• CaneCPI showed strong inhibitory activity against

  2019-12-17

  

  CaneCPI-4 showed strong inhibitory activity against recombinant falcipain-2 and falcipain-3, with IC values of 11.9±0.4nM and 42.3±0.8nM, respectively (Table 1, Supplementary material). Falcipains are involved in hemoglobin cleavage, with generation of two fractions: the heme and the globin. The hem

• calpain inhibitor 1 Ethyl naphthoates a h were successfully

  2019-12-17

  

  Ethyl 1-naphthoates (10a–h) were successfully reduced to 1-naphthylmethanols (12a–h) by using LiAlH4 with 8–87% yields. Then PCC was used to convert the alcohols into the corresponding 4-alkyl-1-naphthaldehyde derivatives (13a–h) with relatively higher yields (58–90%) as represented in Scheme 2. The

• Placental insufficiency is regarded as

  2019-12-17

  

  Placental insufficiency is regarded as the main etiology for FGR. Placental development is highly unique in eutherians and is regulated by numerous factors. For example, the novel retrotransposon-derived gene retrotransposon-like 1 (RTL1) was recently shown to play a key role in placental developmen

• Estrogen related receptors ERRs are orphan nuclear receptors

  2019-12-17

  

  Estrogen-related receptors (ERRs) are orphan nuclear receptors and have three members including ERRα, ERRβ, and ERRγ (Yasumoto et al., 2007). Though they are termed as ERRs due to the sequence homology with estrogen receptors, they don’t need to bind estrogens to exert action. Generally, ERRs bind t

• br O GlcNAc transferase OGT

  2019-12-16

  

  O-GlcNAc transferase OGT belongs to the metal-independent GT-B superfamily of glycosyltransferases, which has been well-reviewed previously [14,15]. OGT is an essential gene encoded on the X-chromosome, and it has two main regions: a long N-terminal tetratricopeptide repeat (TPR) region and a C-t

• br Effects of culture conditions on

  2019-12-16

  

  Effects of culture conditions on drug-induced gene Isochlorogenic acid A in primary human hepatocytes Past progress in elucidating the optimal conditions for the long-term cultivation of rodent hepatocytes has helped define some of the key components in the matrix and medium environment that are

• br Materials and methods br Results br Discussion

  2019-12-16

  

  Materials and methods Results Discussion The investigation of oxysterols is highly complex and challenging, arising not only from the large number of molecules in this family, but also due to their low abundance in biological systems compared to cholesterol and their susceptibility for auto

• br Discussion and conclusion Ubiquitination and deubiquitina

  2019-12-16

  

  Discussion and conclusion Ubiquitination and deubiquitination have emerged as important mechanisms involved in p53 management. This review revealed that various DUBs can regulate p53 or p53-Mdm2-MdmX networks. Herein, we reviewed the current progress made toward elucidating the complexities in th

• Current therapeutic interventions are directed both to preve

  2019-12-16

  

  Current therapeutic interventions are directed both to prevent (primarily by proper glycemic control) and to treat the advanced stages of diabetic retinopathy, when vision has already been significantly affected. Although these therapies can be very effective in preventing, delaying or reducing visi

• Previous studies have indicated that hSSB may be

  2019-12-16

  

  Previous studies have indicated that hSSB1 may be phosphorylated at threonine residue 117 (T117) [13] and acetylated at lysine residue 94 (K94) [15], both of which promote hSSB1 function in response to ionising radiation exposure. Mass spectrometry screens of proteins immunoprecipitated with phospho

• Norfloxacin The ribosomal synthesis of D proteins is not cur

  2019-12-16

  

  The ribosomal synthesis of D-proteins is not currently feasible; the best effort undertaken so far was limited to the translational incorporation of two D-amino acids into the nascent protein chain by means of modified ribosomes (Dedkova et al., 2006). We therefore apply solid-phase peptide synthesi

• LPA is known to regulate the peroxisome

  2019-12-16

  

  LPA is known to regulate the peroxisome proliferator-activated receptor γ and the reorganization of actin cytoskeleton [58]. However, the physiological functions of LPA in cells are still poorly understood. The simultaneous production of PA with/without 1-LPA or 2-LPA may be important to maximize a

• Kuo et al Have shown that DAPK function

  2019-12-16

  

  Kuo et al. (2006) Have shown that DAPK1 function in inhibiting microtubule (MT) assembly is through the activation of microtubule affinity-regulating kinases (MARK)/PAR-1 family kinases MARK1/2, which destabilize MT by phosphorylating tau and related MAP2/4. This relation with DAPK1 has demonstrated

• Pyrazolopyrimidines are bioisostere of purine exhibit

  2019-12-16

  

  Pyrazolopyrimidines are bioisostere of purine exhibit promising antitumor activity by competitively binding to the ATP active site of different kinase Alisol B 23-acetate [16,17]. Several compounds of this family were found to induce apoptosis and/or reduce cell proliferation in various solid tumou

• Our structures also provide new

  2019-12-16

  

  Our structures also provide new insights into CRTH2 drug development. The ligand binding pocket revealed by our structures comprises many aromatic residues and a few polar residues at the distal end. Correspondingly, most CRTH2 antagonists share a similar structural feature characterized by an aceta

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