• A novel series of DHODH

  2021-07-27

  

  A novel series of DHODH inhibitors was developed by us based on a lead that was discovered during a docking procedure and medicinal chemistry exploration. The activity of the initial lead was improved by a QSAR method and yielded low nanomolar inhibitors. Introduction The most common metabolic h

• Among the CYP enzymes CYP D

  2021-07-26

  

  Among the CYP450 enzymes, CYP2D has been considered a crucial protein that involves in the metabolism of xenobiotics and drugs (Zanger and Schwab, 2013). Some isoforms of the CYP2D subfamily have been well characterized, such as CYP2D6 due to its clinical importance and CYP2D14 in black cattle (Hama

• br Acknowledgements This work was supported

  2021-07-26

  

  Acknowledgements This work was supported by grants from National Natural Science Foundation of China (31772196 and 31301693), the Chinese Ministry of Agriculture (the 948 project no. 2014-S10). Rothamsted Research also receives grant-aided support from the UK Biotechnology and Biological Sciences

• br Introduction Breast cancer is the most common cancer in

  2021-07-26

  

  Introduction Breast cancer is the most common cancer in women and one of the leading causes of death worldwide. Estrogen receptor alpha (ERα, “wild-type” estrogen receptor), encoded by the estrogen receptor1 (ESR1) gene, is expressed in approximately 70% of all breast cancers. Hormonal therapy ha

• Materials and methods br Results Assay of

  2021-07-26

  

  Materials and methods Results Assay of botulinum toxin activity is critical for the risk-assessment, diagnosis, and treatment of botulism cases. The frequently encountered active forms of the toxin are; L chain (inside intoxicated neuronal cells), BoNT (in the blood stream of a botulism patient,

• Because EBI is expressed on the major subsets of

  2021-07-26

  

  Because EBI2 is expressed on the major subsets of immune cells, and small molecule antagonists for EBI2 were recently described (Benned-Jensen et al., 2013, Gessier et al., 2014), EBI2 constitutes a tempting drug target reminiscent of the sphingosine-1-phosphate receptor superagonist fingolimod/Gile

• We recently reported that the information about the electron

  2021-07-26

  

  We recently reported that the information about the electronic density obtained from a QTAIM analysis is useful to describe the molecular interactions that stabilize and destabilize the different complexes L-R [13], [14], [15]. Specifically in our previous work reported for DHFR inhibitors, the QTAI

• Our finding that activating DDR variants are a cause of

  2021-07-26

  

  Our finding that activating DDR2 variants are a cause of this disease suggested that the ABL inhibitor dasatinib, a leukemia drug that also inhibits DDR2, could be used for treatment of affected individuals.10, 11 To examine the effect of dasatinib on p.Leu610Pro- and p.Tyr740Cys-induced autophospho

• br Application of the screening system for

  2021-07-26

  

  Application of the screening system for ITP-binding proteins Inosine is a nucleoside with hypoxanthine as a base. Inosine nucleotides are relatively abundant in human jtc motors because inosine monophosphate (IMP) is a general precursor molecule for the de novo synthesis of AMP and GMP or a prod

• br Conflict of interest statement br Acknowledgement The stu

  2021-07-26

  

  Conflict of interest statement Acknowledgement The study was financially supported by the Ministry of Education, Youth and Sports of the Czech Republic – projects “CENAKVA” (No. CZ.1.05/2.1.00/01.0024) and “CENAKVA II” (No. LO1205 under the NPU I program), by the Grant Agency of the University

• br Neuroimaging Neuroimaging has not yet

  2021-07-26

  

  Neuroimaging Neuroimaging has not yet been systematically reported in individuals with CDD, although case reports document normal ZM 306416 anatomy or less often, show cortical atrophy or T2 fluid-attenuated inversion recovery hyperintensities in the white matter.15, 17, 18, 19, 48, 52, 54, 55,

• Recent studies showed that the activity of CK

  2021-07-23

  

  Recent studies showed that the activity of CK2 was significantly reduced in ischemic stroke model rats, and cerebral I/R injury significantly decreased the expression of CK2α (Lee et al., 2004; Kim et al., 2012; Zhou et al., 2016). In addition, the dysregulation of CK2 is involved in ERS/UPR in non-

• During the past decade it became increasingly clear

  2021-07-23

  

  During the past decade, it became increasingly clear that the affinity and efficacy of small agonists acting on the orthosteric binding site of a GPCR can be modulated by ligands that bind to a topographically distinct (allosteric) binding site on the same GPCR molecule 33, 39, 40, 41, 42. This allo

• Among the members of the GH family which groups different

  2021-07-23

  

  Among the members of the GH106 family, which groups 319 different sequences, a single 3D-structure has been reported, the BT0986 from Bacteroides thetaiotaomicron that shows a (β/α)8 barrel and catalyzes the hydrolysis of an α-l-rhamnopyranoside bound to the C2 position of an arabinofuranoside (L-Rh

• br Conclusions br Declaration of interest br

  2021-07-23

  

  Conclusions Declaration of interest Acknowledgements Introduction Uncorrected obesity has been a major health problem and the prevalence of obesity is fast rising reaching an epidemic proportion [[1], [2], [3]]. Ample of clinical and experimental evidence has suggested that obesity leads

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