Design and chemoproteomic functional characterization of a chemical probe targeted to bromodomains of BET family proteins

MedChemComm ◽  
2014 ◽  
Vol 5 (12) ◽  
pp. 1871-1878 ◽  
Author(s):  
Jiang Wu ◽  
Julia Shin ◽  
Cara M. M. Williams ◽  
Kieran F. Geoghegan ◽  
Stephen W. Wright ◽  
...  
Keyword(s):  
Functional Characterization ◽  
Human Cells ◽  
Chemical Probe ◽  
Affinity Capture ◽  
Nuclear Extracts

Selectivity of a PFI-1 based BET bromodomain probe was demonstrated using affinity capture in nuclear extracts from human cells.

scholarly journals Correction: Design and chemoproteomic functional characterization of a chemical probe targeted to bromodomains of BET family proteins

MedChemComm ◽  
2015 ◽  
Vol 6 (1) ◽  
pp. 247-247
Author(s):  
Jiang Wu ◽  
Julia Shin ◽  
Cara M. M. Williams ◽  
Kieran F. Geoghegan ◽  
Stephen W. Wright ◽  
...  
Keyword(s):  
Functional Characterization ◽  
Chemical Probe

Correction for ‘Design and chemoproteomic functional characterization of a chemical probe targeted to bromodomains of BET family proteins’ by Jiang Wu et al., Med. Chem. Commun., 2014, 5, 1871–1878.

scholarly journals Identification and functional characterization of transcriptional activators in human cells

2022 ◽  
Author(s):  
Nader Alerasool ◽  
He Leng ◽  
Zhen-Yuan Lin ◽  
Anne-Claude Gingras ◽  
Mikko Taipale
Keyword(s):  
Functional Characterization ◽  
Human Cells ◽  
Transcriptional Activators

scholarly journals Functional characterization of ribosomal P1/P2 proteins in human cells

2008 ◽  
Vol 413 (3) ◽  
pp. 527-534 ◽  
Author(s):  
Francisco Martinez-Azorin ◽  
Miguel Remacha ◽  
Juan P. G. Ballesta
Keyword(s):  
Functional Characterization ◽  
Ribosomal Subunit ◽  
Human Cell Line ◽  
Human Cells ◽  
Translation Efficiency ◽  
Ribosomal Stalk ◽  
P Proteins ◽  
Subunit Joining

The ‘stalk’ is a large ribosomal subunit domain that regulates translation. In the present study the role of the ribosomal stalk P proteins in modulating ribosomal activity has been investigated in human cells using RNA interference. A strong down-regulation of P2 mRNA and a drastic decrease in P2 protein in a stable human cell line was achieved using a doxycycline-inducible system. Interestingly, the amount of P1 protein was similarly decreased in these cells, in contrast with the expression of P1 mRNA. The loss of P1/P2 proteins produced a decrease in the growth rate of these cells, as well as an altered polysome pattern with reduced translation efficiency, but without affecting the free 40 S/60 S subunit ratio. A decrease in the ribosomal-subunit joining capacity was also observed. These data indicate that P1/P2 proteins modulate cytoplasmic translation by influencing the interaction between subunits, thereby regulating the rate of cell proliferation.

scholarly journals Functional Characterization of Novel Human and Mouse Equilibrative Nucleoside Transporters (hENT3 and mENT3) Located in Intracellular Membranes

2005 ◽  
Vol 280 (16) ◽  
pp. 15880-15887 ◽  
Author(s):  
Stephen A. Baldwin ◽  
Sylvia Y. M. Yao ◽  
Ralph J. Hyde ◽  
Amy M. L. Ng ◽  
Sophie Foppolo ◽  
...  
Keyword(s):  
Plasma Membranes ◽  
Functional Characterization ◽  
Human Cells ◽  
Nucleoside Transporters ◽  
Nucleoside Transport ◽  
Nucleoside Transporter ◽  
Transport Activity ◽  
Transporter Family ◽  
Human And Mouse

The first mammalian examples of the equilibrative nucleoside transporter family to be characterized, hENT1 and hENT2, were passive transporters located predominantly in the plasma membranes of human cells. We now report the functional characterization of members of a third subgroup of the family, from human and mouse, which differ profoundly in their properties from previously characterized mammalian nucleoside transporters. The 475-residue human and mouse proteins, designated hENT3 and mENT3, respectively, are 73% identical in amino acid sequence and possess long N-terminal hydrophilic domains that bear typical (DE)XXXL(LI) endosomal/lysosomal targeting motifs. ENT3 transcripts and proteins are widely distributed in human and rodent tissues, with a particular abundance in placenta. However, in contrast to ENT1 and ENT2, the endogenous and green fluorescent protein-tagged forms of the full-length hENT3 protein were found to be predominantly intracellular proteins that co-localized, in part, with lysosomal markers in cultured human cells. Truncation of the hydrophilic N-terminal region or mutation of its dileucine motif to alanine caused the protein to be relocated to the cell surface both in human cells and inXenopusoocytes, allowing characterization of its transport activity in the latter. The protein proved to be a broad selectivity, low affinity nucleoside transporter that could also transport adenine. Transport activity was relatively insensitive to the classical nucleoside transport inhibitors nitrobenzylthioinosine, dipyridamole, and dilazep and was sodium ion-independent. However, it was strongly dependent upon pH, and the optimum pH value of 5.5 probably reflected the location of the transporter in acidic, intracellular compartments.

scholarly journals Structural and Functional Characterization of Noncoding Repetitive RNAs Transcribed in Stressed Human Cells

2005 ◽  
Vol 16 (6) ◽  
pp. 2597-2604 ◽  
Author(s):  
Rut Valgardsdottir ◽  
Ilaria Chiodi ◽  
Manuela Giordano ◽  
Fabio Cobianchi ◽  
Silvano Riva ◽  
...  
Keyword(s):  
Functional Characterization ◽  
Human Cells ◽  
Heat Shock Factor 1 ◽  
Small Interfering Rnas ◽  
Argonaute 2 ◽  
Specific Subset ◽  
Nuclear Structures ◽  
Sirna Knockdown ◽  
Processing Factors

Thermal and chemical stresses induce the formation in human cells of novel and transient nuclear structures called nuclear stress bodies (nSBs). These contain heat shock factor 1 (HSF-1) and a specific subset of pre-mRNA processing factors. Nuclear stress bodies are assembled on specific pericentromeric heterochromatic domains containing satellite III (SatIII) DNA. In response to stress, these domains change their epigenetic status from heterochromatin to euchromatin and are transcribed in poly-adenylated RNAs that remain associated with nSBs. In this article, we describe the cloning, sequencing, and functional characterization of these transcripts. They are composed of SatIII repeats and originate from the transcription of multiple sites within the SatIII arrays. Interestingly, the level of SatIII RNAs can be down-regulated both by antisense oligonucleotides and small interfering RNAs (siRNA). Knockdown of SatIII RNA by siRNAs requires the activity of Argonaute 2, a component of the RNA-induced silencing complex. Down-regulation of satellite III RNAs significantly affects the recruitment of RNA processing factors to nSBs without altering the association of HSF-1 with these structures nor the presence of acetylated histones within nSBs. Thus, satellite III RNAs have a major role in the formation of nSBs.

Functional characterization of human brown adipose tissue metabolism

2020 ◽  
Vol 477 (7) ◽  
pp. 1261-1286 ◽  
Author(s):  
Marie Anne Richard ◽  
Hannah Pallubinsky ◽  
Denis P. Blondin
Keyword(s):  
Adipose Tissue ◽  
Brown Adipose Tissue ◽  
Functional Characterization ◽  
Human Infants ◽  
Positron Emission ◽  
Brown Adipose ◽  
Treatment Of Obesity ◽  
And Function

Brown adipose tissue (BAT) has long been described according to its histological features as a multilocular, lipid-containing tissue, light brown in color, that is also responsive to the cold and found especially in hibernating mammals and human infants. Its presence in both hibernators and human infants, combined with its function as a heat-generating organ, raised many questions about its role in humans. Early characterizations of the tissue in humans focused on its progressive atrophy with age and its apparent importance for cold-exposed workers. However, the use of positron emission tomography (PET) with the glucose tracer [18F]fluorodeoxyglucose ([18F]FDG) made it possible to begin characterizing the possible function of BAT in adult humans, and whether it could play a role in the prevention or treatment of obesity and type 2 diabetes (T2D). This review focuses on the in vivo functional characterization of human BAT, the methodological approaches applied to examine these features and addresses critical gaps that remain in moving the field forward. Specifically, we describe the anatomical and biomolecular features of human BAT, the modalities and applications of non-invasive tools such as PET and magnetic resonance imaging coupled with spectroscopy (MRI/MRS) to study BAT morphology and function in vivo, and finally describe the functional characteristics of human BAT that have only been possible through the development and application of such tools.

Identification and Functional Characterization of CYP2D6*10 and CYP2D6*15 in the Uighur population

2010 ◽  
Vol 34 (8) ◽  
pp. S34-S34
Author(s):  
SiFan XU ◽  
XuCong Man ◽  
ShuChun Li
Keyword(s):  
Functional Characterization
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