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While previously reported optimizations on
2021-04-20

While previously reported optimizations on cyclin dependent kinase inhibitor focused on the phenyl ring A () and substituents on isoxazole ring, other alternatives to replace isoxazole ring were never explored. Herein, we propose to replace the isoxazole with its bioisosteric substituted phenyl ri
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br Cytochrome P monooxygenases Cytochrome P monooxygenases
2021-04-20

Cytochrome P450 monooxygenases Cytochrome P450 monooxygenases (P450s) belong to one of Nature’s most versatile group of enzymes for C–H functionalization and are able to perform challenging regioselective and stereoselective activations of remote, unactivated C(sp3)–H bonds, for which there are o
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br Transparency document br Acknowledgments This
2021-04-20

Transparency document Acknowledgments This study was funded by ICMR, Govt. of India. Alisha Dhiman acknowledges UGC-DSKPDF, India for post-doctoral fellowship and Monisha Gopalani acknowledges CSIR, India for Senior Research Fellowship. AIRF, JNU is acknowledged for TEM, confocal microscopy an
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In regards to regional variation in metabolic behavior of ad
2021-04-20

In regards to regional variation in metabolic behavior of adipose tissue, subcutaneous adipose tissue transplantation has been shown to reprogram visceral adipose tissue to have subcutaneous-like phenotypic behavior, whereas visceral-to-subcutaneous transplantation does not promote a more detrimenta
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CYP A and CYP D
2021-04-20

CYP3A4/5 and CYP2D6 are among the main drug-metabolizing enzymes in humans that are responsible for the metabolism of more than 50% of marketed drugs [19], [21]. Drugs metabolized by CYPs are prone to drug–drug interactions, thereby modifying their response [18], [32]. Metabolic inhibition is also i
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Programmed cellular death or apoptosis is a process
2021-04-20

Programmed cellular death or apoptosis is a process genetically controlled that plays an important role in cellular homeostasis, being an important defense mechanism to remove cells that have been infected, damaged or mutated (Smith and Smith, 2012, Wlodkowic et al., 2011). Nevertheless, apoptosis s
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br Significance Dysregulation of dopamine homeostasis
2021-04-20

Significance Dysregulation of dopamine homeostasis contributes to Parkinson's disease (PD). The nuclear receptor Nurr1 plays a central role in dopamine homeostasis, regulating the transcription of MLN 2480 governing the synthesis, packaging, and reuptake of dopamine. Efforts to capitalize on Nurr
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Contrary to the profuse dopaminergic innervation of the thal
2021-04-20

Contrary to the profuse dopaminergic innervation of the thalamus found in human and non-human primates (Brown et al., 1979, Sanchez-Gonzalez et al., 2005), in rodents, the RTn is one the few thalamic nuclei that receives dopaminergic input (Anaya-Martinez et al., 2006, Garcia-Cabezas et al., 2007, G
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The Lysine mutant is located in
2021-04-20

The Lysine429 mutant is located in the tail region of 5-HT2A, which is predicted to be unstructured. This region has been shown to interact, in vitro, with PSD95 and leads to differences in signaling (Xia et al., 2003). The ASK motif, a component of the tail region, is also important for regulation
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Previous in vitro studies have demonstrated that DNA PK
2021-04-20

Previous in vitro studies have demonstrated that DNA-PK-deficient cell line (MO59J) is approximately 30-fold more sensitive to radiation than DNA-PK-proficient cell line (MO59K) [31]. Moreover, specific DNA-PK inhibitors SU11752 and wortmannin have been shown to sensitize GBM BI-D1870 synthesis (MO
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Some mechanistic experiments performed in the early
2021-04-20

Some mechanistic experiments performed in the early 2000s by Ongusaha et al. [78], suggest that DDR1 induction protects MAPK Inhibitor Library from apoptosis in a p53-dependent manner, and that impairment of DDR1 expression or function leads to a pronounced increase of DNA damage-induced apoptosis.
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The IP R is a ubiquitously
2021-04-20

The IP3R is a ubiquitously expressed Ca2+-release channel from the ER, activated by IP3, produced upon cellular stimulation by hormones, growth factors or neurotransmitters. Three genes are coding for the IP3R and their gene products (IP3R1, IP3R2, IP3R3) assemble in functional homo- or heterotetram
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Cells expressing the CDK S D mutant exhibit impaired
2021-04-20

Cells expressing the CDK5 S47D mutant exhibit impaired migration and enhanced proliferation: Finally, we wished to determine the functional significance of this phosphoevent. Multiple studies have implicated active CDK5 in promotion of cell migration [9,16,[21], [22], [23], [24]] and in one study th
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MK-8745 The ability of TKIs in inducing CRTH expression
2021-04-20

The ability of TKIs in inducing CRTH2 expression could be related to the c-terminal of CRTH2 receptor that is important molecular determinant in the down-stream signaling cascade activation [20]. This requires further studies to prove it or disprove it. Additionally, further studies are needed to ex
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R-848 receptor Fear like behaviors are produced by intracere
2021-04-19

Fear-like behaviors are produced by intracerebroventricular CRF administration (Meloni et al., 2006, Radulovic et al., 1999), as well its administration into specific R-848 receptor areas such as the amygdala (Daniels et al., 2004, Donatti and Leite-Panissi, 2011), the periaqueductal gray matter (M
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