• Our initial approach to identify hits was two pronged

  2023-09-27

  

  Our initial approach to identify hits was two-pronged and included a high-throughput screening (HTS) campaign of the OSI DPQ library as well as a virtual screening (VS) campaign, utilizing a publically available crystal structure of ACK1 (PDB code: ). A tolerance for protein flexibility was incorpo

• The nAChR has been considered an interesting potential targe

  2023-09-26

  

  The α7 nAChR has been considered an interesting potential target for numerous therapeutic indications over the last two decades, with GTS-21 one of the first candidates proposed for Alzheimer's disease [2], [3], [23]. Unfortunately, although many α7-selective agonists have been developed [21], none

• rs G allele was previously associated with a decrease

  2023-09-26

  

  rs523349 G allele was previously associated with a decrease in the conversion rate of testosterone to DHT (Beesley et al., 2007). This SRDA52 variant may have a trend towards higher testosterone availability, which according to the US Food and Drug Administration is described as a teratogen of categ

• The synthetic route to M developed by

  2023-09-26

  

  The synthetic route to M100907 developed by Rice was utilized, however, the chiral resolution was carried out at an earlier stage to provide the possibility of introducing different substituents onto the piperidinyl group. The conditions for this resolution were different from previously reported.

• Aurora A and B are required for the

  2023-09-26

  

  Aurora A and B are required for the control of mitosis whereas Aurora C is mainly invoved in meiosis (Goldenson and Crispino, 2015). Interestingly, Aurora B is partnered with inner centromere protein (INCENP), survivin and Borealin to form a chromosomal passenger complex (CPC) that is critical for t

• Along with the improvement of the cadmium transport from

  2023-09-26

  

  Along with the improvement of the cadmium transport from roots to aerial tissues, as is required for phytoremediation, over-expression of PtoHMA5 also led to the excessive accumulation of cadmium in leaves that was harmful to plant growth and physiological performance. Thus, detoxification of the he

• Aromatization of the pyrrole ring after anion capturing

  2023-09-26

  

  Aromatization of the pyrrole ring after anion capturing, using acceptor atoms with electron deficiency (B & Be), and substitution of strong electron withdrawing groups such as CN were three strategies used to design a new class of anion receptors. Comparison of the anion affinities of these anion re

• ASK belongs to the family of MAPKKK ASK mediated apoptosis

  2023-09-26

  

  ASK1 belongs to the family of MAPKKK. ASK1-mediated apoptosis is involved in the pathogenesis of several diseases such as I/R injury, infectious diseases and neurodegenerative disorders [33], [34], [35]. ASK1 can be activated through different mechanisms. One mechanism is that oxidative stress direc

• br Conflicts of interest br Introduction

  2023-09-26

  

  Conflicts of interest Introduction Arginase catalyzes the reaction in which l-arginine is converted to l-ornithine and urea. In humans, two arginase isoenzymes have been identified, arginase 1 and arginase 2, that differ in cellular location and tissue distribution [1]. Both arginase enzymes a

• In order to determine whether the faster Rh induced

  2023-09-26

  

  In order to determine whether the faster Rh2-induced apoptosis is specific of cholesterol depletion, we determined the cytotoxic effect of Rh2 in rho kinase inhibitor depleted or not in sphingomyelin, another abundant plasma membrane lipid exhibiting enrichment in lipid rafts. We showed that, in con

• The fluorescence in a fluorescent antibiotic

  2023-09-26

  

  The fluorescence in a fluorescent antibiotic can be derived either from functional groups with intrinsic fluorescence in an existing antibiotic, or via synthetic conjugation of a fluorophore to an antibiotic core to enable visualisation. Attachment of fluorophore to an antibiotic should ideally not

• br Method of literature search br Disclosures br Acknowledgm

  2023-09-26

  

  Method of literature search Disclosures Acknowledgment The authors thank and acknowledge Mrs. Jaini Parekh, BFA, for illustrating the diagram in Figure 1. An overview of angiogenesis Angiogenesis is a biological process through which there is the formation of new blood vessels from pre-

• Under some pathological conditions AT R

  2023-09-26

  

  Under some pathological conditions, AT1R internalization is decreased when agonist exposure is prolonged. This weakens or removes the AT1R desensitization effect and leads to AT1R and downstream signal overactivation. AT1R overactivation can result in continued biological effects such as sustained v

• br AR expression in breast tissue Although androgenic signal

  2023-09-26

  

  AR expression in breast tissue Although androgenic signalling is chiefly associated with the development and maintenance of primary and secondary male characteristics, especially during puberty when the testes are by far the major source of testosterone, the AR also plays important functions in f

• br Material and methods br Results Table

  2023-09-26

  

  Material and methods Results Table 1 shows that in addition to Leu/CysAP and DPPIV, genes for AspAP, ArgAP, MetAP, APM and PSA are expressed in adipocytes. The kinetic parameters of these AP are also shown in Table 1, revealing that APM has the highest Vmax and catalytic efficiency (Kcat/Km),

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