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G7127

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Bing Wang et al.
Nucleic acids research, 49(15), 8822-8835 (2021-08-06)
The catalytic subunit of SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) contains two active sites that catalyze nucleotidyl-monophosphate transfer (NMPylation). Mechanistic studies and drug discovery have focused on RNA synthesis by the highly conserved RdRp. The second active site, which resides in
Manoj K Rathinaswamy et al.
Science advances, 7(35) (2021-08-29)
The class IB phosphoinositide 3-kinase (PI3K), PI3Kγ, is a master regulator of immune cell function and a promising drug target for both cancer and inflammatory diseases. Critical to PI3Kγ function is the association of the p110γ catalytic subunit to either
Jason Lowery et al.
The Journal of biological chemistry, 286(42), 36898-36906 (2011-08-11)
ADP-ribosylation factors (ARFs) and their activating guanine nucleotide exchange factors (GEFs) play key roles in membrane traffic and signaling. All ARF GEFs share a ∼200-residue Sec7 domain (Sec7d) that alone catalyzes the GDP to GTP exchange that activates ARF. We
Maria de la Fuente et al.
Biochemistry, 59(5), 671-681 (2020-01-21)
Protease-activated receptors (PARs) are G-protein-coupled receptors that are activated by proteolysis of the N-terminus, which exposes a tethered ligand that interacts with the receptor. Numerous studies have focused on the signaling pathways mediated by PARs. However, the structural basis for
Alanna E McCarthy et al.
Cell, 179(3), 659-670 (2019-10-08)
P2X receptors are trimeric, non-selective cation channels activated by extracellular ATP. The P2X7 receptor subtype is a pharmacological target because of involvement in apoptotic, inflammatory, and tumor progression pathways. It is the most structurally and functionally distinct P2X subtype, containing
Jakub A Bielnicki et al.
The Journal of biological chemistry, 286(40), 35163-35175 (2011-08-06)
PDZRhoGEF (PRG) belongs to a small family of RhoA-specific nucleotide exchange factors that mediates signaling through select G-protein-coupled receptors via Gα(12/13) and activates RhoA by catalyzing the exchange of GDP to GTP. PRG is a multidomain protein composed of PDZ
A p120 catenin isoform switch affects Rho activity, induces tumor cell invasion, and predicts metastatic disease
Yanagisawa M, et al.
The Journal of Biological Chemistry, 283(26), 18344-18354 (2008)
Marco H Hofmann et al.
Cancer discovery, 11(1), 142-157 (2020-08-21)
KRAS is the most frequently mutated driver of pancreatic, colorectal, and non-small cell lung cancers. Direct KRAS blockade has proved challenging, and inhibition of a key downstream effector pathway, the RAF-MEK-ERK cascade, has shown limited success because of activation of
Christian Schlein et al.
Cell reports, 34(2), 108624-108624 (2021-01-14)
Thermoneutral conditions typical for standard human living environments result in brown adipose tissue (BAT) involution, characterized by decreased mitochondrial mass and increased lipid deposition. Low BAT activity is associated with poor metabolic health, and BAT reactivation may confer therapeutic potential.
Yasmin ElMaghloob et al.
eLife, 10 (2021-01-14)
The ADP-ribosylation factor-like 3 (ARL3) is a ciliopathy G-protein which regulates the ciliary trafficking of several lipid-modified proteins. ARL3 is activated by its guanine exchange factor (GEF) ARL13B via an unresolved mechanism. BART is described as an ARL3 effector which
Amitha K Hewavitharana et al.
Journal of chromatography. A, 1567, 233-238 (2018-07-10)
Separation of highly charged compounds has always been a challenge in chromatography. Ion-pair reversed phase chromatography has been the most successful approach to date. Although polar reversed phase and HILIC columns have been introduced, they have limitations with highly charged
Qingci Zhao et al.
Cell reports, 32(8), 108074-108074 (2020-08-28)
The small guanosine triphosphatase (GTPase) RAS serves as a molecular switch in signal transduction, and its mutation and aberrant activation are implicated in tumorigenesis. Here, we perform real-time, in-cell nuclear magnetic resonance (NMR) analyses of non-farnesylated RAS to measure time
Vidhi Pareek et al.
Science (New York, N.Y.), 368(6488), 283-290 (2020-04-18)
Metabolons, multiprotein complexes consisting of sequential enzymes of a metabolic pathway, are proposed to be biosynthetic "hotspots" within the cell. However, experimental demonstration of their presence and functions has remained challenging. We used metabolomics and in situ three-dimensional submicrometer chemical
Meng Shi et al.
Nature communications, 9(1), 4987-4987 (2018-11-28)
The endosome-to-Golgi or endocytic retrograde trafficking pathway is an important post-Golgi recycling route. Here we show that amino acids (AAs) can stimulate the retrograde trafficking and regulate the cell surface localization of certain Golgi membrane proteins. By testing components of
Irina G Shabalina et al.
Biochimica et biophysica acta, 1837(12), 2017-2030 (2014-04-29)
Whether active UCP1 can reduce ROS production in brown-fat mitochondria is presently not settled. The issue is of principal significance, as it can be seen as a proof- or disproof-of-principle concerning the ability of any protein to diminish ROS production
John J H Shin et al.
Developmental cell, 52(4), 461-476 (2020-01-14)
Phosphoinositides, diacylglycerolpyrophosphate, ceramide-1-phosphate, and phosphatidic acid belong to a unique class of membrane signaling lipids that contain phosphomonoesters in their headgroups having pKa values in the physiological range. The phosphomonoester headgroup of phosphatidic acid enables this lipid to act as
N-desalkylquetiapine, a potent norepinephrine reuptake inhibitor and partial 5-HT 1A agonist, as a putative mediator of quetiapine's antidepressant activity
Jensen N H, et al.
Neuropsychopharmacology, 33(10), 2303-2303 (2008)
Nami Kim et al.
Scientific reports, 7, 41066-41066 (2017-01-25)
This study characterizes the human metabolic response to piperine, a curcumin extract, and the details of its underlying molecular mechanism. Using
Jürgen Kreiter et al.
International journal of molecular sciences, 22(5) (2021-04-04)
Adenine nucleotide translocase (ANT) is a well-known mitochondrial exchanger of ATP against ADP. In contrast, few studies have shown that ANT also mediates proton transport across the inner mitochondrial membrane. The results of these studies are controversial and lead to
Giovanna Del Vecchio et al.
Scientific reports, 9(1), 19344-19344 (2019-12-20)
The non-selective activation of central and peripheral opioid receptors is a major shortcoming of currently available opioids. Targeting peripheral opioid receptors is a promising strategy to preclude side effects. Recently, we showed that fentanyl-derived μ-opioid receptor (MOR) agonists with reduced
Changrui Xing et al.
Cell, 180(4), 645-654 (2020-02-01)
Drugs selectively targeting CB2 hold promise for treating neurodegenerative disorders, inflammation, and pain while avoiding psychotropic side effects mediated by CB1. The mechanisms underlying CB2 activation and signaling are poorly understood but critical for drug design. Here we report the
Nicola M Martucci et al.
Biochimie, 94(2), 503-509 (2011-09-20)
The effect of pulvomycin on the biochemical and fluorescence spectroscopic properties of the archaeal elongation factor 1α from Sulfolobus solfataricus (SsEF-1α), the functional analog of eubacterial EF-Tu, was investigated. The antibiotic was able to reduce in vitro the rate of protein
Lizhen Qiao et al.
Journal of chromatography. A, 1360, 240-247 (2014-08-19)
Glucaminium-based ionic liquids are a new class of recently developed ionic liquids and prepared by functionalizing the amine group of N-methyl-d-glucamine, which renders them good hydrophilicity due to the presence of the glucose structure and charged quaternary ammonium group. In
Neuropeptide Y promotes neurogenesis in murine subventricular zone
Agasse F, et al.
Stem Cells, 26(6), 1636-1645 (2008)
Athena M Klutz et al.
Journal of nanobiotechnology, 6, 12-12 (2008-10-25)
An approach to use multivalent dendrimer carriers for delivery of nucleoside signaling molecules to their cell surface G protein-coupled receptors (GPCRs) was recently introduced. A known adenosine receptor (AR) agonist was conjugated to polyamidoamine (PAMAM) dendrimer carriers for delivery of
Julie V Selkirk et al.
The Journal of pharmacology and experimental therapeutics, 379(3), 386-399 (2021-09-19)
Ozanimod, a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5), is approved for the treatment of relapsing multiple sclerosis (MS) in multiple countries. Ozanimod profiling revealed a species
Viola Spahn et al.
Scientific reports, 8(1), 8965-8965 (2018-06-14)
Novel pain killers without adverse effects are urgently needed. Opioids induce central and intestinal side effects such as respiratory depression, sedation, addiction, and constipation. We have recently shown that a newly designed agonist with a reduced acid dissociation constant (pKa)
Laura L Thomas et al.
Molecular biology of the cell, 32(11), 1104-1120 (2021-04-01)
Rab family GTPases are key organizers of membrane trafficking and function as markers of organelle identity. Accordingly, Rab GTPases often occupy specific membrane domains, and mechanisms exist to prevent the inappropriate mixing of distinct Rab domains. The yeast Golgi complex
Ivana Yen et al.
Cancer cell, 34(4), 611-625 (2018-10-10)
Targeting KRAS mutant tumors through inhibition of individual downstream pathways has had limited clinical success. Here we report that RAF inhibitors exhibit little efficacy in KRAS mutant tumors. In combination drug screens, MEK and PI3K inhibitors synergized with pan-RAF inhibitors
Philipp Hörmann et al.
Cell death discovery, 7(1), 151-151 (2021-07-07)
L-3,4-Dihydroxyphenylalanin (L-DOPA or levodopa) is currently the most used drug to treat symptoms of Parkinson's disease (PD). After crossing the blood-brain barrier, it is enzymatically converted to dopamine by neuronal cells and restores depleted endogenous neurotransmitter levels. L-DOPA is prone
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