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br Conflict of interest br CRediT authorship
2021-12-07
Conflict of interest CRediT authorship contribution statement Magdalena Olga Ciechanowska: Conceptualization, Data curation, Investigation, Methodology, Project administration, Writing - original draft. Magdalena Łapot: Formal analysis, Investigation, Methodology. Marek Kowalczyk: Writing - re
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In conclusion starting from the
2021-12-07
In conclusion, starting from the weakly potent GSM , exploration of various spacer groups between the triazole ring and the aromatic SKL2001 led to the discovery of a new series of potent gamma secretase modulators, with an improved drug-like profile—compared with the originally reported series aro
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Somatostatin analogues are among the first peptide based dru
2021-12-06
Somatostatin analogues are among the first peptide-based drugs used in cancer imaging and therapy (for review see Reubi, 2003). Treatment of tumors by the use of peptide analogues labeled with cytotoxic agents acting via specific receptors is also under investigation for neuropeptide Y (Koglin and B
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We tested formyl MYVKWPWYVWL which we had previously shown
2021-12-06
We tested formyl-MYVKWPWYVWL, which we had previously shown to have essentially identical Kis for W190/N192, R190/K192 and R190/N190 [8] of 130 nM, for its ability to downregulate surface receptor (Fig. 5A). R190/K192 exhibited the lowest EC50 of 44±4 nM about 3 fold below the observed Ki and a maxi
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br Introduction The fibroblast growth factor
2021-12-06
Introduction The fibroblast growth factor receptor (FGFR) pathway is an important oncogenic driver in malignant cancer. It controls cellular processes such as cell proliferation, differentiation, migration, gw research ltd sale progression, metabolism, and survival. In non–small-cell lung cancer,
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In addition to the four classical FGFRs
2021-12-06
In addition to the four classical FGFRs there is an additional receptor, FGFR like-1 (FGFRL1, also known as FGFR5) (Ornitz and Itoh, 2015, Trueb et al., 2003). FGFRL1 gene was discovered in a cartilage specific cDNA library in 2000 (Trueb, 2011, Trueb et al., 2003) and thereafter it has been found i
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Several transgenic and knockout congenic mouse models have b
2021-12-06
Several transgenic and knockout/congenic mouse models have been generated in order to assess the role of FFAR1 for proper insulin secretion and maintenance of glucose homeostasis. The results obtained with three different receptor knockout mouse models were not consistent. The protection against hig
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On the other hand Li Zhang et al and
2021-12-06
On the other hand, Li+ (Zhang et al., 1996) and Ca2+ (Gizak et al., 2004) cations inhibit FBPases. However, in the case of Ca2+, the inhibition is attributed solely to the muscle isozyme which is over 100 times more susceptible to the cation action than the liver isoform (Gizak et al., 2004). At the
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Much is known about FPPS structure and
2021-12-06
Much is known about FPPS structure and function, with over 120 FPPS crystal structures being currently available. This wealth of information is largely the consequence of human FPPS serving as a drug target for the treatment and/or prevention of pathologies such as osteoporosis, hypercalcemia and Pa
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Although drug monitoring is not usually requested there are
2021-12-06
Although drug monitoring is not usually requested, there are some cases where measurement of DOACs in p38 mapk inhibitor is useful, and of special help for managing patients at risk. These cases include the control of adherence to a therapeutic protocol, surveillance of drug accumulation risk in lo
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br Experimental procedures br Results br Discussion
2021-12-06
Experimental procedures Results Discussion The data herein confirm the well documented neuroinflammatory effect of TLR3 activation following systemic administration of the viral mimetic poly I:C and the associated acute sickness response which includes fever, reduced body weight and allodyn
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Emodin The finding that a peptide consisting of d amino
2021-12-06
The finding that a peptide consisting of d-amino acids binds to LSD1-CoREST1 with equal affinity as the l-amino Emodin ligand indicates that the assays detect a generally non-specific association between two highly charged molecules. Nonetheless, p53-CTD is an effective inhibitor of LSD1 and its bi
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To efficiently develop bioactive ligands even
2021-12-06
To efficiently develop bioactive ligands even if the structural information of the target protein is unknown, we have presented a three-dimensional structural diversity-oriented strategy based on structural properties of a chiral cyclopropane. Our strategy has allowed us to design and synthesize a s
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Cyclopamine a steroidal alkaloid type secondary
2021-12-06
Cyclopamine, a steroidal alkaloid type secondary metabolite from Veratrum californicum Durand (Melanthiaceae), serves as an anti-Hh constituent blocking the activation of Smo [96,100]. According to previous studies, cyclopamine was shown to inhibit the development of human hepatocellular carcinomas
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Gene expression of both GPR A and GPR in
2021-12-06
Gene expression of both GPR109A and GPR81 in adipocytes has been linked to PPARγ activation [22]. Treatment with the thiazolidinedione (TZD) PPARγ agonist, rosiglitazone, increases GPR109A and GPR81 expression, and knockdown of PPARγ suppresses receptor expression in fully differentiated human multi
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