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https://www.readbyqxmd.com/read/30307091/new-irreversible-%C3%AE-l-iduronidase-inhibitors-and-activity-based-probes
#1
Marta Artola, Chi-Lin Kuo, Stephen A McMahon, Verena Oehler, Thomas Hansen, Martijn van der Lienden, Xu He, Hans van den Elst, Bogdan I Florea, Allison R Kermode, Tracey M Gloster, Gijsbert A van der Marel, Jeroen D C Codée, Hermen S Overkleeft, Johannes M F G Aerts
Cyclophellitol aziridines are potent irreversible inhibitors of retaining glycosidases and versatile intermediates in the synthesis of activity-based glycosidase probes (ABPs). Direct 3-amino-2-(trifluoromethyl)quinazolin-4(3H)-one-mediated aziridination on L-ido-configured cyclohexene has enabled the synthesis of new covalent inhibitors and ABPs of α-L-iduronidase, deficiency of which underlies the lysosomal storage disorder mucopolysaccharidosis type I (MPS I). The iduronidase ABPs react covalently and irreversibly in an activity-based manner with human recombinant α-L-iduronidase (rIDUA, Aldurazyme®)...
October 11, 2018: Chemistry: a European Journal
https://www.readbyqxmd.com/read/30261049/mechanisms-underlying-immune-tolerance-caused-by-recombinant-echinococcus-granulosus-antigens-eg-mmdh-and-eg10-in-dendritic-cells
#2
Yana Wang, Shiyu Lv, Qiang Wang, Chan Wang, Mingxing Zhu, Zhanbing Ma, Wei Zhao
Mice immunized with recombinant Echinococcus granulosus antigens Eg10 and Eg mMDH do not show elevated resistance to E. granulosus infection but show aggravated infection instead. To gain a deeper insight in the immune tolerance mechanisms in mice immunized with Eg10 and Eg mMDH, this study simulated the immune tolerance process in vitro by culturing bone marrow-derived dendritic cells (BMDCs) in the presence of Eg10 or Eg mMDH. Scanning electron microscopy revealed that Eg10- and Eg mMDH-treated DCs exhibited immature cell morphology, while addition of LPS to the cells induced changes in cell morphology and an increase in the number of cell-surface protrusions...
2018: PloS One
https://www.readbyqxmd.com/read/30254983/indoximod-an-immunometabolic-adjuvant-that-empowers-t-cell-activity-in-cancer
#3
REVIEW
Eric Fox, Thomas Oliver, Melissa Rowe, Sunil Thomas, Yousef Zakharia, Paul B Gilman, Alexander J Muller, George C Prendergast
Exploding interest in immunometabolism as a source of new cancer therapeutics has been driven in large part by studies of tryptophan catabolism mediated by IDO/TDO enzymes. A chief focus in the field is IDO1, a pro-inflammatory modifier that is widely overexpressed in cancers where it blunts immunosurveillance and enables neovascularization and metastasis. The simple racemic compound 1-methyl-D,L-tryptophan (1MT) is an extensively used probe of IDO/TDO pathways that exerts a variety of complex inhibitory effects...
2018: Frontiers in Oncology
https://www.readbyqxmd.com/read/30243842/palmatine-ameliorated-murine-colitis-by-suppressing-tryptophan-metabolism-and-regulating-gut-microbiota
#4
Xiao-Jun Zhang, Zhong-Wen Yuan, Chang Qu, Xiu-Ting Yu, Tao Huang, Ping Vicky Chen, Zi-Ren Su, Yao-Xing Dou, Jia-Zhen Wu, Hui-Fang Zeng, Ying Xie, Jian-Nan Chen
Inflammatory bowel disease (IBD), majorly include Crohn's disease (CD) and ulcerative colitis (UC), is chronic and relapsing inflammatory disorders of the gastrointestinal tract, which treatment options remain limited. Here we examined the therapeutic effects of an isoquinoline alkaloid, Palmatine (Pal), on mice experimental colitis induced by dextran sulfate sodium (DSS) and explored underlying mechanisms. Colitis was induced in BALB/c mice by administering 3% DSS in drinking water for 7 days. Pal (50 and 100 mg kg-1 ) and the positive drug Sulfasalazine (SASP, 200 mg kg-1 ) were orally administered for 7 days...
September 19, 2018: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/30231371/emerging-strategies-in-systemic-therapy-for-the-treatment-of-melanoma
#5
Paolo A Ascierto, Keith Flaherty, Stephanie Goff
Recent years have seen major improvements in survival of patients with advanced melanoma with the advent of various novel systemic immunotherapies and targeted therapies. As our understanding of these agents and their various mechanisms of action improves, even more impressive outcomes are being achieved through use of various combination strategies, including the combining of different immunotherapies with one another as well as with other modalities. However, despite the improved outcomes that have been achieved in advanced melanoma, responses to treatment are heterogeneous and may not always be durable...
May 23, 2018: American Society of Clinical Oncology Educational Book
https://www.readbyqxmd.com/read/30231333/combination-immunotherapy-development-in-melanoma
#6
Alexander M M Eggermont, Marka Crittenden, Jennifer Wargo
Melanoma has been the most important cancer to drive immunotherapy development of solid tumors. Since 2010, immunotherapy has been revolutionized by the concept of breaking tolerance. It represents a major paradigm shift and marks the beginning of a new era. The impact of the first immune checkpoint inhibitors, anti-CTLA-4 and anti-PD-1/anti-PD-L1, is unprecedented. In 7 years, it transformed advanced-stage melanoma into a curable disease in over 50% of patients. Another major step has been the development of the combination of BRAF inhibitors plus MEK inhibitors in the treatment of BRAF-mutant melanomas...
May 23, 2018: American Society of Clinical Oncology Educational Book
https://www.readbyqxmd.com/read/30227416/hepatocyte-growth-factor-facilitates-esophageal-mucosal-repair-and-inhibits-the-submucosal-fibrosis-in-a-rat-model-of-esophageal-ulcer
#7
Yuga Komaki, Shuji Kanmura, Fumisato Sasaki, Hidehito Maeda, Kohei Oda, Shiho Arima, Shiroh Tanoue, Yuichiro Nasu, Shinichi Hashimoto, Seiichi Mawatari, Hirohito Tsubouchi, Akio Ido
BACKGROUND/AIMS: Esophageal mucosal damage often causes scar tissue, leading to refractory stricture. The aim of this study was to clarify the effect of hepatocyte growth factor (HGF) on esophageal mucosal repair and fibrosis leading to stricture in a rat model of esophageal ulcer. METHODS: Esophageal ulcers were induced in rats by topical exposure of the lower esophageal serosa to acetic acid, followed by intraperitoneal administration of HGF (200 µg/day) using an osmotic pump for 7 days...
September 18, 2018: Digestion
https://www.readbyqxmd.com/read/30198719/saturn-shaped-ice-burst-pattern-and-fast-basal-binding-of-an-ice-binding-protein-from-an-antarctic-bacterial-consortium
#8
Aleksei Kaleda, Lotem Haleva, Guy Sarusi, Tova Pinsky, Marco Mangiagalli, Maya Bar Dolev, Marina Lotti, Marco Nardini, Ido Braslavsky
Ice-binding proteins (IBPs) bind to ice crystals and control their growth, enabling host organisms to adapt to subzero temperatures. By binding to ice, IBPs can affect the shape and recrystallization of ice crystals. The shapes of ice crystals produced by IBPs vary and are partially due to which ice planes the IBPs are bound to. Previously, we have described a bacterial IBP found in the metagenome of the symbionts of Euplotes focardii ( EfcIBP). EfcIBP shows remarkable ice recrystallization inhibition activity...
September 26, 2018: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/30186285/the-combined-use-of-melatonin-and-an-indoleamine-2-3-dioxygenase-1-inhibitor-enhances-vaccine-induced-protective-cellular-immunity-to-hpv16-associated-tumors
#9
Ana C R Moreno, Bruna F M M Porchia, Roberta L Pagni, Patrícia da Cruz Souza, Rafael Pegoraro, Karine B Rodrigues, Tácita B Barros, Luana R de Melo Moraes Aps, Eliseu F de Araújo, Vera L G Calich, Luís C de Souza Ferreira
Immunotherapy has become an important ally in the fight against distinct types of cancer. However, the metabolic plasticity of the tumor environment frequently influences the efficacy of therapeutic procedures, including those based on immunological tools. In this scenario, immunometabolic adjuvants arise as an alternative toward the development of more efficient cancer therapies. Here we demonstrated that the combination of melatonin, a neuroimmunomodulator molecule, and an indoleamine 2,3-dioxygenase (IDO) inhibitor (1-methyl-DL-tryptophan, DL-1MT) improves the efficacy of an immunotherapy (gDE7) targeting human papillomavirus (HPV)-associated tumors...
2018: Frontiers in Immunology
https://www.readbyqxmd.com/read/30170210/design-synthesis-and-biological-evaluation-of-a-novel-library-of-antimitotic-c-2-aroyl-arylimino-tryptamine-derivatives-that-are-also-potent-inhibitors-of-indoleamine-2-3-dioxygenase-ido
#10
Jyoti Chauhan, Moumita Dasgupta, Tania Luthra, Akanksha Awasthi, Sayantan Tripathy, Anindyajit Banerjee, Santanu Paul, Debasish Nag, Saikat Chakrabarti, Gopal Chakrabarti, Subhabrata Sen
A novel library of C2 -substituted tryptamines (based on diverse C2 -aroyl/arylimino indoles and indole-diketopiperazine hybrids) possessing antimitotic properties were designed, synthesized and screened for their inhibitory activity against tubulin polymerization, and against proliferation of A549 lung cancer, HeLa cervical cancer, MCF7 breast cancer and HePG2 liver cancer cell lines. The design of molecules were inspired from known antimitotic compounds and natural products. The molecular docking of the designed compounds indicated that they bind to the colchicin binding site of tubulin...
November 1, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/30159037/indoleamine-2-3-dioxygenase-dependent-expansion-of-t-regulatory-cells-maintains-mucosal-healing-in-ulcerative-colitis
#11
Aleksandar Acovic, Bojana Simovic Markovic, Marina Gazdic, Aleksandar Arsenijevic, Nemanja Jovicic, Nevena Gajovic, Marina Jovanovic, Natasa Zdravkovic, Tatjana Kanjevac, C Randall Harrell, Crissy Fellabaum, Zana Dolicanin, Valentin Djonov, Nebojsa Arsenijevic, Miodrag L Lukic, Vladislav Volarevic
Background: Dendritic cell (DC)-derived indolamine 2,3-dioxygenase (IDO) degrades tryptophan to kynurenine, which promotes conversion of inflammatory T cells in immunosuppressive regulatory T cells (Tregs). We analyzed the significance of the IDO:Treg axis for inducing and maintaining mucosal healing in ulcerative colitis (UC). Methods: Dextran sodium sulphate (DSS)-induced colitis in BALB/c mice (model for mucosal healing) and C57BL/6 mice (model for persistent disease) was used...
2018: Therapeutic Advances in Gastroenterology
https://www.readbyqxmd.com/read/30108982/discovery-of-indoleamine-2-3-dioxygenase-inhibitors-using-machine-learning-based-virtual-screening
#12
Hongao Zhang, Wei Liu, Zhihong Liu, Yingchen Ju, Mengyang Xu, Yue Zhang, Xinyu Wu, Qiong Gu, Zhong Wang, Jun Xu
Indoleamine 2,3-dioxygenase (IDO), an immune checkpoint, is a promising target for cancer immunotherapy. However, current IDO inhibitors are not approved for clinical use yet; therefore, new IDO inhibitors are still demanded. To identify new IDO inhibitors, we have built naive Bayesian (NB) and recursive partitioning (RP) models from a library of known IDO inhibitors derived from recent publications. Thirteen molecular fingerprints were used as descriptors for the models to predict IDO inhibitors. An in-house compound library was virtually screened using the best machine learning model, which resulted in 50 hits for further enzyme-based IDO inhibitory assays...
June 1, 2018: MedChemComm
https://www.readbyqxmd.com/read/30087159/indoleamine-2-3-dioxygenase-suppresses-the-cytotoxicity-of-1-nk-cells-in-response-to-ectopic-endometrial-stromal-cells-in-endometriosis
#13
Xuan-Tong Liu, Hui-Ting Sun, Zhong-Fang Zhang, Ru-Xia Shi, Li-Bing Liu, Jia-Jun Yu, Wen-Jie Zhou, Chun-Jie Gu, Shao-Liang Yang, Yu-Kai Liu, Hui-Li Yang, Feng-Xuan Xu, Ming-Qing Li
It has been reported that the impaired cytotoxicity of natural killer (NK) cells and abnormal cytokines that are changed by the interaction between ectopic endometrial cells and immune cells is indispensable for the initiation and development of endometriosis (EMS). However, the mechanism of NK cells dysfunction in EMS remains largely unclear. Here, we found that NK cells in peritoneal fluid from women with EMS highly expressed indoleamine 2,3-dioxygenase (IDO). Furthermore, IDO+NK cells possessed lower NKp46 and NKG2D but higher IL-10 than that of IDO-NK...
August 7, 2018: Reproduction: the Official Journal of the Society for the Study of Fertility
https://www.readbyqxmd.com/read/30081936/can-ido-activity-predict-primary-resistance-to-anti-pd-1-treatment-in-nsclc
#14
Andrea Botticelli, Bruna Cerbelli, Luana Lionetto, Ilaria Zizzari, Massimiliano Salati, Annalinda Pisano, Mazzuca Federica, Maurizio Simmaco, Marianna Nuti, Paolo Marchetti
BACKGROUND: Immune checkpoint inhibitors have revolutionized the treatment paradigm of highly lethal malignancies like advanced non-small cell lung cancer (NSCLC), demonstrating long-term tumour control and extended patient survival. Unfortunately, only 25-30% of patients experience a durable benefit, while the vast majority demonstrate primary or acquired resistance. Recently, indoleamine 2,3-dioxygenase (IDO) activity has been proposed as a possible mechanism of resistance to anti-PD-1 treatment leading to an immunosuppressive microenvironment...
August 6, 2018: Journal of Translational Medicine
https://www.readbyqxmd.com/read/30055888/cyclic-analogue-of-s-benzylisothiourea-that-suppresses-kynurenine-production-without-inhibiting-indoleamine-2-3-dioxygenase-activity
#15
Miwa Fukuda, Tomomi Sasaki, Tomoko Hashimoto, Hiroyuki Miyachi, Minoru Waki, Akira Asai, Osamu Takikawa, Osamu Ohno, Kenji Matsuno
Kynurenine is biosynthesised from tryptophan catalysed by indoleamine 2,3-dioxygenase (IDO). The abrogation of kynurenine production is considered a promising therapeutic target for immunological cancer treatment. In the course of our IDO inhibitor programme, formal cyclisation of the isothiourea moiety of the IDO inhibitor 1 afforded the 5-Cl-benzimidazole derivative 2b-6, which inhibited both recombinant human IDO (rhIDO) activity and cellular kynurenine production. Further derivatisation of 2b-6 provided the potent inhibitor of cellular kynurenine production 2i (IC50  = 0...
July 20, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/30036146/unusually-long-term-responses-to-vemurafenib-in-braf-v600e-mutated-colon-and-thyroid-cancers-followed-by-the-development-of-rare-ras-activating-mutations
#16
Tali Ofir Dovrat, Ethan Sokol, Garrett Frampton, Eliya Shachar, Sharon Pelles, Ravit Geva, Ido Wolf
INTRODUCTION: V600E BRAF mutation is an established driver mutation in a variety of tumors. Vemurafenib is a selective inhibitor of the BRAF V600E kinase, known to be highly effective in BRAF V600E-positive metastatic melanoma. As a single agent, vemurafenib is relatively ineffective in other V600E-positive malignancies. Case 1: A 72 year old man with metastatic CRC who failed several previous lines of chemotherapy. Genetic analysis of 315 cancer-related genes (Foundation Medicine, FMI) revealed a BRAF V600E mutation...
July 23, 2018: Cancer Biology & Therapy
https://www.readbyqxmd.com/read/30007645/discovery-of-a-polysaccharide-from-the-fruiting-bodies-of-lepista-sordida-as-potent-inhibitors-of-indoleamine-2-3-dioxygenase-ido-in-hepg2-cells-via-blocking-of-stat1-mediated-jak-pkc-%C3%AE-signaling-pathways
#17
Qiang Luo, Liang Yan, Pan Xu, Chuan Xiong, Zhirong Yang, Peng Hu, Huidong Hu, Ren Hong
The present study examined the role of a polysaccharide (LSP, 25 and 100 μg/ml) from the fruiting bodies of Lepista sordid on the immunosuppressive enzyme indoleamine 2, 3-dioxygenase (IDO) in HepG2 cells, and the possible mechanism of action. IDO expression and kynurenine production from LSP-treated HepG2 cells following IFN-γ stimulation were dramatically inhibited by LSP treatment. In line with this, the medium of HepG2 cells pretreated with LSP improved the survival rate of primary CD4+ and CD8+ T cells as compared with IFN-γ-treated control cells...
October 1, 2018: Carbohydrate Polymers
https://www.readbyqxmd.com/read/29967604/hsa-mir-99b-let-7e-mir-125a-cluster-regulates-pathogen-recognition-receptor-stimulated-suppressive-antigen-presenting-cells
#18
Dagmar Hildebrand, Mariel-Esther Eberle, Sabine Marie Wölfle, Franziska Egler, Delal Sahin, Aline Sähr, Konrad A Bode, Klaus Heeg
Antigen-presenting cells (APCs) regulate the balance of our immune response toward microbes. Whereas immunogenic APCs boost inflammation and activate lymphocytes, the highly plastic cells can switch into a tolerogenic/suppressive phenotype that dampens and resolves the response. Thereby the initially mediated inflammation seems to prime the switch of APCs while the strength of activation determines the grade of the suppressive phenotype. Recently, we showed that pathogen recognition receptor-mediated pro-inflammatory cytokines reprogram differentiating human blood monocytes in vitro toward an immunosuppressive phenotype through prolonged activation of signal transducer and activator of transcription (STAT) 3...
2018: Frontiers in Immunology
https://www.readbyqxmd.com/read/29959458/indoleamine-2-3-dioxygenase-provides-adaptive-resistance-to-immune-checkpoint-inhibitors-in-hepatocellular-carcinoma
#19
Zachary J Brown, Su Jong Yu, Bernd Heinrich, Chi Ma, Qiong Fu, Milan Sandhu, David Agdashian, Qianfei Zhang, Firouzeh Korangy, Tim F Greten
Hepatocellular carcinoma (HCC) is the second leading cause of cancer-related death worldwide. Immune checkpoint blockade with anti-CTLA-4 and anti-PD-1 antibodies has shown promising results in the treatment of patients with advanced HCC. The anti-PD-1 antibody, nivolumab, is now approved for patients who have had progressive disease on the current standard of care. However, a subset of patients with advanced HCC treated with immune checkpoint inhibitors failed to respond to therapy. Here, we provide evidence of adaptive resistance to immune checkpoint inhibitors through upregulation of indoleamine 2,3-dioxygenase (IDO) in HCC...
August 2018: Cancer Immunology, Immunotherapy: CII
https://www.readbyqxmd.com/read/29901571/indoleamine-2-3-dioxygenase-in-non-small-cell-lung-cancer-a-targetable-mechanism-of-immune-resistance-frequently-coexpressed-with-pd-l1
#20
Ashley Volaric, Ryan Gentzler, Richard Hall, James H Mehaffey, Edward B Stelow, Timothy N Bullock, Linda W Martin, Anne M Mills
The immune regulatory enzyme indoleamine-2,3-dioxygenase (IDO-1) suppresses T cell responses and may reduce efficacy of therapies targeting immune checkpoints such as programmed death receptor-1/programmed death ligand-1 (PD-1/PD-L1). Early phase clinical trials combining IDO-1 and PD-1/PD-L1 inhibitors have shown some promise in non-small cell lung cancers (NSCLCs). However, the coexpression of IDO-1 and PD-L1 has not been thoroughly investigated, and the potential for IDO-1 immunohistochemical expression as a therapeutic biomarker is unknown...
September 2018: American Journal of Surgical Pathology
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