashi Yanagisawa, Ruth Ann Word, Hiromi Yanagisawa   +8 more
doaj   +1 more source

Characterization of the Hemagglutinin Cleaving Transmembrane Serine Proteases Matriptase and TMPRSS2 [PDF]

, 2019
Influenza is one of the commonest infectious diseases affecting millions of people every year including 290,000 – 650,000 heavy casualties. Influenza viruses undergo constant genetic changes and every 10 – 50 years new influenza virus strains emerge that
Keils, Aline
core   +1 more source

Advancing the Identification of Bioactive Molecules and the Construction of a Synergistic Drug Delivery System in Combating Lung Injury

Advanced Science, EarlyView.
Traditional Chinese Medicine (TCM), while holistic and historically esteemed, faces challenges in “miracle cures” due to slow onset, long cycles, and difficulty controlling quality. This study obtains the active ingredients, glabridin (GLA) and puerarin (PUE), from Ge‐Gen Decoction (GGD), developing a safe and effective drug delivery system, GLA‐PUE ...
Jianhong Qi, Yanxia Wang, Huan Chen, Kaitian Wu, Pei Zhou, Yue Dou, Bingqi Xiong, Wei Zhou   +7 more
wiley   +1 more source

Pollens destroy respiratory epithelial cell anchors and drive alphaherpesvirus infection [PDF]

, 2019
Pollens are well-known triggers of respiratory allergies and asthma. The pollen burden in today's ambient air is constantly increasing due to rising climate change and air pollution.
Gevaert, Kris, Impens, Francis, Laval, Kathlyn, Nauwynck, Hans, Poelaert, Katrien, Van Cleemput, Jolien, Van Den Broeck, Wim   +6 more
core   +3 more sources

PCSK9 Promotes the Malignancy of Triple‐negative Breast Cancer Cells by Reducing Cholesterol Levels at the Plasma Membrane to Activate EGFR and HER3

Advanced Science, EarlyView.
By decreasing cholesterol and lipid raft levels in the plasma membrane, proprotein convertase subtilisin/kexin type 9 (PCSK9) boosts human epidermal growth factor receptor 1 and 3 (EGFR and HER3) activation, driving tumor growth and metastasis in triple‐negative breast cancer (TNBC).
Tianhong Li, Renfei Wu, Kathy Qian Luo
wiley   +1 more source

Novel bi- and trifunctional inhibitors of tumor-associated proteolytic systems [PDF]

, 2003
Serine proteases, cysteine proteases, and matrix metalloproteinases (MMPs) are involved in cancer cell invasion and metastasis. Recently, a recombinant bifunctional inhibitor (chCysuPA(19-31)) directed against cysteine proteases and the urokinasetype ...
Brew K., Kitts P.A., Kos J., Kotzsch M., Lah T.T., Magdolen U., Possee R.D., Rabbani S.A., Reuning U., Stetler-Stevenson W.G., Szpaderska A.M., Thomas C.J.   +11 more
core   +2 more sources

α‐Synuclein Pathology Spreads in a Midbrain–Hindbrain Assembloid Model

Advanced Science, EarlyView.
A novel midbrain–hindbrain assembloid model demonstrates the spread of α‐synuclein pathology, a hallmark of Parkinson's disease, mimicking Braak's hypothesis. This model reveals how pathology propagates from the hindbrain to the midbrain, inducing synaptic changes and early signs of neuronal vulnerability. It offers an innovative platform for exploring
Gemma Gomez‐Giro, Daniela Frangenberg, Daniela Vega, Alise Zagare, Kyriaki Barmpa, Paul M. A. Antony, Graham Robertson, Rahman Sabahi‐Kaviani, Kristian Haendler, Nathalie Kruse, Florentia Papastefanaki, Rebecca Matsas, Malte Spielmann, Regina Luttge, Jens C. Schwamborn   +14 more
wiley   +1 more source