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Mice with GSTP knock out
2021-12-18

Mice with GSTP1 knock out show increased risk of skin cancer when exposed to carcinogens like polycyclic aromatic hydrocarbons [23]. Most of the genetic association studies have focused on GSTP1 c.313G > A variant which results in isoleucine to valine substitution at amino dillution residue number
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PBI is an agonist of GPR and acts as
2021-12-18

PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th
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In this study we explore
2021-12-18

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
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br Discussion Recent progresses in osteoblast biology reveal
2021-12-18

Discussion Recent progresses in osteoblast biology reveal that aerobic glycolysis was the main pathway to supply energy and materials that need by osteoblast differentiation [3]. In current study, we showed that LA enhanced the effect of PTH on osteblast differentiation and revealed an unrecogniz
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The manuscript provides mechanistic insights into the
2021-12-18

The manuscript provides mechanistic insights into the suppression of EGFR, BCRP, PKM2, and other cancer biomarkers in response to pharmacological inhibition of GPR55 with MNF and CID (Fig. 7). Firstly, inactivation of ERK has been previously demonstrated following treatment of PANC-1 matrix metallop
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A general synthetic pathway to these tricyclic structures is
2021-12-18

A general synthetic pathway to these tricyclic structures is described in (detailed procedures can be accessed in the patent application WO 2011/014520 A2). Benzylation of the appropriate ketoester using KHMDS, followed by treatment with DMF-dimethyl acetal yielded the racemic (dimethylamino)-methy
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In three independent groups identified GPR A
2021-12-18

In 2003, three independent groups identified GPR109A (HM74A) and GPR109B (HM74), two GPCRs, as the receptors for niacin., , GPR109A, which is present in all species, is a high affinity receptor for niacin., GPR109B, which is only present in human and chimpanzee, is a low affinity receptor for niac
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br Evolution of multiple GnRH forms
2021-12-18

Evolution of multiple GnRH forms and GnRH receptors across vertebrates GnRH is an evolutionary ancient peptide that first appears prior to the protostome-deuterostome split, and is a member of the GnRH-adipokinetic hormone-corazonin superfamily of peptides (Roch et al., 2011, Roch et al., 2014).
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Neurotransmitter transporters are rapidly recycled from
2021-12-18

Neurotransmitter transporters are rapidly recycled from and to the membrane. For instance, the GABA transporter GAT1 is recycled in a calcium and depolarization dependent manner. GAT1 located in the plasma membrane is internalized to a subpopulation of small vesicles different from the classical neu
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In the present study both experimental and theoretical studi
2021-12-18

In the present study, both experimental and theoretical studies were performed to explore the inhibitory mechanisms of indomethacin and its analogues towards GLOI. A remarkable correlation (=0.974) was derived for the four structurally similar NSAIDs and two curcumins between the experimental bindin
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Although we showed that RBL H Sc cells took up
2021-12-18

Although we showed that RBL-2H3 Sc98 fluvastatin sodium receptor 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 fami
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br Acknowledgments br The authors would like to acknowledge
2021-12-18

Acknowledgments The authors would like to acknowledge the technical assistance of J. Lee. This work was supported by the U.S. National Institute of Health grant HL111206 (to R.A.H.) the Italian Ministry for University and Research (MIUR 2010329EKE). Introduction The liver plays a vital role
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MAPK are involved in a large variety
2021-12-18

MAPK are involved in a large variety of solid and hematolgical neoplasms and, indeed, several components of the MAPK network have already been proposed as targets in cancer therapy, such as p38, JNK, ERK1/2, MEK1/2, RAF, RAS, DUSP1 and ERK5 [11], [12]. Among them, alteration of the RAS-RAF-MEK1/2-ER
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In the Joint United Nations Program on
2021-12-17

In 2015, the Joint United Nations Program on HIV/AIDS (UNAIDS) proposed that by 2020, 90% of people living with HIV should be aware of their HIV status, as the first part of 90-90-90 strategy to end AIDS epidemic. Early detection of HIV allows initiating care for proper treatment, which impacts in m
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In humans mutations in KDM A
2021-12-17

In humans, mutations in KDM5A, KDM5B, and KDM5C are found in patients with ID, implicating KDM5-regulated transcription in the development or activity of neuronal tissues (Vallianatos and Iwase, 2015). KDM5D is Y-linked, and its role in cognition remains uncharacterized. Mutations in KDM5C are the m
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