• Tetrazole is one of the most commonly used bioisosteres

  2021-09-11

  

  1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive a

• The relationship between increased GPR expression in the EDL

  2021-09-11

  

  The relationship between increased GPR120 expression in the EDL skeletal muscle and systemic glucose control is yet to be investigated. However, if the increased expression of GPR120 correlates with enhanced insulin-stimulated glucose uptake in skeletal muscle, particularly the EDL muscle, this migh

• br Conflict of interest statement br Acknowledgements We ack

  2021-09-11

  

  Conflict of interest statement Acknowledgements We acknowledge the support of Zoetis Animal Health, Estrotect, Select Sires and Texas A&M AgriLife Research. The assistance of Randle Franke and Ernest Soto is also gratefully acknowledged. Background Luteal phase deficiency (LPD) is caused b

• Introduction Adaptations in the metabolism of cancers contri

  2021-09-11

  

  Introduction Adaptations in the metabolism of cancers contribute to tumor survival and growth and present opportunities to develop novel therapeutic strategies (Kelloff et al., 2005, Som et al., 1980). In particular, glutamine metabolism plays such an important role in cancer growth that a phenomen

• br Author contribution br Declaration of

  2021-09-11

  

  Author contribution Declaration of interest Acknowledgements This work was supported by National Natural Science Foundation of China (Grants 81473093) and State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM1601ZZ-02). Introduction Diabetes represents a majo

• br Introduction Most organisms require

  2021-09-11

  

  Introduction Most organisms require glucose as a key metabolite, and it is critical that mammalian cells regulate glucose levels properly to maintain bioenergetic homeostasis. The major transporters responsible for the uptake of glucose from systemic circulation into cells are the GLUTs, members

• MRcKO mice showed a comparable degree

  2021-09-11

  

  MRcKO mice showed a comparable degree of cardiac remodeling compared to control (MRf/f) mice. Moreover, the worse cardiac remodeling in pressure-overloaded GRcKO mice is not due to compensatory activation of cardiomyocyte MR, because GRMRdcKO mice displayed cardiac remodeling to the same extent as G

• Cryptochlorogenic acid The effects of galanin on anxiety may

  2021-09-10

  

  The effects of galanin on anxiety may depend on the site of drug administration, on the galanin receptor subtypes activated and on the animal models of anxiety employed (Barrera et al., 2005, Holmes and Picciotto, 2006, Soares et al., 2016a, Soares et al., 2016b). For instance, administration of gal

• br Materials and methods br Results

  2021-09-10

  

  Materials and methods Results Bgal from Alteromonas sp. ML117 had an open reading frame of 3126 bp encoding 1042 amino ubiquitin residues with a predicted mass of 120 kDa and a theoretical pI (isoelectric point) of 5.44. The recombinant Bgal contained a His tag, as well as other additional am

• PF-431396 Introduction RNA splicing occurs in the nucleus wh

  2021-09-10

  

  Introduction RNA splicing occurs in the nucleus when noncoding sequences (introns) are removed from the pre-mRNA transcript and coding sequences (exons) are joined to form a mature mRNA [1,2]. This reaction is catalyzed by a multiprotein complex called spliceosome. The spliceosome consists of five

• CDX is also a tumor suppressor gene the ablation

  2021-09-10

  

  CDX1 is also a tumor suppressor gene; the ablation of CDX1 and CDX2 results in a significant increase in tumor formation in the colon. CDX1 is regulated by epigenetic modification; the hypermethylation of the CpG island at the promoter is positively associated with severe clinical phenotypes. In add

• pilocarpine hcl br Experimental br Acknowledgments We

  2021-09-10

  

  Experimental Acknowledgments We thank Mintek and Rhodes University for generous financial support and permission to publish these findings. T.O.O. gratefully acknowledges Obafemi Awolowo University, Ile-Ife, Nigeria for study leave. Introduction There are ∼35.3 million people living with H

• Although we showed that RBL H Sc cells

  2021-09-10

  

  Although we showed that RBL-2H3 Sc98 pmsf took up histamine from the microenvironment, it was unclear which transporter mediated its passage across the plasma membrane. Other biogenic amines have selective transporters that belong to the neurotransmitter sodium symporter family, including SERT for

• In the course of studies leading to the discovery

  2021-09-10

  

  In the course of studies leading to the discovery of , modifications at the P3-P4 interface of these tripeptide-based inhibitors were examined with the goal of improving potency while maintaining a PK profile similar to . In this report, we summarize those studies which led to the identification of

• The differential tissue and ligand dependent signaling descr

  2021-09-10

  

  The differential tissue- and ligand-dependent signaling described here has important implications for the therapeutic potential of synthetic GPR109A agonists for the treatment of atherosclerosis. The failure of MK-0354, a biased, partial GPR109A agonist, to activate signaling pathways upstream of va

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