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https://www.readbyqxmd.com/read/29749733/an-inexpensive-and-scalable-synthesis-of-shld
#1
Frederik Præstholm Jørgensen, Mikael Bols
A synthesis of the important FKBP-ligand Shld (or Shield-1) is reported. The synthesis avoids stoichiometric use of expensive and chiral reagents, maintains enantioselectivity and provides a high overall yield (39%). The main features in the method are enantioselective alkylation for preparation of the phenyl acetic acid moiety (building block A), catalytic enantioselective reduction for obtaining the chiral diaryl-1-propanol (building block C) and direct acylation of S-pipecolic tartrate rather than use of expensive Fmoc-pipecolic acid...
May 11, 2018: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/29733646/drug-inducible-control-of-lethality-genes-a-low-background-destabilizing-domain-architecture-applied-to-the-gal4-uas-system-in-drosophila
#2
Manjunatha Kogenaru, Mark Isalan
Destabilizing domains (DDs) are genetic tags that conditionally control the level of abundance of proteins-of-interest (POI) with specific stabilizing small-molecule drugs, rapidly and reversibly, in a wide variety of organisms. The amount of the DD-tagged fusion protein directly impacts its molecular function. Hence, it is important that the background levels be tightly regulated in the absence of any drug. This is especially true for classes of proteins that function at extremely low levels, such as lethality genes involved in tissue development and certain transcriptional activator proteins...
May 7, 2018: ACS Synthetic Biology
https://www.readbyqxmd.com/read/29671583/optochemical-control-of-protein-localization-and-activity-within-cell-like-compartments
#3
Reese M Caldwell, Jessica G Bermudez, David Thai, Chanat Aonbangkhen, Benjamin S Schuster, Taylor Courtney, Alexander Deiters, Daniel A Hammer, David M Chenoweth, Matthew C Good
We report inducible dimerization strategies for controlling protein positioning, enzymatic activity, and organelle assembly inside synthetic cell-like compartments upon photostimulation. Using a photocaged TMP-Haloligand compound, we demonstrate small molecule and light-induced dimerization of DHFR and Haloenzyme to localize proteins to a compartment boundary and reconstitute tripartite sfGFP assembly. Using photocaged rapamycin and fragments of split TEV protease fused to FRB and FKBP, we establish optical triggering of protease activity inside cell-size compartments...
April 19, 2018: Biochemistry
https://www.readbyqxmd.com/read/29587629/comparative-analysis-of-fkbp-family-protein-evaluation-structure-and-function-in-mammals-and-drosophila-melanogaster
#4
REVIEW
George Ghartey-Kwansah, Zhongguang Li, Rui Feng, Liyang Wang, Xin Zhou, Frederic Z Chen, Meng Meng Xu, Odell Jones, Yulian Mu, Shawn Chen, Joseph Bryant, Williams B Isaacs, Jianjie Ma, Xuehong Xu
BACKGROUND: FK506-binding proteins (FKBPs) have become the subject of considerable interest in several fields, leading to the identification of several cellular and molecular pathways in which FKBPs impact prenatal development and pathogenesis of many human diseases. MAIN BODY: This analysis revealed differences between how mammalian and Drosophila FKBPs mechanisms function in relation to the immunosuppressant drugs, FK506 and rapamycin. Differences that could be used to design insect-specific pesticides...
March 27, 2018: BMC Developmental Biology
https://www.readbyqxmd.com/read/29578710/chemogenomic-profiling-of-human-and-microbial-fk506-binding-proteins
#5
Sebastian Pomplun, Claudia Sippel, Andreas Hähle, Donald Tay, Kensuke Shima, Alina Klages, Can Murat Ünal, Benedikt Rieß, Hui Ting Toh, Guido Hansen, Ho Sup Yoon, Andreas Bracher, Peter Rainer Preiser, Jan Rupp, Michael Steinert, Felix Hausch
FK506-binding proteins (FKBPs) are evolutionary conserved proteins that display peptidyl-prolyl isomerase activity and act as co-receptors for immunosuppressants. Microbial macrophage infectivity potentiator (Mip) type FKBPs can enhance infectivity. However, developing drug-like ligands for FKBPs or Mips has proven difficult and many FKBPs/Mips still lack a biologically useful ligand. To explore the scope and potential of C5-substituted-[4.3.1]-aza-bicyclic sulfonamides as a broadly applicable class of FKBP inhibitors, we developed a new synthesis for the bicyclic core scaffold and used it to prepare a FKBP/Mip-focused library...
March 26, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29578315/genes-involved-in-stress-response-influence-lithium-efficacy-in-bipolar-patients
#6
Aleksandra Szczepankiewicz, Beata Narozna, Janusz K Rybakowski, Sebastian Kliwicki, Piotr Czerski, Monika Dmitrzak-Węglarz, Maria Skibińska, Joanna Twarowska-Hauser, Joanna Pawlak
OBJECTIVES: In mood disorders, chronic stimulation with stress results in aberrant regulation of the hypothalamic-pituitary-adrenal (HPA) axis. Lithium was shown to influence HPA axis function. The underlying genetic background as well as environmental context may influence the stress response, and therefore lithium efficacy. The aim of the present study was to analyze if genetic variants located in genes involved in HPA axis regulation affect the response to long-term lithium treatment in bipolar patients...
March 26, 2018: Bipolar Disorders
https://www.readbyqxmd.com/read/29565292/association-of-proteomics-changes-with-al-sensitive-root-zones-in-switchgrass
#7
Mahesh Rangu, Zhujia Ye, Sarabjit Bhatti, Suping Zhou, Yong Yang, Tara Fish, Theodore W Thannhauser
In this paper, we report on aluminum (Al)-induced root proteomic changes in switchgrass. After growth in a hydroponic culture system supplemented with 400 μM of Al, plants began to show signs of physiological stress such as a reduction in photosynthetic rate. At this time, the basal 2-cm long root tips were harvested and divided into two segments, each of 1-cm in length, for protein extraction. Al-induced changes in proteomes were identified using tandem mass tags mass spectrometry (TMT-MS)-based quantitative proteomics analysis...
March 22, 2018: Proteomes
https://www.readbyqxmd.com/read/29552333/bioinformatic-analysis-reveals-conservation-of-intrinsic-disorder-in-the-linker-sequences-of-prokaryotic-dual-family-immunophilin-chaperones
#8
Sailen Barik
The two classical immunophilin families, found essentially in all living cells, are: cyclophilin (CYN) and FK506-binding protein (FKBP). We previously reported a novel class of immunophilins that are natural chimera of these two, which we named dual-family immunophilin (DFI). The DFIs were found in either of two conformations: CYN-linker-FKBP (CFBP) or FKBP-3TPR-CYN (FCBP). While the 3TPR domain can serve as a flexible linker between the FKBP and CYN modules in the FCBP-type DFI, the linker sequences in the CFBP-type DFIs are relatively short, diverse in sequence, and contain no discernible motif or signature...
2018: Computational and Structural Biotechnology Journal
https://www.readbyqxmd.com/read/29551923/establishment-of-optimal-regulatory-network-of-colorectal-cancer-based-on-p42-3-protein
#9
Yibin Hao, Jianhua Zhang, Guoyong Shan, Ning Zhang, Wenwen Jin, Kejun Nan
Objective: to establish regulatory network of colorectal cancer involving p42.3 protein and to provide theoretical evidence for deep functional exploration of p42.3 protein in the onset and development of colorectal cancer. Methods: with protein similarity algorithm, reference protein set of p42.3 cell apoptosis was built according to structural features of p42.3. GO and KEGG databases were used to establish regulatory network of tumor cell apoptosis involving p42.3; meanwhile, the largest possible working pathway that involves p42...
December 2017: Saudi Journal of Biological Sciences
https://www.readbyqxmd.com/read/29390154/bacterial-gene-control-by-dna-looping-using-engineered-dimeric-transcription-activator-like-effector-tale-proteins
#10
Nicole A Becker, Tanya L Schwab, Karl J Clark, L James Maher
Genetic switches must alternate between states whose probabilities are dependent on regulatory signals. Classical examples of transcriptional control in bacteria depend on repressive DNA loops anchored by proteins whose structures are sensitive to small molecule inducers or co-repressors. We are interested in exploiting these natural principles to engineer artificial switches for transcriptional control of bacterial genes. Here, we implement designed homodimeric DNA looping proteins ('Transcription Activator-Like Effector Dimers'; TALEDs) for this purpose in living bacteria...
March 16, 2018: Nucleic Acids Research
https://www.readbyqxmd.com/read/29379118/regulation-of-kv2-1-channel-inactivation-by-phosphatidylinositol-4-5-bisphosphate
#11
Mayra Delgado-Ramírez, José J De Jesús-Pérez, Iván A Aréchiga-Figueroa, Jorge Arreola, Scott K Adney, Carlos A Villalba-Galea, Diomedes E Logothetis, Aldo A Rodríguez-Menchaca
Phosphatidylinositol 4,5-bisphosphate (PIP2 ) is a membrane phospholipid that regulates the function of multiple ion channels, including some members of the voltage-gated potassium (Kv) channel superfamily. The PIP2 sensitivity of Kv channels is well established for all five members of the Kv7 family and for Kv1.2 channels; however, regulation of other Kv channels by PIP2 remains unclear. Here, we investigate the effects of PIP2 on Kv2.1 channels by applying exogenous PIP2 to the cytoplasmic face of excised membrane patches, activating muscarinic receptors (M1R), or depleting endogenous PIP2 using a rapamycin-translocated 5-phosphatase (FKBP-Inp54p)...
January 29, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29361176/the-prolyl-isomerase-fkbp25-regulates-microtubule-polymerization-impacting-cell-cycle-progression-and-genomic-stability
#12
David Dilworth, Geoff Gudavicius, Xiaoxue Xu, Andrew K J Boyce, Connor O'Sullivan, Jason J Serpa, Misha Bilenky, Evgeniy V Petrochenko, Christoph H Borchers, Martin Hirst, Leigh Anne Swayne, Perry Howard, Christopher J Nelson
FK506 binding proteins (FKBPs) catalyze the interconversion of cis-trans proline conformers in proteins. Importantly, FK506 drugs have anti-cancer and neuroprotective properties, but the effectors and mechanisms underpinning these properties are not well understood because the cellular function(s) of most FKBP proteins are unclear. FKBP25 is a nuclear prolyl isomerase that interacts directly with nucleic acids and is associated with several DNA/RNA binding proteins. Here, we show the catalytic FKBP domain binds microtubules (MTs) directly to promote their polymerization and stabilize the MT network...
March 16, 2018: Nucleic Acids Research
https://www.readbyqxmd.com/read/29346269/identification-of-secreted-proteins-involved-in-nonspecific-dsrna-mediated-lutzomyia-longipalpis-ll5-cell-antiviral-response
#13
Andrea Martins-da-Silva, Erich Loza Telleria, Michel Batista, Fabricio Klerynton Marchini, Yara Maria Traub-Csekö, Antonio Jorge Tempone
Hematophagous insects transmit infectious diseases. Sand flies are vectors of leishmaniasis, but can also transmit viruses. We have been studying immune responses of Lutzomyia longipalpis , the main vector of visceral leishmaniasis in the Americas. We identified a non-specific antiviral response in L. longipalpis LL5 embryonic cells when treated with non-specific double-stranded RNAs (dsRNAs). This response is reminiscent of interferon response in mammals. We are investigating putative effectors for this antiviral response...
January 18, 2018: Viruses
https://www.readbyqxmd.com/read/29316283/split-cas9-not-hairs-advancing-the-therapeutic-index-of-crispr-technology
#14
REVIEW
Carolin Schmelas, Dirk Grimm
The discovery that the bacterial CRISPR/Cas9 system can be translated into mammalian cells continues to have an unprecedented impact on the biomedical research community, as it largely facilitates efforts to experimentally interrogate or therapeutically modify the cellular genome. In particular, CRISPR promises the ability to correct disease-associated genetic defects, or to target and destroy invading foreign DNA, in a simple, efficient, and selective manner directly in affected human cells or tissues. Here, we highlight a set of exciting new strategies that aim at further increasing the therapeutic index of CRISPR technologies, by reducing the size of Cas9 expression cassettes and thus enhancing their compatibility with viral gene delivery vectors...
January 5, 2018: Biotechnology Journal
https://www.readbyqxmd.com/read/29246765/fkbp12-immunopositive-inclusions-in-patients-with-%C3%AE-synucleinopathies
#15
Yasuyuki Honjo, Takashi Ayaki, Tomohisa Horibe, Hidefumi Ito, Ryosuke Takahashi, Koji Kawakami
α-Synuclein (α-SYN), a presynaptic protein with the tendency to aggregate, is linked to α-synucleinopathies such as Parkinson's disease (PD), dementia with Lewy bodies (DLB), and multiple system atrophy (MSA). α-SYN is the main component of round intracytoplasmic inclusions called Lewy bodies (LBs), which are the hallmark of PD and DLB. In addition, accumulation of amyloid-β and neurofibrillary tangles as in the pathology of Alzheimer's disease has been found in the DLB brain. Glial cytoplasmic inclusions are an MSA-specific type of inclusion found in oligodendrocytes and mainly comprise α-SYN...
February 1, 2018: Brain Research
https://www.readbyqxmd.com/read/29206196/the-fkbp51-glucocorticoid-receptor-co-chaperone-regulation-function-and-implications-in-health-and-disease
#16
REVIEW
Gabriel R Fries, Nils C Gassen, Theo Rein
Among the chaperones and co-chaperones regulating the glucocorticoid receptor (GR), FK506 binding protein (FKBP) 51 is the most intensely investigated across different disciplines. This review provides an update on the role of the different co-chaperones of Hsp70 and Hsp90 in the regulation of GR function. The development leading to the focus on FKBP51 is outlined. Further, a survey of the vast literature on the mechanism and function of FKBP51 is provided. This includes its structure and biochemical function, its regulation on different levels-transcription, post-transcription, and post-translation-and its function in signaling pathways...
December 5, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29194511/prolyl-isomerization-of-the-cenp-a-n-terminus-regulates-centromeric-integrity-in-fission-yeast
#17
Hwei Ling Tan, Kim Kiat Lim, Qiaoyun Yang, Jing-Song Fan, Ahmed Mahmoud Mohammed Sayed, Liy Sim Low, Bingbing Ren, Teck Kwang Lim, Qingsong Lin, Yu-Keung Mok, Yih-Cherng Liou, Ee Sin Chen
Centromeric identity and chromosome segregation are determined by the precise centromeric targeting of CENP-A, the centromere-specific histone H3 variant. The significance of the amino-terminal domain (NTD) of CENP-A in this process remains unclear. Here, we assessed the functional significance of each residue within the NTD of CENP-A from Schizosaccharomyces pombe (SpCENP-A) and identified a proline-rich 'GRANT' (Genomic stability-Regulating site within CENP-A N-Terminus) motif that is important for CENP-A function...
February 16, 2018: Nucleic Acids Research
https://www.readbyqxmd.com/read/29155566/structure-based-insights-into-the-dynamics-and-function-of-two-domain-slpa-from-escherichia-coli
#18
Anne-Juliane Geitner, Ulrich Weininger, Hauke Paulsen, Jochen Balbach, Michael Kovermann
SlpA (SlyD-like protein A) comprises two domains, a FK506 binding domain (FKBP fold) of moderate prolyl cis/trans-isomerase activity and an inserted in flap (IF) domain that hosts its chaperone activity. Here we present the nuclear magnetic resonance (NMR) solution structure of apo Escherichia coli SlpA determined by NMR that mirrors the structural properties seen for various SlyD homologues. Crucial structural differences in side-chain orientation arise for F37, which points directly into the hydrophobic core of the active site...
December 19, 2017: Biochemistry
https://www.readbyqxmd.com/read/29148176/differential-proteomic-analysis-reveals-protein-networks-and-pathways-that-may-contribute-to-helicobacter-pylori-fkbp-type-ppiase-associated-gastric-diseases
#19
Yanmei Zhu, Yuehua Gong, Aodi Li, Moye Chen, Dan Kang, Jun Liu, Yuan Yuan
PURPOSE: Though Helicobacter pylori (H. pylori) has been classified as class I carcinogen, key virulence factor generated by H. pylori that causes gastric cancer remains to be fully determined. Recently, we identified a gastric cancer-associated H. pylori gene, peptidylprolyl isomerase-FK506 binding protein (PPIase-FKBP), and showed that PPIase-FKBP was capable of inducing oncogenic transformation of gastric epithelial cells. But its mechanism was unclear. EXPERIMENTAL DESIGN: We carried out a comparative proteomic analysis of human gastric epithelial cells that either express PPIase-FKBP or green fluorescent protein using 2-DE and then MALDI-TOF-MS/MS...
November 16, 2017: Proteomics. Clinical Applications
https://www.readbyqxmd.com/read/29115621/effects-of-shield1-on-the-viral-replication-of-varicella%C3%A2-zoster-virus-containing-fkbp%C3%A2-tagged-orf4-and-48
#20
Shuying Li, Zhanjun Liu, Ji Li, Aihua Liu, Lihua Zhu, Kui Yu, Ke Zhang
The present study aimed to explore the effects of a stabilizing ligand, Shield‑1, on the replication of recombinant varicella‑zoster virus (VZV) containing FK506 binding protein (FKPB) tags in essential open reading frames (ORF) 4 and 48. A specific galactokinase (galK) selection method was conducted, following the addition of galK labels to VZV ORF4 and 48, using a SW102 VZV bacterial artificial chromosome (BAC) system. Subsequently, recombinant VZV containing FKPB tags in ORF4 and 48 was constructed by counterselection and homologous recombination...
January 2018: Molecular Medicine Reports
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