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Despite hydrolysis with commercial enzymes like trypsin peps
2024-03-20

Despite hydrolysis with commercial enzymes like trypsin, pepsin, Alcalase, Flavourzyme and Thermolysin have been used to digest parent proteins and generate peptides, microbial fermentation by proteolytic species has also proved to be a successful strategy (Fakhfakh et al., 2013, Jemil et al., 2016,
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Nevertheless though the LO pathway dictates
2024-03-20

Nevertheless, though the 5-LO pathway dictates the production of lipid mediators with opposite roles in the immune reactions, like LTs and LXA4 [32], our results seemed to corroborate others that pointed to LTB4 as an outstanding mediator involved in persistent and chronic inflammatory skin diseases
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br Cytochrome b br Cytochrome P
2024-03-20

Cytochrome b5 Cytochrome P450 17α-hydroxylase/17,20-lyase (P450 17A1) A number of P450s involved in steroid biosynthesis are multifunctional as they carry out two or more sequential hydroxylation reactions on the same substrate(s). P450 17A1 is a dual function endoplasmic reticulum enzyme enco
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Steroidal CYP inhibitors can further
2024-03-18

Steroidal CYP17 inhibitors can further be classified based on their mode of action, namely as mechanism-based inhibitors and type I and type II competitive inhibitors [129]. Recent studies investigated other biological targets than CYP17, and some new compounds have shown interesting dual activity a
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br Aurora A Aurora B
2024-03-18

Aurora-A, Aurora-B and Aurora-C small molecule inhibitors Nicholas et al. described phenotypic cellular screening of new highly potent and selective class of Aurora kinase inhibitors. Fragment based approach was utilized; core structure of 57 (Fig. 5) was optimized and selective inhibitor 58 (Fig
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Loss of expression or functional activity
2024-03-18

Loss of expression or functional activity of cell adhesion is intricately related to advanced stages of tumour progression and invasiveness. Martin-Belmonte and Perez-Moreno recently mentioned that the deregulation of adhesion can alter tumourgenesis in the early stage. We have shown for the first t
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exemplifies three of the compounds investigated in the
2024-03-18

exemplifies three of the compounds investigated in the selection for a candidate drug (CD). Our first criteria was an IC phosphatidylinositol 4-kinase as such did not show any genotoxicity in the SOS/umu assay, but this does not say anything about any possible genotoxicity of its metabolites or degr
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br Acknowledgments br Introduction Cancer is a deadly
2024-03-18

Acknowledgments Introduction Cancer is a deadly disease of uncontrolled cell division and has the potential to invade or spread to other parts of the body and affects normal functioning of the vital organs. Nowadays cancer is considered as leading cause of human death in all over the world and
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AP plays a pivotal role in transcriptional regulation of MMP
2024-03-18

AP-1 plays a pivotal role in transcriptional regulation of MMP expression. The decoy technique allows the neutralization of AP-1 without any transfection reagents for cellular uptake that cause potential side effects or immune reactions. This energy-dependent transport mechanism of “naked” dODN is c
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br Prostate cancer and resistance to
2024-03-18

Prostate cancer and resistance to AR targeting treatment The AR plays a pivotal role in the development, differentiation, homeostasis and secretory function of the normal prostate (Wilson, 2011). The AR is also a key player in many phases of prostate carcinogenesis (Huggins et al., 1941, Scher an
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br Author contributions br Acknowledgements We thank Dr
2024-03-18

Author contributions Acknowledgements We thank Dr. Bob Hammer and the Transgenic Core Facility at UTSW for the generation of the transgenic lines, John Shelton and the Histology Core for assistance with histology and the UTSW Metabolic Core Unit for help in phenotyping. We acknowledge support
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Our studies also reveal the normal functional roles of the
2024-03-16

Our studies also reveal the normal functional roles of the MIR. Interaction between the MIR loop and the N-terminal α helix nucleates conformational maturation of AChR subunits, thereby promoting assembly of mature AChRs [52], [55]. This interaction in homologous parts of all AChR subunits appears t
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Owing to efficient catalytic character high electrolyte
2024-03-16

Owing to efficient catalytic character, high electrolyte accessible area, easy fabrication and many other interesting properties, metal oxide nanoparticles are extensively used in a variety of electro-analytical processes [14]. Metal oxide nanoparticles immobilized over a conductive and large area s
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As a continuation of our search for a selective
2024-03-16

As a continuation of our search for a selective AChE radioligand bearing a meta-F substituted N-benzyl moiety, we designed and synthesized a novel meta-F-CP-118,954 analog along with a meta-18F-labeled form via diaryliodonium salt-based precursor (Fig. 1). For comparative purposes, we incorporate th
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br Disclosure br Acknowledgement br Introduction CYP
2024-03-16

Disclosure Acknowledgement Introduction CYP17A1 is a multifunctional enzyme with both 17α-hydroxylase and 17,20-lyase activities and is essential for the biosynthesis of steroidal Mechlorethamine HCl in male testes and adrenal glands. The 17α-hydroxylase activity of CYP17A1 is involved in
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