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Enzyme mimics belong to a type
2020-11-10

Enzyme mimics belong to a type of rising catalysts which show the similar function with their corresponding natural enzymes [20], [21], [22], [23], [24], [25], [26], [27], although their structures are different from natural enzymes. In the area of prodrug activation, the widely-used enzyme mimics a
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br Cytochrome P monooxygenases Cytochrome P monooxygenases P
2020-11-10

Cytochrome P450 monooxygenases Cytochrome P450 monooxygenases (P450s) belong to one of Nature’s most versatile group of enzymes for C–H functionalization and are able to perform challenging regioselective and stereoselective activations of remote, unactivated C(sp3)–H bonds, for which there are o
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br STAR Methods br Acknowledgments We would
2020-11-10

STAR★Methods Acknowledgments We would like to thank Dr. Tsung-Ping and Dr. Shang-Yi Tsai, National Institute on Drug Abuse, NIH for sharing protocols on pulse chase experiments and analysis. We would like to thank Dr. William G. Telford for his valuable input on Amnis flow cytometry experiment
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Introduction CYP is a superfamily of heme containing monooxy
2020-11-10

Introduction CYP450 is a superfamily of heme-containing monooxygenases, many of which are expressed in the liver, and they are significant phase-I pge2 in drug metabolism and detoxification. There are three subfamilies (CYP1, CYP2 and CYP3) that are mainly involved in the metabolism of drugs in bo
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Likewise the conserved cysteine in the E protein
2020-11-10

Likewise, the conserved cysteine in the E2 protein is the only residue shown to be essential for the transfer of Ub/Ubl from E2 to the HECT ligases (Dye and Schulman, 2007, Wu et al., 2003). However, all other terminal Ub/Ubl transfer reactions involving E2 enzymes suggest a critical role for the ta
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N acetylation by N acetyltransferase NAT is an important
2020-11-10

N-acetylation by N-acetyltransferase (NAT) is an important metabolic pathway for some substances, and there are 2 functional NAT isoforms in humans—NAT1 and NAT2. Studies of etamicastat in healthy subjects showed an extensive N-acetylation of etamicastat to the inactive metabolite BIA 5-961, and a l
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We have compared the potency of a
2020-11-10

We have compared the potency of a series of DNA-directed alkylating agents, including N-mustard-acridine, N-mustard-quinoline, and N-mustard-quinazoline conjugates previously synthesized in our laboratory [7], [13], and currently used drugs (oxaliplatin, cisplatin, or 5-FU) for the treatment of CRC
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The current study provides evidence for a previously unknown
2020-11-10

The current study provides evidence for a previously unknown role for DHODH as a growth/survival factor in KRAS mutant tumors. While many aspects of the link between DHODH inhibition and survival of KRAS mutant cells remain to be established, de novo pyrimidine biosynthesis appears to be a crucial p
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For example nM MTX markedly stimulates the differentiation
2020-11-10

For example, 200nM MTX markedly stimulates the differentiation of the monocytic U937 FK228 [39], but only 10nM MTX is sufficient for the inhibition of clonogenicity in the ALL and APL cell lines [22]. Furthermore, an even lower concentration of MTX (2nM) selectively induces the expression of p27 an
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In conclusion DDR ECD was shown to be
2020-11-10

In conclusion, DDR1 ECD was shown to be sufficient for collagen mediated DDR1 oligomerization, and the oligomerized form binds to collagen with increased affinity. In full length receptors expressed on live cells, DDR1 oligomerization occurred on the cell surface in agreement with the role of DDR1 E
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795 In order to assess quantitatively the contribution of th
2020-11-10

In order to assess quantitatively the contribution of the ung, dug and dut 795 to uracil-DNA accumulation in E. coli, we have developed a novel method for measuring uracil residues in DNA that is based on the approach of Kow and co-workers [33] for measuring AP-sites in DNA. The method, which we cal
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1 98 To better understand Wolbachia s dependence on these en
2020-11-10

To better understand Wolbachia’s dependence on these enzymes, RNAi experiments targeting these transcripts will be required to examine the consequences of their down-regulation on Wolbachia in the different tissues of the parasite. Initial studies have shown that decreases in Bm-cpl-3 and Bm-cpl-6 t
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CysLTs trigger contractile and inflammatory processes throug
2020-11-10

CysLTs trigger contractile and inflammatory processes through the specific interaction with cell surface receptors belonging to the rhodopsin family of the G protein-coupled receptor (GPCR) genes. Until now, two receptor subtypes have been cloned, namely CysLT1 and CysLT2[8]. In particular, when the
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br Results br Discussion GPCRs recognize a broad range
2020-11-09

Results Discussion GPCRs recognize a broad range of molecules with a vast chemical 2-Hydroxypropyl-β-cyclodextrin mg through different mechanisms. Our understanding of the recognition of lipid mediators by GPCRs primarily comes from the structural studies of receptors for lysophospholipids and
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We thank Dr Hongqiang Qin at Dalian Institute
2020-11-09

We thank Dr. Hongqiang Qin at Dalian Institute of Chemical Physics, Chinese Academy of Sciences for technical assistance in mass-spectrometric analysis. We thank Prof. Quentin Liu at Dalian Medical University and Prof. Qiang Shen at M.D. Anderson Cancer Center for helpful discussion and comments. Dr
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