• In summary we obtained and

  2022-03-18

  

  In summary, we obtained - and -type of linaclotide by protein chemical synthesis and acquired the X-ray crystal structure of linaclotide for the first time through racemic crystallization technique. The structure of linaclotide forms a compact spatial structure containing three- turns through three

• One previously unreported discovery is

  2022-03-18

  

  One previously unreported discovery is that Ptgds is alternatively spliced, such that partial removal of exon 3 correlates with higher levels of regeneration. The absence of exon 3 likely affects the functionality of the final product. The structure of Ptgds is that of the typical lipocalin β-barrel

• GPR is present primarily in the pancreas and the

  2022-03-18

  

  GPR119 is present primarily in the pancreas and the intestine. Activation of GPR119 increases insulin, GLP-1, GIP and PYY secretion. GPR119 agonists stimulate insulin release in a glucose-dependent manner. The glucose dependent insulin secretion (GIDS) mechanism makes GPR119 an attractive target for

• Fig summarizes the underlying mechanism

  2022-03-18

  

  Fig. 7 summarizes the underlying mechanism of SB on inhibiting inflammation and maintaining epithelium barrier integrity in the TNBS-induced colitis model. Our findings not only explained the protective effect of SB on colon health, but also provided evidence that GPR109A likely constitutes a valid

• Compared to methadone or morphine buprenorphine is

  2022-03-18

  

  Compared to methadone or morphine, buprenorphine is a partial mu-opioid agonist, which shows high affinity for, and slow dissociation from, mu-opioid receptors. This maintenance of homeostasis may help to counter the development of an overt withdrawal syndrome, and may explain the lower risk of deve

• The use of HIV peptide

  2022-03-18

  

  The use of HIV-1 peptide epitope-based vaccines is safer and cheaper than live or inactivated vaccines [8]. However, peptide epitope vaccines could show poor immunogenicity and have poor uptake by APCs [9]. Nevertheless, nanocarrier-based delivery platforms have been demonstrated to enhance the pept

• In summary we discovered azaindole substituted hydroxypyrido

  2022-03-18

  

  In summary, we discovered 7-azaindole substituted -hydroxypyridone as a potent zinc-binding GLO1 inhibitor (IC=11nM) through lead generation from HTS and structure-based inhibitor design. The X-ray cocrystal structure and the comparison of binding energies with the indole counterpart revealed that b

• The calculations for the R substrate showed that

  2022-03-18

  

  The calculations for the R substrate showed that, like the S substrate, the coordination shell of the Zn Fmoc-D-Phe(4-Cl)-OH mg is more symmetric than in the HIC-SG crystal structure. This symmetry indicates that the enzyme could use the same reaction mechanisms as for the S substrate, but with exc

• First class II fusion proteins are

  2022-03-18

  

  First, class II fusion proteins are known to transition from a (homo- or hetero-) pre-fusion dimer to a post-fusion trimer [57], [58], [59], [60], [61], [62] through a monomeric intermediate [63], [64], and a crystalline structure of a monomer of Rift Valley fever virus (a phlebovirus, member of the

• Pam2CSK4 Introduction l Glutamate is a major excitatory neur

  2022-03-18

  

  Introduction l-Glutamate is a major excitatory neurotransmitter in the mammalian central nervous system (CNS) that contributes not only to fast synaptic neurotransmission, but also to complex physiological processes like memory, learning, plasticity, and neuronal cell death [30], [81]. Glutamate is

• With these cyclopropene glutamate derivatives in hand we tes

  2022-03-18

  

  With these cyclopropene-glutamate derivatives in hand, we tested their ability to ligate with popular bioorthogonal reagents (Fig 3). First, we tested their ability to ligate with a tetrazine (3,6-Di-2-pyridyl-1,2,4,5-tetrazine) via an inverse electron demand Diels-Alder reaction by monitoring the c

• The role of cell to cell interactions

  2022-03-17

  

  The role of cell-to-cell interactions in coordinating the cells’ behaviour to ensure an appropriate anterior pituitary hormone response is receiving increasing attention. Anterior pituitary 822 interact with neighbouring cells through junctional complexes. As their name implies, the complexed are c

• The gene structures of cGalR and cGalR L

  2022-03-17

  

  The gene structures of cGalR2 and cGalR2-L were determined by in silico comparison with the chicken genomic DNA sequences retrieved from the Ensembl database. Both cGalR2 and cGalR2-L genes are composed of two coding exons, separated by single introns of 0.9kb (cGalR2) or 3kb (cGalR2-L) locating wit

• Growing evidence supporting the anti inflammatory

  2022-03-17

  

  Growing evidence supporting the anti-inflammatory and tissue-protective effects of FPR antagonists led to the screening of commercial libraries for novel small-molecule FPR antagonists. As result of these screening efforts and/or structure–activity relationship (SAR)-directed design and synthesis, a

• Recently we indicated that cell motility was

  2022-03-17

  

  Recently, we indicated that cell motility was regulated by the different induction of GPR120 and GPR40 in liver epithelial WB-F344 Irsogladine treated with chemical agents. The cell motility of WB-F344 cells was stimulated by phorbol ester 12-O-tetradecanoylphorbol-13-acetate (TPA) which is a potent

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