• From an industrial perspective the low turnover numbers and

  2020-05-16

  

  From an industrial perspective, the low turnover numbers and limited substrate scope of α-KG halogenases still represents a significant challenge. However, in light of the fact that currently no chemical processes are available for the selective halogenation of aliphatic carbon centers in complex mo

• Diagnosis of NCC can be

  2020-05-16

  

  Diagnosis of NCC can be accomplished via imaging techniques and serological confirmatory testing. The best immunodiagnostic test for NCC, the enzyme-linked immunotransfer blot EITB (Tsang et al., 1989), is based on the detection of 3\'-Azido-3\'-deoxythymidine β-D-glucuronide sodium salt to one or

• It has previously been established that

  2020-05-16

  

  It has previously been established that DDRs play an important role in collagen regulation in at least two distinct ways: (1) activation of DDRs by collagen results in up-regulation of the matrix metalloproteinases, which results in cleavage and degradation of the ECM20., 21., [22] and (2) SP 141 o

• It has previously been established that

  2020-05-16

  

  It has previously been established that DDRs play an important role in collagen regulation in at least two distinct ways: (1) activation of DDRs by collagen results in up-regulation of the matrix metalloproteinases, which results in cleavage and degradation of the ECM20., 21., [22] and (2) SB408124

• dihydroxycholesterol OHC was recently identified by

  2020-05-16

  

  7α,25-dihydroxycholesterol (7α,25-OHC) was recently identified by classic analytical methods as a high-affinity ligand for EBI2 (Hannedouche et al., 2011; Liu et al., 2011). 7α,25-OHC was previously identified as an intermediate in the alternate pathway of hepatic bile WAY-100635 maleate salt synthe

• We also discovered important clues

  2020-05-16

  

  We also discovered important clues to domain LDN-212854 of DGKs and how to exploit these regions for development of DGKα-selective inhibitors. The identification of a probe-modified site at the C1 domain provided the first evidence of a ligand binding site remote from the ATP binding region of DGKs.

• Dgat mice however had less adipose tissue

  2020-05-16

  

  Dgat−/− mice, however, had less adipose tissue, as reflected by lower total fat pad weights and body triglyceride content. Because of these findings, we hypothesized that, although Dgat−/− mice could make triglycerides through non-DGAT pathway(s), their triglyceride synthesis capacity might not be e

• br Fragment based drug discovery FBDD

  2020-05-16

  

  Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical FDA-approved Drug Library space with libraries which are smaller in size, producing drug leads with high ligand-binding

• With a favorable spectrum of CRTh dependent in

  2020-05-16

  

  With a favorable spectrum of CRTh2 dependent in vitro and in vivo efficacy demonstrated, the off-target activity of compound 18 was investigated, first against a panel of prostanoid receptors and related eicosanoid targets (Table 8), where no significant activities at 10μM concentration were found i

• Ropivacaine HCl receptor Early studies from the mollusk Aply

  2020-05-15

  

  Early studies from the mollusk, Aplysia, reported the presence of a unique class of Ropivacaine HCl receptor receptors in neurons, the acetylcholine-gated chloride channels (ACCs) (Kehoe and McIntosh, 1998). Later, studies identified these receptors in the model nematode Caenorhabditis elegans (Put

• Nrf and HO are key factors in the regulation of

  2020-05-15

  

  Nrf2 and HO-1 are key factors in the regulation of oxidative stress in the body. Research has shown that KLF2 can activate Nrf2 and HO-1 [14]. To investigate the mechanisms by which KLF2 regulates eNOS uncoupling and oxidative stress, Nrf2 was inhibited or HO-1 was knocked down in KLF2 overexpressin

• Results from experiments in model systems have suggested tha

  2020-05-15

  

  Results from experiments in model systems have suggested that the DPRs translated from the HRE of C9ORF72 are toxic and play a role in disease pathogenesis (reviewed in Taylor et al. (2016)). Although the DPRs are present in neurons and glia in various regions of the central nervous system (CNS) ear

• Itch also known as astrophin interacting protein AIP

  2020-05-15

  

  Itch, also known as astrophin-1 interacting protein-4 (AIP4), is a HECT domain-E3 ligase. It was discovered in 1998 in mouse coat color genetic studies which displayed the disruption caused by the Itch gene inducing a lethal autoimmune inflammatory condition. The substrates of Itch are transmembrane

• br Introduction O Methylguanine DNA methyltransferase MGMT i

  2020-05-15

  

  Introduction O6-Methylguanine-DNA methyltransferase (MGMT) is a DNA-repair enzyme that specifically transfers alkyl adducts from the O6 position of guanine to the cysteine residue (Cys145) in its active site. In cancer cells, this ability of MGMT disrupts the cytotoxic actions of alkylating antic

• Funding sources This study was funded by European

  2020-05-15

  

  Funding sources This study was funded by European Community’s Seventh Framework Programme under grant agreement No. 305662 (Project: Community-based scheduled screening and treatment of malaria in pregnancy for improved maternal and infant health: a cluster-randomized trial ‘COSMIC’). Acknowledg

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