Results 71 to 80 of about 1,513,260 (338)

Mechanistic basis for inhibition of the extended‐spectrum β‐lactamase GES‐1 by enmetazobactam and tazobactam

FEBS Letters, EarlyView.
Antimicrobial resistance (AMR) is of huge importance, resulting in over 1 million deaths each year. Here, we describe how a new drug, enmetazobactam, designed to help fight resistant bacterial diseases, inhibits a key enzyme (GES‐1) responsible for AMR. Our data show it is a more potent inhibitor than the related tazobactam, with high‐level computation
Michael Beer, Philip Hinchliffe, Marko Hanževački, Christopher R. Bethel, Catherine L. Tooke, Marc W. Van der Kamp, Krisztina M. Papp‐Wallace, Robert A. Bonomo, Stuart Shapiro, Adrian J. Mulholland, James Spencer   +10 more
wiley   +1 more source

Pathologically Activated Neuroprotection via Uncompetitive Blockade of \u3cem\u3eN\u3c/em\u3e-Methyl-d-aspartate Receptors with Fast Off-rate by Novel Multifunctional Dimer Bis(propyl)-cognitin [PDF]

, 2010
Uncompetitive N-methyl-d-aspartate (NMDA) receptor antagonists with fast off-rate (UFO) may represent promising drug candidates for various neurodegenerative disorders.
Fu, Hongjun, Han, Yifan, Huang, Pingbo, Li, Chaoying, Li, Fushun, Li, Wenming, Luo, Jialie, Ma, Dik-Lung, Pang, Yuanping, Peoples, Robert W., Tang, Jing, Wang, Qinwen, Xia, Jun, Zhao, Yuming   +13 more
core   +1 more source

Novel and unscrutinized immune entities of the zebrafish gut

FEBS Letters, EarlyView.
Understudied cells of the zebrafish immune system include bona fide immune cells and epithelial (‐derived) cells with immune functions. Research focusing on zebrafish cells which demonstrate similarities to mammalian immune cell counterparts may help us understand the pathologies in which they are implicated. Currently available and advanced tools make
Audrey Inge Schytz Andersen‐Civil, Marine Mantel, Julia Soh, Serge Mostowy, Sylvia Brugman, Gilles Claude Vanwalleghem   +5 more
wiley   +1 more source

Orexin-Corticotropin-Releasing Factor Receptor Heteromers in the Ventral Tegmental Area as Targets for Cocaine [PDF]

, 2015
Release of the neuropeptides corticotropin-releasing factor (CRF) and orexin-A in the ventral tegmental area (VTA) play an important role in stress-induced cocaine-seeking behavior.
Aguinaga, David, Cai, Ning-Sheng, Canela, Enric I, Casadó, Vicent, Cortés, Antonio, Ferré, Sergi, Hausch, Felix, Howell, Lesley A., Lluís, Carme, Mallol, Josefa, McCormick, Peter J., McDowell, Kimberly, Moreno, Estefanía, Moreno-Delgado, David, Navarro, Gemma, Quiroz, César, Rea, William, Sierakowiak, Adam   +17 more
core   +1 more source

From lactation to malignancy: A comparison between healthy and cancerous breast gland at single‐cell resolution reveals new issues for tumorigenesis

FEBS Letters, EarlyView.
Single‐cell RNA sequencing reveals an opposite role of SLPI in basal tumors based on metastatic spread, along with shared activation of specific regulons in cancer cells and mature luminal lactocytes, as well as downregulation of MALAT1 and NEAT1 in the latter.
Pietro Ancona, Carlo M. Bergamini, Carlo Ferrari, Stefano Volinia, Nicoletta Bianchi   +4 more
wiley   +1 more source

Imeglimin attenuates liver fibrosis by inhibiting vesicular ATP release from hepatic stellate cells

FEBS Letters, EarlyView.
Imeglimin, at clinically relevant concentrations, inhibits vesicular ATP accumulation and release from hepatic stellate cells, thereby attenuating purinergic signaling and reducing fibrogenic activation. This mechanism reveals a newly identified antifibrotic action of imeglimin beyond glycemic control.
Seiji Nomura, Lixiang Wang, Nao Hasuzawa, Ayako Nagayama, Sawako Moriyama, Kenji Ashida, Yoshinori Moriyama, Masatoshi Nomura, Ken Yamamoto   +8 more
wiley   +1 more source

Cancer cell death induced by the NAD antimetabolite Vacor discloses the antitumor potential of SARM1

FEBS Letters, EarlyView.
Vacor, a compound converted into the toxic metabolite Vacor adenine dinucleotide (VAD) by the nicotinamide salvage pathway enzymes NAMPT and NMNAT2, exhibits antitumor activity by inducing rapid and complete NAD depletion. We report that Vacor toxicity is limited to cell lines expressing high levels of SARM1, a NAD glycohydrolase.
Giuseppe Ranieri, Andrea Lapucci, Giuseppe Orsomando, Nadia Raffaelli, Alberto Chiarugi, Daniela Buonvicino   +5 more
wiley   +1 more source

RAD50 missense variants differentially affect the DNA damage response and mitotic progression

FEBS Letters, EarlyView.
RAD50 incorporates into the MRN complex and initiates the DNA damage response. Furthermore, RAD50 promotes mitotic progression. RAD50 missense variants capable of forming an MRN complex supported the DNA damage response and mitotic features to different extents in complementation experiments, indicating these functions are separable and might impact ...
Hanna Redeker, Swantje Kebel, Lea Völkening, Anna Vatselia, Louisa Weinhold, Girmay Asgedom, Axel Schambach, Detlev Schindler, Thilo Dörk, Kristine Bousset   +9 more
wiley   +1 more source

Mapping the evolution of mitochondrial complex I through structural variation

FEBS Letters, EarlyView.
Respiratory complex I (CI) is crucial for bioenergetic metabolism in many prokaryotes and eukaryotes. It is composed of a conserved set of core subunits and additional accessory subunits that vary depending on the organism. Here, we categorize CI subunits from available structures to map the evolution of CI across eukaryotes. Respiratory complex I (CI)
Dong‐Woo Shin, Tingting Chen, James A. Letts   +2 more
wiley   +1 more source

Use of Premixed Pethidine and Antagonists in Obstetrical Analgesia [PDF]

, 1959
John D. Bullough
openalex   +1 more source