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Recently two distinct small molecule inhibitors of PHGDH wer
2023-12-08

Recently, two distinct small-molecule inhibitors of PHGDH were identified using high-throughput screens, both of which inhibit de novo serine biosynthesis and show selective toxicity to cancer Pravastatin sodium with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, reduces t
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br Conflict of interest br Financial Support The
2023-12-07

Conflict of interest Financial Support The work is supported by research grants from Clinical Key Specialty Project of China and Clinical Medical Center of Suzhou, China (Szzx201502) and Jiangsu Province Special Program of Medical Science, China (BE2016672). Introduction Recently, function
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In chicken ovary the adiponectin gene
2023-12-07

In chicken ovary, the adiponectin gene was found to be mainly expressed in theca cells and is suggested to exert a paracrine or autocrine effect on ovarian steroidogenesis (Chabrolle et al., 2007). A limited number of studies have revealed the effect of adiponectin on ovarian steroidogenesis or its
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Actin is capable of polymerizing
2023-12-07

Actin is capable of polymerizing spontaneously. However, this process is relatively slow and kinetically unfavorable in cells. Formation of D-NMAPPD synthesis dimers and trimers, which can easily disassemble due to their instability, is a rate-determining step in actin polymerization [5], [6]. The
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Luciferase Immunoprecipitation Systems LIPS which utilizes r
2023-12-07

Luciferase Immunoprecipitation Systems (LIPS), which utilizes recombinant antigens fused to the enzyme reporter Renilla luciferase (Ruc) to detect patient antibodies, provides a unique platform to investigate 4-P-PDOT receptor directed against a variety of antigenic targets [25]. Previously, LIPS h
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The first rationally designed dual mPGES LO inhibitor was
2023-12-07

The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic 22 - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have been synthesized and
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Many metalloenzyme inhibitors consist of
2023-12-07

Many metalloenzyme inhibitors consist of two chemical components: the MBG, the portion of the inhibitor designed to bind to the metal, and the scaffold, the portion of the inhibitor recognized by the amino SB 366791 residues that form the substrate-binding site of the metalloenzyme. The MGB is ofte
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ATX LPA signaling in cancer is also well known to
2023-12-07

ATX/LPA signaling in cancer is also well known to promote chemotherapy and radiotherapy resistance [7]. Furthermore, others have recently shown that endothelial-derived ATX activity in renal cell carcinoma promotes renal tumorgenesis and acquired resistance to sunitinib through an IL-8-mediated mech
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Further important evidence for G
2023-12-07

Further important evidence for G protein signaling on early endosomes has been subsequently obtained for the β2-adrenegic receptor using fluorescently-tagged conformation-sensitive nanobodies selectively recognizing the active receptor and Gs protein [43]. More recently, our group used a combinatio
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The therapeutic potential of ML
2023-12-07

The therapeutic potential of ML327-induced MET against ORY-1001 receptor of mesenchymal origin has not been explored. In the present study, we hypothesized that induction of MET using ML327 would block the growth of ES cells and sensitize to TRAIL-mediated apoptosis. Herein, we report that ML327 in
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Experimentally the ECD spectrum of showed three ECD bands po
2023-12-07

Experimentally, the ECD spectrum of 1 showed three ECD bands: positive ones at 260 and 200nm, and a negative one at 230nm (Fig. 4). Meanwhile, there is only one broad positive ECD band starting from 300nm in the ECD spectrum of 2. ECD spectra of 1 and its derivatives attracted great interest because
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Despite the absence of disulfide bonds in
2023-12-07

Despite the absence of disulfide bonds in its linear structure, KT43C displays antifungal and antibacterial activity. Disulfide bonds are determinants of defensins' integrity and have been reported to increase the antimicrobial activity (Jenssen et al., 2006). However, some linear derivatives of AMP
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and LO are members of the lipoxygenase family that
2023-12-06

5- and 12/15-LO are members of the lipoxygenase family that convert arachidonic eflornithine hydrochloride into lipid mediators such as leukotriene B4 (LTB) and 12()-hydroxyeicosatetraenoic acid (HETE) and 15()-HETE, respectively. Evidence from several in vitro and in vivo studies has shown that act
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To investigate the potential link between G
2023-12-06

To investigate the potential link between Gβγ and MT assembly in vivo, cultured NIH3T3 and PC12 cells were used. The role of Gβγ in MT assembly was demonstrated using nocodazole, a MT depolymerizing drug [14]. We found that Gβγ was preferentially bound to MTs in NIH3T3 and PC12 cells and treatment w
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The assay performance was estimated using Z factors plotted
2023-12-06

The assay performance was estimated using Z′-factors (plotted in Fig. 2A) according to Zhang et al. calculated for each plate comparing positive (in the absence of an inhibitor) and negative controls (in the presence of an AdK inhibitor). The mean Z′-factor±SD was determined to be 0.7±0.1, indicativ
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