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https://www.readbyqxmd.com/read/28506584/development-of-nonsteroidal-glucocorticoid-receptor-modulators-based-on-n-benzyl-n-4-phenoxyphenyl-benzenesulfonamide-scaffold
#1
Hiromasa Yoshioka, Ayumi Yamada, Yuko Nishiyama, Hiroyuki Kagechika, Yuichi Hashimoto, Shinya Fujii
N-Benzyl-N-(4-phenoxyphenyl)benzenesulfonamide derivatives were developed as a novel class of nonsteroidal glucocorticoid receptor (GR) modulators, which are promising drug candidates for treating immune-related disorders. Focusing on the similarity of the GR and progesterone receptor (PR) ligand-binding domain (LBD) structures, we adopted our recently developed PR antagonist 10 as a lead compound and synthesized a series of derivatives. We found that the N-(4-phenoxyphenyl)benzenesulfonamide skeleton serves as a versatile scaffold for GR antagonists...
April 29, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28499078/genome-wide-analysis-of-the-lateral-organ-boundaries-domain-lbd-gene-family-in-eucalyptus-grandis-reveals-members-that-differentially-impact-secondary-growth
#2
Qiang Lu, Fenjuan Shao, Colleen Macmillan, Iain W Wilson, Karen van der Merwe, Steven G Hussey, Alexander A Myburg, Xiaomei Dong, Deyou Qiu
Lateral Organ Boundaries Domain (LBD) proteins are plant-specific transcription factors playing crucial roles in growth and development. However, the function of LBD proteins in Eucalyptus grandis remains largely unexplored. In the present study, LBD genes in E. grandis were identified and characterized using bioinformatics approaches. Gene expression patterns in various tissues and the transcriptional responses of EgLBDs to exogenous hormones were determined by qRT-PCR. Functions of the selected EgLBDs were studied by ectopically overexpressing in a hybrid poplar (Populus alba × Populus glandulosa)...
May 12, 2017: Plant Biotechnology Journal
https://www.readbyqxmd.com/read/28493531/ternary-complex-of-human-ror%C3%AE-ligand-binding-domain-inverse-agonist-and-smrt-peptide-shows-a-unique-mechanism-of-corepressor-recruitment
#3
Masato Noguchi, Akihiro Nomura, Ken Murase, Satoki Doi, Keishi Yamaguchi, Kazuyuki Hirata, Makoto Shiozaki, Shintaro Hirashima, Masayuki Kotoku, Takayuki Yamaguchi, Yoshiaki Katsuda, Ruo Steensma, Xioalin Li, Haiyan Tao, Bruno Tse, Morgan Fenn, Robert Babine, Erin Bradley, Paul Crowe, Scott Thacher, Tsuyoshi Adachi, Masafumi Kamada
Retinoid-related orphan receptor gamma (RORγ) directly controls the differentiation of Th17 cell and the production of interleukin-17, which plays an integral role in autoimmune diseases. To obtain insight into RORγ, we have determined the first crystal structure of a ternary complex containing RORγ ligand-binding domain (LBD) bound with a novel synthetic inhibitor and a repressor peptide, 22-mer peptide from silencing mediator of retinoic acid and thyroid hormone receptor (SMRT). Comparison of a binary complex of nonliganded (apo) RORγ-LBD with a nuclear receptor co-activator (NCoA-1) peptide has shown that our inhibitor displays a unique mechanism different from those caused by natural inhibitor, ursolic acid (UA)...
May 11, 2017: Genes to Cells: Devoted to Molecular & Cellular Mechanisms
https://www.readbyqxmd.com/read/28474150/association-of-arterial-stiffness-with-cognition-in-patients-with-lewy-body-disorder
#4
Dong-Woo Ryu, Joong-Seok Kim, Jee-Eun Lee, Jeong-Wook Park, Yoon-Sang Oh, Jae-Young An, Kwang-Soo Lee
The brachial-ankle pulse wave velocity (baPWV) is a marker for arterial stiffness, which is associated with cardiovascular diseases. Arterial stiffness is associated with cognitive function in the elderly and patients with Alzheimer's disease (AD). We aimed to investigate the association between arterial stiffness and cognitive function in patients with Lewy body disorder (LBD), including Parkinson's disease (PD) and dementia with Lewy bodies (DLB). We consecutively included 123 patients with PD, 10 patients with DLB, and 27 AD controls...
May 5, 2017: Neurological Sciences
https://www.readbyqxmd.com/read/28472464/the-arabidopsis-jagged-lateral-organs-jlo-gene-sensitizes-plants-to-auxin
#5
Madlen I Rast-Somssich, Petra Žádníková, Stephan Schmid, Martin Kieffer, Stefan Kepinski, Rüdiger Simon
Plant growth and development of new organs depend on the continuous activity of the meristems. In the shoot, patterns of organ initiation are determined by PINFORMED (PIN)-dependent auxin distribution, while the undifferentiated state of meristem cells requires activity of KNOTTED LIKE HOMEOBOX (KNOX) transcription factors. Cell proliferation and differentiation of the root meristem are regulated by the largely antagonistic functions of auxin and cytokinins. It has previously been shown that the transcription factor JAGGED LATERAL ORGANS (JLO), a member of the LATERAL ORGAN BOUNDARY DOMAIN (LBD) family, coordinates KNOX and PIN expression in the shoot and promotes root meristem growth...
May 2, 2017: Journal of Experimental Botany
https://www.readbyqxmd.com/read/28468946/novel-mode-of-antagonist-binding-in-nmda-receptors-revealed-by-the-crystal-structure-of-the-glun1-glun2a-ligand-binding-domain-complexed-to-nvp-aam077
#6
Annabel Romero-Hernandez, Hiro Furukawa
Competitive antagonists against N-methyl-D-aspartate (NMDA) receptors have played critical roles throughout the history of neuropharmacology and basic neuroscience. There are currently numerous NMDA receptor antagonists containing a variety of chemical groups. Among those compounds, a GluN2-specific antagonist, (R)-[(S)-1-(4-bromo-phenyl)-ethylamino]-(2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-yl)-methyl]-phosphonic acid (NVP-AAM077), contains a unique combination of a dioxoquinoxalinyl ring, a bromophenyl group, and a phosphono group...
May 3, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28459509/effects-of-basic-traditional-chinese-diet-on-body-mass-index-lean-body-mass-and-eating-and-hunger-behaviours-in-overweight-or-obese-individuals
#7
Frida Leonetti, Aldo Liguori, Filomena Petti, Susanna Rughini, Laura Silli, Stefano Liguori, Sergio Bangrazi
OBJECTIVE: To compare the effects of a basic traditional Chinese diet with a Western standard diet on body mass index (BMI), lean body mass (LBD), and eating and hunger behaviours. METHODS: A sample of 284 patients were randomized into 2 groups: group A (n = 142) followed a basic traditional Chinese diet (BCTD) and group B (n = 142) followed a Western standard diet (WSD). Both diets were set at approximately 1200 calories. The patients enrolled were compared before treatment and 6 weeks after treatment, and then follow-ups were made at 1 year and 5 years...
August 2016: Journal of Traditional Chinese Medicine, Chung i Tsa Chih Ying Wen Pan
https://www.readbyqxmd.com/read/28439742/exploration-of-the-binding-affinities-between-ecdysone-agonists-and-ecr-usp-by-docking-and-mm-pb-gbsa-approaches
#8
Xueping Hu, Jin Xie, Song Hu, Li Zhang, Yanhong Dong
Ecdysone receptor (EcR) is a significant target in the identification of new environmentally friendly pesticides. There are two types of ecdysone agonists: steroidal ecdysone agonists and dibenzoylhydrazines (DBHs). In this study, various modeling methods (homology modeling, molecular docking, MD simulation, binding free energy calculation, and per-residue binding free energy decomposition) were utilized to study the different binding mechanisms of two types of ecdysone agonists. Our theoretical results indicated that the relative binding potencies of DBHs can be ranked sufficiently accurately using the MOE docking method...
May 2017: Journal of Molecular Modeling
https://www.readbyqxmd.com/read/28438556/the-brain-and-the-subjective-experience-of-time-a-voxel-based-symptom-lesion-mapping-study
#9
Luigi Trojano, Michelina Caccavale, Francesco De Bellis, Claudio Crisci
The aim of the study was to identify the anatomical bases involved in the subjective experience of time, by means of a voxel based symptom-lesion mapping (VLSM) study on patients with focal brain damage. Thirty-three patients (nineteen with right-hemisphere lesions -RBD, and fourteen with left lesion- LBD) and twenty-eight non-neurological controls (NNC) underwent the semi-structured QUEstionnaire for the Subjective experience of Time (QUEST) requiring retrospective and prospective judgements on self-relevant time intervals...
April 21, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28436456/synthesis-and-anti-obesity-effects-in-vivo-of-crotadihydrofuran-c-as-a-novel-ppar%C3%AE-antagonist-from-crotalaria-albida
#10
Qin-Hu Sun, Yu Zhang, Gui-Xin Chou
Crotadihydrofuran C (CC) from the herbs of Crotalaria albida is able to inhibit adipocyte differentiation and lipid accumulation. However, the effects of CC on obesity and metabolic disorders have not yet been elucidated. In our study, the first enantioselective synthesis of the 2-isopropenyl dihydrofuran isoflavone skeleton (CC) is described. The convenient and efficient synthetic protocols developed skilfully solve the problems of the ortho-para directing group and Suzuki coupling reaction using a boronic acid pinacol ester that was more stable and easy to obtain...
April 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28412386/characterization-of-rodent-constitutively-active-estrogen-receptor-%C3%AE-variants-and-their-constitutive-transactivation-mechanisms
#11
Hirotaka Ishii, Yujiro Hattori, Arisa Munetomo, Hiroshi Watanabe, Yasuo Sakuma, Hitoshi Ozawa
Estrogen receptor α (ERα) mRNAs exhibit remarkable heterogeneity owing to complicated alternative splicing. Some encode C-terminally-truncated ERα proteins, which display ligand-independent transactivation or dominant-negative activity. We previously characterized C-terminally-truncated ERα mRNA variants with cryptic sequences in humans and mice, and demonstrated that helices in the ligand-binding domains (LBDs) of ERα variants contribute to ligand-independent transcriptional activity. However, existence of non-conventional coding exons and generation of constitutively active ERα variants have remained to be examined in rats...
April 13, 2017: General and Comparative Endocrinology
https://www.readbyqxmd.com/read/28411541/spectroscopic-and-molecular-modeling-approaches-to-investigate-the-interaction-of-bisphenol-a-bisphenol-f-and-their-diglycidyl-ethers-with-ppar%C3%AE
#12
Jie Zhang, Tiehua Zhang, Tianzhu Guan, Ping Ruan, Dayong Ren, Weichang Dai, Hansong Yu, Tiezhu Li
A fluorescence polarization (FP) assay for the simultaneous determination of bisphenol A (BPA), bisphenol F (BPF), bisphenol A diglycidyl ether (BADGE) and bisphenol F diglycidyl ether (BFDGE) was developed. The method was based on the competition between bisphenols (BPs) and fluorescein-labeled dexamethasone derivative (Dex-fl) for mouse peroxisome proliferator-activated receptor α ligand binding domain (mPPARα-LBD). A recombinant soluble protein derivative mPPARα-LBD* was prepared, then in vitro binding of 4 BPs to mPPARα-LBD* was investigated...
April 9, 2017: Chemosphere
https://www.readbyqxmd.com/read/28401333/interactions-of-pathological-proteins-in-neurodegenerative-diseases
#13
REVIEW
Tara L Spires-Jones, Johannes Attems, Dietmar Rudolf Thal
Neurodegenerative diseases such as Alzheimer's disease (AD), frontotemporal lobar degeneration (FTD), Lewy body disease (LBD), Parkinson's disease (PD), and amyotrophic lateral sclerosis (ALS) have in common that protein aggregates represent pathological hallmark lesions. Amyloid β-protein, τ-protein, α-synuclein, and TDP-43 are the most frequently aggregated proteins in these disorders. Although they are assumed to form disease-characteristic aggregates, such as amyloid plaques and neurofibrillary tangles in AD or Lewy bodies in LBD/PD, they are not restricted to these clinical presentations...
April 11, 2017: Acta Neuropathologica
https://www.readbyqxmd.com/read/28396564/structural-analysis-of-the-glucocorticoid-receptor-ligand-binding-domain-in-complex-with-triamcinolone-acetonide-and-a-fragment-of-the-atypical-coregulator-shp
#14
Emily R Weikum, Denise C Okafor, Emma H D'Agostino, Jennifer K Colucci, Eric A Ortlund
The synthetic glucocorticoids (GCs) dexamethasone, mometasone furoate, and triamcinolone acetonide have been pharmaceutical mainstays to treat chronic inflammatory diseases. These drugs bind to the glucocorticoid receptor (GR), a ligand- activated transcription factor and member of the nuclear receptor superfamily. GR is widely recognized as a therapeutic target for its ability to counter pro-inflammatory signaling. Despite the popularity of GCs in the clinic, long-term use leads to numerous side effects, driving the need for new and improved drugs with less off-target pharmacology...
April 10, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28395086/regional-overlap-of-pathologies-in-lewy-body-disorders
#15
Martí Colom-Cadena, Oriol Grau-Rivera, Lluís Planellas, Catalina Cerquera, Estrella Morenas, Sergio Helgueta, Laia Muñoz, Jaime Kulisevsky, Maria Jose Martí, Eduard Tolosa, Jordi Clarimon, Alberto Lleó, Ellen Gelpi
Lewy body disorders (LBD) are common neurodegenerative diseases characterized by the presence of aggregated α-synuclein in Lewy bodies and Lewy neurites in the central and peripheral nervous systems. The brains of patients with LBD often display other comorbid pathologies, i.e. insoluble tau, β-amyloid aggregates, TAR DNA-binding protein 43 (TDP-43) deposits, and argyrophilic grain disease (AGD). The incidence and physiological relevance of these concurrent pathological findings remain controversial. We performed a semiquantitative detailed mapping of α-synuclein, tau, β-amyloid (Aβ), TDP-43, and AGD pathologies in 17 areas in 63 LBD cases (44 with Parkinson disease [PD], 28 with dementia, and 19 with dementia with Lewy bodies)...
March 1, 2017: Journal of Neuropathology and Experimental Neurology
https://www.readbyqxmd.com/read/28391039/divergent-functional-connectivity-during-attentional-processing-in-lewy-body-dementia-and-alzheimer-s-disease
#16
Xenia Kobeleva, Michael Firbank, Luis Peraza, Peter Gallagher, Alan Thomas, David J Burn, John O'Brien, John-Paul Taylor
Attention and executive dysfunction are features of Lewy body dementia (LBD) but their neuroanatomical basis is poorly understood. To investigate underlying dysfunctional attention-executive network (EXEC) interactions, we examined functional connectivity (FC) in 30 patients with LBD, 20 patients with Alzheimer's disease (AD), and 21 healthy controls during an event-related functional magnetic resonance imaging (fMRI) experiment. Participants performed a modified Attention Network Test (ANT), where they were instructed to press a button in response to the majority direction of arrows, which were either all pointing in the same direction or with one pointing in the opposite direction...
March 18, 2017: Cortex; a Journal Devoted to the Study of the Nervous System and Behavior
https://www.readbyqxmd.com/read/28378791/computationally-discovered-potentiating-role-of-glycans-on-nmda-receptors
#17
Anton V Sinitskiy, Nathaniel H Stanley, David H Hackos, Jesse E Hanson, Benjamin D Sellers, Vijay S Pande
N-methyl-D-aspartate receptors (NMDARs) are glycoproteins in the brain central to learning and memory. The effects of glycosylation on the structure and dynamics of NMDARs are largely unknown. In this work, we use extensive molecular dynamics simulations of GluN1 and GluN2B ligand binding domains (LBDs) of NMDARs to investigate these effects. Our simulations predict that intra-domain interactions involving the glycan attached to residue GluN1-N440 stabilize closed-clamshell conformations of the GluN1 LBD. The glycan on GluN2B-N688 shows a similar, though weaker, effect...
April 5, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28367941/changes-in-bone-metabolic-parameters-following-oral-calcium-supplementation-in-an-adult-patient-with-vitamin-d-dependent-rickets-type-2a
#18
Yuka Kinoshita, Nobuaki Ito, Noriko Makita, Masaomi Nangaku, Seiji Fukumoto
Vitamin D-dependent rickets type 2A (VDDR2A) is a rare inherited disorder with decreased tissue responsiveness to 1,25-dihydroxyvitamin D [1,25(OH)2D], caused by loss of function mutations in the vitamin D receptor (VDR) gene. Approximately 50 types of mutations have been identified so far that change amino acids in either the N-terminal DNA binding domain (DBD) or the C-terminal ligand binding domain (LBD) of the VDR protein. The degree of responsiveness to 1,25(OH)2D varies between patients with VDDR2A, which may depend on their residual VDR function...
March 31, 2017: Endocrine Journal
https://www.readbyqxmd.com/read/28342864/oslbd37-and-oslbd38-two-class-ii-type-lbd-proteins-are-involved-in-the-regulation-of-heading-date-by-controlling-the-expression-of-ehd1-in-rice
#19
Chaonan Li, Shanshan Zhu, Huan Zhang, Liping Chen, Maohong Cai, Jiachang Wang, Juntao Chai, Fuqing Wu, Zhijun Cheng, Xiuping Guo, Xin Zhang, Jianmin Wan
LATERAL ORGAN BOUNDARIES DOMAIN (LBD) proteins are plant-specific transcription factors which are involved in many biological process of plant development, including lateral organ development, photomorphogenesis, pathogen response, pollen development and plant regeneration. Here, we report new functions of LBD proteins that participate in the regulation of heading date and yield in rice. OsLBD37 and OsLBD38 are two class II type LBD proteins, function as transcriptional activators. Overexpression of OsLBD37 and OsLBD38 separately causes delayed heading date and increased yield...
March 22, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28342850/structural-basis-for-differential-activities-of-enantiomeric-ppar%C3%AE-agonists-binding-of-s35-to-the-alternate-site
#20
Jun Young Jang, Minseob Koh, Hwan Bae, Doo Ri An, Ha Na Im, Hyoun Sook Kim, Ji Young Yoon, Hye-Jin Yoon, Byung Woo Han, Seung Bum Park, Se Won Suh
Peroxisome proliferator-activated receptor γ (PPARγ) is a member of the nuclear receptor superfamily. It functions as a ligand-activated transcription factor and plays important roles in the regulation of adipocyte differentiation, type 2 diabetes mellitus, and inflammation. Many PPARγ agonists bind to the canonical ligand-binding pocket near the activation function-2 (AF-2) helix (i.e., helix H12) of the ligand-binding domain (LBD). More recently, an alternate ligand-binding site was identified in PPARγ LBD; it is located beside the Ω loop between the helices H2' and H3...
June 2017: Biochimica et Biophysica Acta
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