• Historically pharmacological investigations have been carrie

  2022-05-17

  

  Historically, pharmacological investigations have been carried out by first identifying a biological response to a ligand, and then subsequently using that ligand to identify the receptor(s) responsible for the response (Wilson et al., 1998). However, this approach needed revision with the discovery

• In this study we explore different mathematical

  2022-05-17

  

  In this study, we explore different mathematical models for describing the IVIVC of a preclinical dataset of 12 different dual GPR109A/GPR81 agonists. The objective is to establish a predictive model of in vivo lipolysis suppression in the rat based on in vitro potency data. First, a nonlinear mixed

• br Introduction High dose niacin or nicotinic acid has been

  2022-05-17

  

  Introduction High dose niacin, or nicotinic acid, has been used as an athero-protective drug for more than 50 years (Carlson, 2005, Offermanns, 2006). When taken in pharmacological doses (>1g/day), the nicotinic Org 25543 form of niacin modulates plasma lipid profiles including decreasing circul

• For a long time the mechanism for the

  2022-05-17

  

  For a long time, the mechanism for the TG-lowering effect of nicotinic 2 deoxy d glucose has been thought that the lowered NEFA substrate from adipose tissue limits TG production from the liver (so-called NEFA hypothesis) [[1], [2], [3], [4]]. However, recent emerging evidences have suggested the i

• br Introduction In the treatment

  2022-05-17

  

  Introduction In the treatment of patients with AIDS and human immunodeficiency virus type 1 (HIV-1), anti-retroviral therapy (ART), which uses anti-HIV drugs such as protease inhibitors, integrase inhibitors and reverse transferase inhibitors, has made a major contribution. There are still some s

• br Materials and Methods br Results All of the studied

  2022-05-16

  

  Materials and Methods Results All of the studied transporter genes were expressed at detectable levels in all the analyzed samples at mRNA level by means of applied rt-PCR method (CTCGS 21680 HCl receptor was observed for ABCC4, ABCC1, ABCG2, SLC22A3, and SLC22A18 (less than 10% of mean expres

• br Acknowledgments This research was supported by a grant

  2022-05-16

  

  Acknowledgments This research was supported by a grant from the Korea Health Technology R&D Project through the Korean Health Industry Development Institute (KHIDI), funded by the Ministry of Health & Welfare, Republic of Korea (grant number: HI17C0616). Dr. Jun-Mo Yang was supported by the Natio

• Introduction Human pathogenic Leishmania protozoa comprise d

  2022-05-16

  

  Introduction Human pathogenic Leishmania protozoa comprise 20 different species that are distributed throughout the world and cause the disease leishmaniasis [1]. Transmission primarily occurs through the bite of a female sand fly and clinical manifestations of the disease span from cutaneous lesio

• The most ubiquitous serine threonine phosphatases

  2022-05-16

  

  The most ubiquitous serine/threonine phosphatases, such as PP1, PP2A, and PP2B are known to contribute to the majority of phosphatase activity in the heart [4]. Dysregulation of these and other PPs have been found in numerous CVDs, including heart failure (HF), and may play a critical role in reduce

• Iodination of commercially available with

  2022-05-16

  

  Iodination of commercially available with excess ICl in AcOH gave a quantitative yield of , which was cyclized with benzyl thioamides to give the 2-benzyl-9,10-dihydro-4-1-thia-3,4-diaza-benzo[]azulenes . Coupling of the iodides with heterocycles including imidazoles, triazoles, or zinc cyanide us

• The effects of galanin on anxiety may depend on the

  2022-05-16

  

  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 ga

• br Conclusion br Methods br Introduction To predict

  2022-05-16

  

  Conclusion Methods Introduction To predict such topologies, several algorithms have been developed. Quadparser (QP), developed by the Balasubramanian group have taken an approach where sequences matching G≥nN≤mG≥nN≤mG≥nN≤mG≥n model in which the lengths of G-tracts are at least n and lengths

• In addition to the type of

  2022-05-16

  

  In addition to the type of food consumed, also the effect of calorie restriction (CR), i.e. an intermittent fasting and re-feeding cycles with concomitant fluctuations in the level of glucose and insulin, can affect the course of IBS through the modulation of the BA homeostasis. This type of nutriti

• Since we were able to reach low micromolar to sub

  2022-05-16

  

  Since we were able to reach low micromolar to sub-micromolar potency in both compound series (6 and 7), we were also keen on assessing the preliminary ADME profile (particularly with respect to plasma and liver microsomal stability) of the most active compounds from these series. As it is evident fr

• br Importance of iron and

  2022-05-16

  

  Importance of iron and lipoxygenase in ferroptosis What remains to be somewhat controversial is the role of iron and lipoxygenases (LOX) in the death process, specifically in lipid peroxidation. So far, iron chelators have been repeatedly shown to halt ferroptosis (hence its name) induced by chem

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