• br Introduction Coping with DNA damage is possible thanks to

  2019-10-24

  

  Introduction Coping with DNA damage is possible thanks to surveillance mechanisms (checkpoints), that detect the problem and promote its solution [1], [2], and to repair and tolerance pathways that remove the lesions or reduce the damage consequences [3], [4]. Failures in these processes have a h

• Effect of a C C double bond

  2019-10-24

  

  Effect of a C4-C5 double bond — The presence of a double bond at the substrate’s C4-C5 position affects the reactivity of Δ1-KSTDs to varying extent, depending on the enzyme. Most 3-ketosteroids that are converted by Δ1- KSTDs have this double bond. For some Δ1-KSTDs this double bond is even require

• Introduction Formate dehydrogenase enzymes FDHs are a

  2019-10-24

  

  Introduction Formate dehydrogenase enzymes (FDHs) are a group of heterogeneous proteins that catalyse the reversible formate () oxidation to carbon dioxide () (Eq. (1)). These enzymes are classified in two families, one gathering the enzymes that hold no redox-active centres and another that includ

• br Results br Discussion Prostate cancer dissemination and

  2019-10-24

  

  Results Discussion Prostate cancer dissemination and skeletal metastases represent major therapeutic challenges. Once the skeletal metastasis occurs, the incurable patient could just be symptomatically treated to alleviate the pain. Therefore it is of great necessity to disclose the molecular

• Collagen compaction and alignment are generated by

  2019-10-24

  

  Collagen compaction and alignment are generated by cell-mediated contractile forces (Stopak and Harris, 1982). The transmission of actomyosin forces to collagen has been mainly attributed to integrins and the activation of the Rho-ROCK pathway (Clark et al., 2007, Kural and Billiar, 2013, Provenzano

• The purposes of this study is to develop

  2019-10-24

  

  The purposes of this study is to develop an experimental model of CysLT2 receptor-mediated LTC4-induced lung air-trapping in guinea pigs using S-hexyl GSH, and to clarify the mechanism underlying response to such trapping using montelukast, a CysLT1 receptor antagonist, BayCysLT2RA, a CysLT2 recepto

• Testosterone is inactivated through hydroxylation and conjug

  2019-10-24

  

  Testosterone is inactivated through hydroxylation and conjugation pathways [3], [4]. 6β-Hydroxylation is the main pathway among testosterone hydroxylation processes in the liver microsome. Testosterone 6β-hydroxylation is mainly catalyzed by cytochrome P450 3A (CYP3A) [5], [6], which is expressed in

• Today many strategies have been

  2019-10-24

  

  Today, many strategies have been developed to enhance CXCR-4 receptor 1,2-Dimyristoyl-sn-glycerol on the cell surface, either by modifying the cell culture medium or by modifying the CXCR-4 gene in BMSCs to stimulate stem cell recruitment (Jiang et al., 2012, Liu et al., 2014b). For instance, the p

• The use of recombinant ER and ER

  2019-10-24

  

  The use of recombinant ERα and ERβ binding assays offers a relatively inexpensive, rapid technique for screening compounds for potential direct Pioglitazone HCl receptor modulatory activity and understanding the mechanisms of existing herbal medicines. For background on the protein production syste

• Raloxifene is a second generation SERM

  2019-10-24

  

  Raloxifene is a second generation SERM that has tissue-specific effects that differ from those of tamoxifen. Raloxifene was marketed for prevention and treatment of osteoporosis in postmenopausal women in the US and Europe. In a phase II randomized double-blind study, tamoxifen and raloxifene were e

• EP receptors belong to the

  2019-10-24

  

  EP1–4 receptors belong to the family of G protein-coupled receptor (GPCR). Trafficking events such as externalization, internalization, recycling and degradation dynamically regulate GPCR cell surface density. A fast-rate of internalization and degradation reduces GPCR surface density to desensitize

• Fomepizole More than thirty enzymes with PLA activity have b

  2019-10-24

  

  More than thirty enzymes with PLA2 activity have been described and, based on sequence similarities, they are currently classified in 16 groups, each containing several sub-groups [16]. However, based on biochemical features these enzymes are frequently grouped into six major families: secreted pho

• br Results br Discussion The structures presented

  2019-10-23

  

  Results Discussion The structures presented here were solved at high KT203 and show in detail how DDR1 achieves high affinity for imatinib and ponatinib, respectively. Both type II inhibitors bind in their more potent extended conformations to the inactive DFG-out conformation of the kinase d

• Nucleophosmin NPM which also plays a role

  2019-10-23

  

  Nucleophosmin (NPM1), which also plays a role on the nuclear export of ribosomal proteins and subunits (Maggi et al., 2008), is also a relevant MYC target, presumably through an interaction with CRM1. Conversely, it has been recently reported that specific SINE compounds reduce the levels of MYC in

• One strategy which is different from the

  2019-10-23

  

  One strategy which is different from the above is to isolate a similar enzyme to the one under study which will not be recognized by the antibody of the original protein. This approach will lead to prolonging an enzyme’s activity. For example, a novel variant of Carboxypeptidase G2 (CPG2), which has

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