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cyclophilin

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https://www.readbyqxmd.com/read/28919180/development-of-a-cyclosporin-a-derivative-with-excellent-anti-hepatitis-c-virus-potency
#1
Jiping Fu, Christopher Becker, Li Cao, Michael Capparelli, Regis Denay, Roger Fujimoto, Yu Gai, Zhaobo Gao, Christian Guenat, Subramanian Karur, Hongyong Kim, Weikuan Li, Xiaolin Li, Wei Li, Thomas Lochmann, Amy Lu, Peichao Lu, Alexandre Luneau, Nicole Meier, Wosenu Mergo, Simon Ng, David Parker, Yunshan Peng, Bernard Riss, Alexey Rivkin, Silvio Roggo, Harald Schroeder, Friedrich Schuerch, Robert L Simmons, Feng Sun, Zachary K Sweeney, Meiliana Tjandra, Michael Wang, Ruidong Wang, Andrew H Weiss, Nicolas Wenger, Quanbing Wu, Xin Xiong, Su Xu, Wenjian Xu, Aregahegn Yifru, Jibin Zhao, Jianguang Zhou, Christian Zürcher, Fabrice Gallou
Synthetic modification of cyclosporin A at P3-P4 positions led to the discovery of NIM258, a next generation cyclophilin inhibitor with excellent anti-hepatitis C virus potency, with decreased transporter inhibition, and pharmacokinetics suitable for coadministration with other drugs. Herein is disclosed the evolution of the synthetic strategy to from the original medicinal chemistry route, designed for late diversification, to a convergent and robust development synthesis. The chiral centers in the P4 fragment were constructed by an asymmetric chelated Claisen rearrangement in the presence of quinidine as the chiral ligand...
September 7, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28918503/coq0-induced-mitochondrial-ptp-opening-triggers-apoptosis-via-ros-mediated-vdac1-upregulation-in-hl-60-leukemia-cells-and-suppresses-tumor-growth-in-athymic-nude-mice-xenografted-nude-mice
#2
You-Cheng Hseu, Varadharajan Thiyagarajan, Ting-Tsz Ou, Hsin-Ling Yang
Coenzyme Q (CoQ) analogs with variable numbers of isoprenoid units have been demonstrated as anticancer and antioxidant/pro-oxidant molecules. This study examined the in vitro and in vivo antitumor and apoptosis activities of CoQ0 (2,3-dimethoxy-5-methyl-1,4-benzoquinone, zero isoprenoid side-chains) through upregulation of the Voltage-dependent anion channel 1 (VDAC1) signaling pathway on human promyelocytic leukemia. CoQ0 (0-40 μg/mL) treatment significantly reduced HL-60 cell viability, and up-regulated mitochondrial VDAC1 expression...
September 16, 2017: Archives of Toxicology
https://www.readbyqxmd.com/read/28913661/discovery-of-non-peptidic-small-molecule-inhibitors-of-cyclophilin-d-as-neuroprotective-agents-in-a%C3%AE-induced-mitochondrial-dysfunction
#3
Insun Park, Ashwini M Londhe, Ji Woong Lim, Beoung-Geon Park, Seo Yun Jung, Jae Yeol Lee, Sang Min Lim, Kyoung Tai No, Jiyoun Lee, Ae Nim Pae
Cyclophilin D (CypD) is a mitochondria-specific cyclophilin that is known to play a pivotal role in the formation of the mitochondrial permeability transition pore (mPTP).The formation and opening of the mPTP disrupt mitochondrial homeostasis, cause mitochondrial dysfunction and eventually lead to cell death. Several recent studies have found that CypD promotes the formation of the mPTP upon binding to β amyloid (Aβ) peptides inside brain mitochondria, suggesting that neuronal CypD has a potential to be a promising therapeutic target for Alzheimer's disease (AD)...
September 14, 2017: Journal of Computer-aided Molecular Design
https://www.readbyqxmd.com/read/28906548/activation-of-g-protein-coupled-estrogen-receptor-1-at-the-onset-of-reperfusion-protects-the-myocardium-against-ischemia-reperfusion-injury-by-reducing-mitochondrial-dysfunction-and-mitophagy
#4
Yansheng Feng, Ngonidzashe B Madungwe, Carolina Victoria da Cruz Junho, Jean C Bopassa
BACKGROUND AND PURPOSE: Recent evidence indicates that Gper1 (G Protein-coupled Estrogen Receptor 1) mediates acute pre-ischemic estrogen-induced protection of the myocardium from ischemia/reperfusion injury via a signaling cascade that includes PKC translocation, ERK1/2 /GSK-3β phosphorylation and the inhibition of the mitochondrial permeability transition pore (mPTP) opening. Here, we investigated the impact and mechanism involved in post-ischemic Gper1 activation in ischemia/reperfusion injury...
September 14, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28899790/alisporivir-rescues-defective-mitochondrial-respiration-in-duchenne-muscular-dystrophy
#5
Marco Schiavone, Alessandra Zulian, Sara Menazza, Valeria Petronilli, Francesco Argenton, Luciano Merlini, Patrizia Sabatelli, Paolo Bernardi
Duchenne muscular dystrophy (DMD) is a severe muscle disease of known etiology without effective, or generally applicable therapy. Mitochondria are affected by the disease in animal models but whether mitochondrial dysfunction is part of the pathogenesis in patients remains unclear. We show that primary cultures obtained from muscle biopsies of DMD patients display a decrease of the respiratory reserve, a consequence of inappropriate opening of the permeability transition pore (PTP). Treatment with the cyclophilin inhibitor alisporivir - a cyclosporin A derivative that desensitizes the PTP but does not inhibit calcineurin - largely restored the maximal respiratory capacity without affecting basal oxygen consumption in cells from patients, thus reinstating a normal respiratory reserve...
September 9, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28895006/bergenin-increases-osteogenic-differentiation-and-prevents-methylglyoxal-induced-cytotoxicity-in-mc3t3-e1-osteoblasts
#6
Kwang Sik Suh, Suk Chon, Eun Mi Choi
Bergenin, an active component of plants in the genus Bergenia, has multiple biological activities, including anti-inflammatory and immunomodulatory properties. We investigated the effects of bergenin on MC3T3-E1 osteoblasts. Bergenin treatment significantly elevated collagen synthesis, alkaline phosphatase activity, osteocalcin synthesis, and mineralization in the cells (p < 0.05). Additionally, bergenin increased the ratio of osteoprotegerin to receptor activator of nuclear factor kappa-B ligand, and cyclophilin B release...
September 11, 2017: Cytotechnology
https://www.readbyqxmd.com/read/28889121/structure-function-analysis-of-the-periplasmic-escherichia-coli-cyclophilin-ppia-in-relation-to-biofilm-formation
#7
Aggeliki Skagia, Eleni Vezyri, Konstantinos Grados, Anastasia Venieraki, Michael Karpusas, Panagiotis Katinakis, Maria Dimou
The presence of peptidyl-prolyl cis/trans isomerases (PPIases, EC: 5.2.1.8) in all domains of life indicates their biological importance. Cyclophilin PpiA, present in the periplasm of gram-negative bacteria, possesses PPIase activity but its physiological functions are still not clearly defined. Here, we demonstrate that the ΔppiA deletion strain from Escherichia coli exhibits an increased ability for biofilm formation and enhanced swimming motility compared to the wild-type strain. To identify structural features of PpiA which are necessary for the negative modulation of biofilm formation, we constructed a series of mutant PpiA proteins using a combination of error-prone and site-directed mutagenesis approaches...
September 9, 2017: Journal of Molecular Microbiology and Biotechnology
https://www.readbyqxmd.com/read/28881606/gsk1059615-kills-head-and-neck-squamous-cell-carcinoma-cells-possibly-via-activating-mitochondrial-programmed-necrosis-pathway
#8
Jing Xie, Quan Li, Xi Ding, Yunyun Gao
This study tested the anti-head and neck squamous cell carcinoma (HNSCC) cell activity by GSK1059615, a novel PI3K and mTOR dual inhibitor. GSK1059615 inhibited survival and proliferation of established (SCC-9, SQ20B and A253 lines) and primary human HNSCC cells. GSK1059615 blocked PI3K-AKT-mTOR activation in HNSCC cells. Intriguingly, GSK1059615 treatment in HNSCC cells failed to provoke apoptosis, but induced programmed necrosis. The latter was tested by mitochondria depolarization, ANT-1-cyclophilin-D mitochondrial association and lactate dehydrogenase (LDH) release...
August 1, 2017: Oncotarget
https://www.readbyqxmd.com/read/28875299/-1-h-13-c-and-15-n-resonance-assignments-and-secondary-structures-of-cyclophilin-2-from-trichomonas-vaginalis
#9
Tesmine Martin, Yuan-Chao Lou, Sarita Aryal, Jung-Hsiang Tai, Chinpan Chen
Cyclophilins are peptidyl prolyl isomerases that play an important role in a wide variety of biological functions like protein folding and trafficking, intracellular and extracellular signaling pathways, nuclear translocation and in pre-mRNA splicing. Two cyclophilins have been identified in the parasitic organism Trichomonas vaginalis and were named as TvCyP1 and TvCyP2. The 2 enzymes have been found to interact with Myb transcription factors in the parasite which regulate the iron induced expression of ap65-1 gene leading to cytoadherence of the parasite to human vaginal epithelial cells to cause the disease trichomoniasis...
September 5, 2017: Biomolecular NMR Assignments
https://www.readbyqxmd.com/read/28874678/mitochondrial-cyclophilin-d-ablation-is-associated-with-the-activation-of-akt-p70s6k-pathway-in-the-mouse-kidney
#10
Jelena Klawitter, Alexander Pennington, Jost Klawitter, Joshua M Thurman, Uwe Christians
The mitochondrial matrix protein cyclophilin D (CypD) is an essential component of the mitochondrial permeability transition pore (MPTP). Here we characterized the effects of CypD ablation on bioenergetics in the kidney. CypD loss triggers a metabolic shift in Ppif-/- male and female mouse kidneys towards glycolysis and Krebs cycle activity. The shift is accompanied by increased glucose consumption and a transcriptional upregulation of effectors of glucose metabolism in the kidney. These included activation of Akt, AMPK (only in males) and p70S6K kinases...
September 5, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28855265/the-role-of-baff-system-molecules-in-host-response-to-pathogens
#11
REVIEW
Jiro Sakai, Mustafa Akkoyunlu
The two ligands B cell-activating factor of the tumor necrosis factor family (BAFF) and a proliferation-inducing ligand (APRIL) and the three receptors BAFF receptor (BAFF-R), transmembrane activator and calcium-modulating cyclophilin ligand interactor (TACI), and B cell maturation antigen (BCMA) are members of the "BAFF system molecules." BAFF system molecules are primarily involved in B cell homeostasis. The relevance of BAFF system molecules in host responses to microbial assaults has been investigated in clinical studies and in mice deficient for each of these molecules...
October 2017: Clinical Microbiology Reviews
https://www.readbyqxmd.com/read/28855258/identification-and-characterization-of-vibrio-vulnificus-plpa-encoding-a-phospholipase-a2-essential-for-pathogenesis
#12
Kyung Ku Jang, Zee-Won Lee, Bityeoul Kim, Young Hyun Jung, Ho Jae Han, Myung Hee Kim, Byoung Sik Kim, Sang Ho Choi
The marine bacterium Vibrio vulnificus causes food-borne diseases, which may lead to life-threatening septicemia in some individuals. Therefore, identifying virulence factors in V. vulnificus is of high priority. We performed a transcriptome analysis on V. vulnificus after infection of human intestinal HT29-methotrexate cells, and found induction of plpA, encoding a putative phospholipase VvPlpA. Bioinformatics, biochemical, and genetic analyses demonstrated that VvPlpA is a phospholipase A2 (PLA2) secreted in the type II secretion system (T2SS)-dependent manner...
August 30, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28837151/mycobacterium-abscessus-glycopeptidolipids-inhibit-macrophage-apoptosis-and-bacterial-spreading-by-targeting-mitochondrial-cyclophilin-d
#13
Jake Whang, Yong Woo Back, Kang-In Lee, Nagatoshi Fujiwara, Seungwha Paik, Chul Hee Choi, Jeong-Kyu Park, Hwa-Jung Kim
Mycobacterium abscessus (MAB) is a species of nontuberculous mycobacteria (NTM) and a major causative pathogen of pulmonary diseases especially in patients with cystic fibrosis. MAB infection is notoriously difficult to treat because of its intrinsic or inducible resistance to most antibiotics. The rough (R) morphotype of MAB, lacking cell surface glycopeptidolipids (GPLs), is associated with more severe and persistent infection than the smooth (S) type; however, the mechanisms underlying the R type's virulence and the relation with GPLs remain unclear...
August 24, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28827840/dynamics-and-regulation-of-nuclear-import-and-nuclear-movements-of-hiv-1-complexes
#14
Ryan C Burdick, Krista A Delviks-Frankenberry, Jianbo Chen, Sanath K Janaka, Jaya Sastri, Wei-Shau Hu, Vinay K Pathak
The dynamics and regulation of HIV-1 nuclear import and its intranuclear movements after import have not been studied. To elucidate these essential HIV-1 post-entry events, we labeled viral complexes with two fluorescently tagged virion-incorporated proteins (APOBEC3F or integrase), and analyzed the HIV-1 dynamics of nuclear envelope (NE) docking, nuclear import, and intranuclear movements in living cells. We observed that HIV-1 complexes exhibit unusually long NE residence times (1.5±1.6 hrs) compared to most cellular cargos, which are imported into the nuclei within milliseconds...
August 2017: PLoS Pathogens
https://www.readbyqxmd.com/read/28818464/one-pot-synthesis-of-bioactive-cyclopentenones-from-%C3%AE-linolenic-acid-and-docosahexaenoic-acid
#15
Daniel Maynard, Sara Mareike Müller, Monika Hahmeier, Jana Löwe, Ivo Feussner, Harald Gröger, Andrea Viehhauser, Karl-Josef Dietz
Oxidation products of the poly-unsaturated fatty acids (PUFAs) arachidonic acid, α-linolenic acid and docosahexaenoic acid are bioactive in plants and animals as shown for the cyclopentenones prostaglandin 15d-PGJ2 and PGA2, cis-(+)-12-oxophytodienoic acid (12-OPDA), and 14-A-4 neuroprostane. In this study an inexpensive and simple enzymatic multi-step one-pot synthesis is presented for 12-OPDA, which is derived from α-linolenic acid, and the analogous docosahexaenoic acid (DHA)-derived cyclopentenone [(4Z,7Z,10Z)-12-[[-(1S,5S)-4-oxo-5-(2Z)-pent-2-en-1yl]-cyclopent-2-en-1yl] dodeca-4,7,10-trienoic acid, OCPD]...
August 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28807916/inhibition-of-calcineurin-or-impdh-exerts-moderate-to-potent-antiviral-activity-against-norovirus-replication
#16
Wen Dang, Yuebang Yin, Yijin Wang, Wenshi Wang, Junhong Su, Dave Sprengers, Luc J W van der Laan, Krzysztof Felczak, Krzysztof W Pankiewicz, Kyeong-Ok Chang, Marion P G Koopmans, Herold J Metselaar, Maikel P Peppelenbosch, Qiuwei Pan
Norovirus is a major cause of acute gastroenteritis worldwide and has emerged as an important issue of chronic infection in transplantation patients. Since no approved antiviral is available, we evaluated the effects of different immunosuppressants and ribavirin on norovirus and explored their mechanism-of-actions by using a human norovirus (HuNV) replicon-harboring model and a surrogate murine norovirus (MNV) infectious model. Roles of corresponding drug targets were investigated by gain- or loss-of-function approaches...
August 14, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28805482/cyclophilin-20-3-is-positioned-as-a-regulatory-hub-between-light-dependent-redox-and-12-oxo-phytodienoic-acid-signaling
#17
Hoon Cheong, Izailda Barbosa Dos Santos, Wenshan Liu, Heather N Gosse, Sang-Wook Park
The jasmonate family of phytohormones plays central roles in plant development and stress acclimation. However, the regulatory modes of their signaling circuitry remain largely unknown. Here we describe that cyclophilin 20-3 (CYP20-3), a binding protein of (+)-12-oxo-phytodienoic acid (OPDA), crisscrosses stress responses with light-dependent redox reactions, which fine-tunes the activity of key enzymes in the plastid photosynthetic carbon assimilation and sulfur assimilation pathways. Under stressed states, OPDA - accumulated in the chloroplasts - binds and promotes CYP20-3 to transfer electron (e(-)) from thioredoxins (i...
August 14, 2017: Plant Signaling & Behavior
https://www.readbyqxmd.com/read/28803887/a-miniaturized-peptidyl-prolyl-isomerase-enzyme-assay
#18
Mirella Vivoli, Julien Renou, Arnaud Chevalier, Isobel H Norville, Suraya Diaz, Christina Juli, Helen Atkins, Ulrike Holzgrabe, Pierre-Yves Renard, Mitali Sarkar-Tyson, Nicholas J Harmer
Prolyl-peptidyl isomerases (PPIases) are enzymes that are found in all living organisms. They form an essential part of the cellular protein folding homeostasis machinery. PPIases are associated with many important human diseases, e.g. cardiovascular disease, cancer and Alzheimer's. The development of novel PPIase inhibitors has been limited by the lack of a rapid, laboratory-based assay for these enzymes, as their substrates and products are challenging to distinguish. A well described continuous assay, coupled with the hydrolysis of a peptide by chymotrypsin is highly effective, but comparatively slow...
August 11, 2017: Analytical Biochemistry
https://www.readbyqxmd.com/read/28791545/microbial-cyclophilins-specialized-functions-in-virulence-and-beyond
#19
REVIEW
Maria Dimou, Anastasia Venieraki, Panagiotis Katinakis
Cyclophilins belong to the superfamily of peptidyl-prolyl cis/trans isomerases (PPIases, EC: 5.2.1.8), the enzymes that catalyze the cis/trans isomerization of peptidyl-prolyl peptide bonds in unfolded and partially folded polypeptide chains and native state proteins. Cyclophilins have been extensively studied, since they are involved in multiple cellular processes related to human pathologies, such as neurodegenerative disorders, infectious diseases, and cancer. However, the presence of cyclophilins in all domains of life indicates a broader biological importance...
August 8, 2017: World Journal of Microbiology & Biotechnology
https://www.readbyqxmd.com/read/28790108/cyclophilin-a-maintains-glioma-initiating-cell-stemness-by-regulating-wnt-%C3%AE-catenin-signaling
#20
Guangzhi Wang, Jia Shen, Jiahang Sun, Zhenfeng Jiang, Jiabing Fan, Hongjun Wang, Shan Yu, Yu Long, Yi Liu, HOngbo Bao, Kelvin X Zhang, Ke Han, Min-Wei Zhu, Yongri Zheng, Zhiguo Lin, Chuanlu Jiang, Mian Guo
PURPOSE: Glioma-initiating cells (GICs) are glioma stem-like cells that contribute to glioblastoma (GBM) development, recurrence, and resistance to chemotherapy and radiotherapy. They have recently become the focus of novel treatment strategies. Cyclophilin A (CypA) is a cytosolic protein that belongs to the peptidyl-prolyl isomerase (PPIase) family and the major intracellular target of the immunosuppressive drug cyclosporin A (CsA). In this study, we investigate the functions of CypA and its mechanism of action in GICs' development...
August 8, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
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