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The G Protein-Coupled Receptor Subset of the Dog Genome Is More Similar
BMC Genomics BioMed Central Research article Open Access The G protein-coupled receptor subset of the dog genome is more similar to that in humans than rodents Tatjana Haitina1, Robert Fredriksson1, Steven M Foord2, Helgi B Schiöth*1 and David E Gloriam*2 Address: 1Department of Neuroscience, Functional Pharmacology, Uppsala University, BMC, Box 593, 751 24, Uppsala, Sweden and 2GlaxoSmithKline Pharmaceuticals, New Frontiers Science Park, 3rd Avenue, Harlow CM19 5AW, UK Email: Tatjana Haitina - [email protected]; Robert Fredriksson - [email protected]; Steven M Foord - [email protected]; Helgi B Schiöth* - [email protected]; David E Gloriam* - [email protected] * Corresponding authors Published: 15 January 2009 Received: 20 August 2008 Accepted: 15 January 2009 BMC Genomics 2009, 10:24 doi:10.1186/1471-2164-10-24 This article is available from: http://www.biomedcentral.com/1471-2164/10/24 © 2009 Haitina et al; licensee BioMed Central Ltd. This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. Abstract Background: The dog is an important model organism and it is considered to be closer to humans than rodents regarding metabolism and responses to drugs. The close relationship between humans and dogs over many centuries has lead to the diversity of the canine species, important genetic discoveries and an appreciation of the effects of old age in another species. The superfamily of G protein-coupled receptors (GPCRs) is one of the largest gene families in most mammals and the most exploited in terms of drug discovery. -
Erteberel (LY500307) Product Data Sheet
Product Name: Erteberel (LY500307) Revision Date: 01/10/2021 Product Data Sheet Erteberel (LY500307) Cat. No.: B1518 CAS No.: 533884-09-2 Formula: C18H18O3 M.Wt: 282.33 Synonyms: Target: Endocrinology and Hormones Pathway: Estrogen/progestogen Receptor Storage: Store at -20°C Solvent & Solubility insoluble in H2O; ≥14.1 mg/mL in DMSO; ≥48.3 mg/mL in EtOH Mass Solvent 1mg 5mg 10mg Preparing Concentration In Vitro Stock Solutions 1 mM 3.5420 mL 17.7098 mL 35.4195 mL 5 mM 0.7084 mL 3.5420 mL 7.0839 mL 10 mM 0.3542 mL 1.7710 mL 3.5420 mL Please refer to the solubility information to select the appropriate solvent. Biological Activity Shortsummary ERβ agonist, potent and selective IC₅₀ & Target Cell Viability Assay Cell Line: Human prostate cancer cell line (PC-3 cells) Preparation method: The solubility of this compound in DMSO is >10 mM. General tips for obtaining In Vitro a higher concentration: Please warm the tube at 37°C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months. Reacting conditions: N/A 1 | www.apexbt.com Applications: Erteberel showed potent and selective binding affinity for ERβ with EC50 value of 0.66 nM [1]. Animal experiment Animal models: Male and female rat fertility and rat and rabbit embryo-fetal development model Dosage form: 0.03 to 10 mg/kg/day for rats, or 1 to 25 mg/kg/day for rabbits, oral gavage, for 2 or 10 weeks Applications: There were no-observed adverse effect levels following LY500307 In Vivo administration of 1 mg/kg/day for male rat fertility, 0.3 mg/kg/day for female rat fertility and embryo-fetal development, and 25 mg/kg/day for rabbit embryo-fetal development [2]. -
The Drug Sensitivity and Resistance Testing (DSRT) Approach
A phenotypic screening and machine learning platform eciently identifies triple negative breast cancer-selective and readily druggable targets Prson Gautam 1 Alok Jaiswal 1 Tero Aittokallio 1, 2 Hassan Al Ali 3 Krister Wennerberg 1,4 Identifying eective oncogenic targets is challenged by the complexity of genetic alterations in 1Institute for Molecular Medicine Finland (FIMM), HiLIFE, University of Helsinki, Finland cancer and their poorly understood relation to cell function and survival. There is a need for meth- Current kinome coverage of kinase inhibitors in TNBC exhibit diverse kinase dependencies MFM-223 is selectively addicted to FGFR2 2Department of Mathematics and Statistics, University of Turku, Finland 3The Miami Project to Cure Paralysis, Peggy and Harold Katz Family Drug Discovery Center, A A Sylvester Comprehensive Cancer Center, and Department of Neurological Surgery and Medicine ods that rapidly and accurately identify “pharmacologically eective” targets without the require- clinical evaluation TN Kinases MFM-223 CAL-120 MDA-MB-231 TNBC TNBC TNBC TNBC TNBC TNBC HER2+ 100 University of Miami Miller School of Medicine, Miami, FL 33136, USA. non- HER2+ FGFR1 0.97 0.00 0.00 MFM-223 BL1 BL2 M MSL IM LAR ER+, PR+ 50 ment for priori knowledge of complex signaling networks. We developed an approach that uses ma- cancerous FGFR2 56.46 0.00 0.00 CAL-120 25 4 MDA-MB-231 Biotech Research & Innovation Centre (BRIC) and Novo Nordisk Foundation Center HCC1937 CAL-85-1 CAL-120 MDA-MB-231 DU4475 CAL-148 MCF-10A SK-BR-3 BT-474 FGFR3 25.10 0.00 0.00 0 chine learning to relate results from unbiased phenotypic screening of kinase inhibitors to their bio- for Stem Cell Biology (DanStem), University of Copenhagen, Denmark HCC1599 HDQ-P1 BT-549 MDA-MB-436 MFM-223 FGFR4 0.00 0.00 0.00 MAXIS*Bk Clinical status MDA-MB-468 CAL-51 Hs578T MDA-MB-453 score chemical activity data. -
Genetic Basis of Idiopathic Scoliosis
Research & Review: Management of Cardiovascular and Orthopedic Complications Volume 1 Issue 1 Genetic Basis of Idiopathic Scoliosis S. Sreeremya Assistant Professor, Department of Biotechnology, Sree Narayana Guru College, Coimbatore, Tamil Nadu, India Email: [email protected] Abstract Idiopathic scoliosis (IS), the most usual spinal deformity, affects otherwise healthy children and adolescents during growth. The etiology is still not quiet understood, although genetic factors are believed to be important. This review corroborates the understanding of IS as a complex disease with a polygenic background. Presumably IS can be typically due to a spectrum of genetic risk variants, ranging from very rare or even private to very common. The most promising candidate genes are highlighted. Keywords: Idiopathic scoliosis, Genetics, Pathogenesis, Heredity INTRODUCTION marked by phenotypic complexity Idiopathic scoliosis (IS), the most general (variations in curve morphology and form of spinal deformity, affects otherwise magnitude, age of onset, rate of healthy children and adolescents during progression), and a prognosis mainly growth (Fig: 1). It usually presents as a rib ranging from increase in curve magnitude, hump visible at forward bending, together to stabilization, or to resolution with with unlevelled shoulders and an growth [5]. Genetic factors are known to asymmetrical waist [1]. According to play a pivotal role, as observed in twin Cobb, the diagnosis is specifically studies and their observation and singleton confirmed by a standing spinal radiograph multigenerational families [6]. A recent showing a lateral curvature of the spine research of monozygotic and dizygotic exceeding 10° [2]. A main concern in IS is twins from the Swedish twin registry the absence of reliable means by which to estimated that overall genetic effects predict risk of progression, leading to accounted for 39 % of the observed frequent follow-ups, radiographs, and phenotypic variance, leaving the remaining potentially unnecessary brace treatments. -
Supplementary Information
Supplementary Information Network-based Drug Repurposing for Novel Coronavirus 2019-nCoV Yadi Zhou1,#, Yuan Hou1,#, Jiayu Shen1, Yin Huang1, William Martin1, Feixiong Cheng1-3,* 1Genomic Medicine Institute, Lerner Research Institute, Cleveland Clinic, Cleveland, OH 44195, USA 2Department of Molecular Medicine, Cleveland Clinic Lerner College of Medicine, Case Western Reserve University, Cleveland, OH 44195, USA 3Case Comprehensive Cancer Center, Case Western Reserve University School of Medicine, Cleveland, OH 44106, USA #Equal contribution *Correspondence to: Feixiong Cheng, PhD Lerner Research Institute Cleveland Clinic Tel: +1-216-444-7654; Fax: +1-216-636-0009 Email: [email protected] Supplementary Table S1. Genome information of 15 coronaviruses used for phylogenetic analyses. Supplementary Table S2. Protein sequence identities across 5 protein regions in 15 coronaviruses. Supplementary Table S3. HCoV-associated host proteins with references. Supplementary Table S4. Repurposable drugs predicted by network-based approaches. Supplementary Table S5. Network proximity results for 2,938 drugs against pan-human coronavirus (CoV) and individual CoVs. Supplementary Table S6. Network-predicted drug combinations for all the drug pairs from the top 16 high-confidence repurposable drugs. 1 Supplementary Table S1. Genome information of 15 coronaviruses used for phylogenetic analyses. GenBank ID Coronavirus Identity % Host Location discovered MN908947 2019-nCoV[Wuhan-Hu-1] 100 Human China MN938384 2019-nCoV[HKU-SZ-002a] 99.99 Human China MN975262 -
New Contributions in Undergraduate Research
PSU McNair Scholars Online Journal Volume 11 Issue 1 Without Borders: Original Contributions Article 6 in Undergraduate Research 2017 Wings Outstretched: New Contributions in Undergraduate Research Follow this and additional works at: https://pdxscholar.library.pdx.edu/mcnair Let us know how access to this document benefits ou.y Recommended Citation (2017) "Wings Outstretched: New Contributions in Undergraduate Research," PSU McNair Scholars Online Journal: Vol. 11: Iss. 1, Article 6. https://doi.org/10.15760/mcnair.2017.01 This open access Full Issue is distributed under the terms of the Creative Commons Attribution-NonCommercial- ShareAlike 4.0 International License (CC BY-NC-SA 4.0). All documents in PDXScholar should meet accessibility standards. If we can make this document more accessible to you, contact our team. Portland State University McNair Research Journal 2017 Without Borders: Original Contributions in Undergraduate Research 2017 Ronald E. McNair Scholars Journal Portland State University 1 About the Program The Portland State University (PSU) Ronald E. McNair Scholars Program at Portland State University works with motivated and talented undergraduates who want to pursue PhDs. It introduces juniors and seniors who are first-generation and low income, and/or members of under-represented groups to academic research and to effective strategies for getting into and graduating from PhD programs. The McNair Scholars Program has academic-year activities and a full-time summer research internship. Scholars take academic and skills-building seminars and workshops during the year, and each scholar works closely with a faculty mentor on original research in the summer. Scholars present their research findings at the McNair Summer Symposium and at other conferences, and are encouraged to publish their papers in the McNair Journal and other scholarly publications. -
The Concise Guide to Pharmacology 2019/20
Edinburgh Research Explorer THE CONCISE GUIDE TO PHARMACOLOGY 2019/20 Citation for published version: Cgtp Collaborators 2019, 'THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Transporters', British Journal of Pharmacology, vol. 176 Suppl 1, pp. S397-S493. https://doi.org/10.1111/bph.14753 Digital Object Identifier (DOI): 10.1111/bph.14753 Link: Link to publication record in Edinburgh Research Explorer Document Version: Publisher's PDF, also known as Version of record Published In: British Journal of Pharmacology General rights Copyright for the publications made accessible via the Edinburgh Research Explorer is retained by the author(s) and / or other copyright owners and it is a condition of accessing these publications that users recognise and abide by the legal requirements associated with these rights. Take down policy The University of Edinburgh has made every reasonable effort to ensure that Edinburgh Research Explorer content complies with UK legislation. If you believe that the public display of this file breaches copyright please contact [email protected] providing details, and we will remove access to the work immediately and investigate your claim. Download date: 28. Sep. 2021 S.P.H. Alexander et al. The Concise Guide to PHARMACOLOGY 2019/20: Transporters. British Journal of Pharmacology (2019) 176, S397–S493 THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Transporters Stephen PH Alexander1 , Eamonn Kelly2, Alistair Mathie3 ,JohnAPeters4 , Emma L Veale3 , Jane F Armstrong5 , Elena Faccenda5 ,SimonDHarding5 ,AdamJPawson5 , Joanna L -
Galeterone for the Treatment of Castration- Resistant Prostate Cancer Bruce Montgomery1, Mario A
Published OnlineFirst November 2, 2015; DOI: 10.1158/1078-0432.CCR-15-1432 Cancer Therapy: Clinical Clinical Cancer Research Androgen Receptor Modulation Optimized for Response (ARMOR) Phase I and II Studies: Galeterone for the Treatment of Castration- Resistant Prostate Cancer Bruce Montgomery1, Mario A. Eisenberger2, Matthew B. Rettig3, Franklin Chu4, Roberto Pili5, Joseph J. Stephenson6, Nicholas J. Vogelzang7, Alan J. Koletsky8, Luke T. Nordquist9, William J. Edenfield10, Khalid Mamlouk11, Karen J. Ferrante11, and Mary-Ellen Taplin12 Abstract Purpose: Galeterone is a selective, multitargeted agent that Results: In ARMOR1, across all doses, 49.0% (24/49) achieved a inhibits CYP17, antagonizes the androgen receptor (AR), and 30% decline in prostate-specific antigen (PSA; PSA30) and reduces AR expression in prostate cancer cells by causing an 22.4% (11/49) demonstrated a 50% PSA decline (PSA50). In increase in AR protein degradation. These open-label phase I ARMOR2 part 1, across all doses, PSA30 was 64.0% (16/25) and and II studies [Androgen Receptor Modulation Optimized PSA50 was 48.0% (12/25). In the 2,550-mg dose cohort, PSA30 for Response-1 (ARMOR1) and ARMOR2 part 1] evaluated was 72.7% (8/11) and PSA50 was 54.5% (6/11). Galeterone was the efficacy and safety of galeterone in patients with treat- well tolerated; the most common adverse events were fatigue, ment-naive nonmetastatic or metastatic castration-resistant increased liver enzymes, gastrointestinal events, and pruritus. Most prostate cancer (CRPC) and established a dose for further were mild or moderate in severity and required no action and there study. were no apparent mineralocorticoid excess (AME) events. -
Classification Decisions Taken by the Harmonized System Committee from the 47Th to 60Th Sessions (2011
CLASSIFICATION DECISIONS TAKEN BY THE HARMONIZED SYSTEM COMMITTEE FROM THE 47TH TO 60TH SESSIONS (2011 - 2018) WORLD CUSTOMS ORGANIZATION Rue du Marché 30 B-1210 Brussels Belgium November 2011 Copyright © 2011 World Customs Organization. All rights reserved. Requests and inquiries concerning translation, reproduction and adaptation rights should be addressed to [email protected]. D/2011/0448/25 The following list contains the classification decisions (other than those subject to a reservation) taken by the Harmonized System Committee ( 47th Session – March 2011) on specific products, together with their related Harmonized System code numbers and, in certain cases, the classification rationale. Advice Parties seeking to import or export merchandise covered by a decision are advised to verify the implementation of the decision by the importing or exporting country, as the case may be. HS codes Classification No Product description Classification considered rationale 1. Preparation, in the form of a powder, consisting of 92 % sugar, 6 % 2106.90 GRIs 1 and 6 black currant powder, anticaking agent, citric acid and black currant flavouring, put up for retail sale in 32-gram sachets, intended to be consumed as a beverage after mixing with hot water. 2. Vanutide cridificar (INN List 100). 3002.20 3. Certain INN products. Chapters 28, 29 (See “INN List 101” at the end of this publication.) and 30 4. Certain INN products. Chapters 13, 29 (See “INN List 102” at the end of this publication.) and 30 5. Certain INN products. Chapters 28, 29, (See “INN List 103” at the end of this publication.) 30, 35 and 39 6. Re-classification of INN products. -
Tanibirumab (CUI C3490677) Add to Cart
5/17/2018 NCI Metathesaurus Contains Exact Match Begins With Name Code Property Relationship Source ALL Advanced Search NCIm Version: 201706 Version 2.8 (using LexEVS 6.5) Home | NCIt Hierarchy | Sources | Help Suggest changes to this concept Tanibirumab (CUI C3490677) Add to Cart Table of Contents Terms & Properties Synonym Details Relationships By Source Terms & Properties Concept Unique Identifier (CUI): C3490677 NCI Thesaurus Code: C102877 (see NCI Thesaurus info) Semantic Type: Immunologic Factor Semantic Type: Amino Acid, Peptide, or Protein Semantic Type: Pharmacologic Substance NCIt Definition: A fully human monoclonal antibody targeting the vascular endothelial growth factor receptor 2 (VEGFR2), with potential antiangiogenic activity. Upon administration, tanibirumab specifically binds to VEGFR2, thereby preventing the binding of its ligand VEGF. This may result in the inhibition of tumor angiogenesis and a decrease in tumor nutrient supply. VEGFR2 is a pro-angiogenic growth factor receptor tyrosine kinase expressed by endothelial cells, while VEGF is overexpressed in many tumors and is correlated to tumor progression. PDQ Definition: A fully human monoclonal antibody targeting the vascular endothelial growth factor receptor 2 (VEGFR2), with potential antiangiogenic activity. Upon administration, tanibirumab specifically binds to VEGFR2, thereby preventing the binding of its ligand VEGF. This may result in the inhibition of tumor angiogenesis and a decrease in tumor nutrient supply. VEGFR2 is a pro-angiogenic growth factor receptor -
IJBCP International Journal of Basic & Clinical Pharmacology Antiepileptic
Print ISSN: 2319-2003 | Online ISSN: 2279-0780 IJBCP International Journal of Basic & Clinical Pharmacology DOI: http://dx.doi.org/10.18203/2319-2003.ijbcp20161495 Review Article Antiepileptic drugs: newer targets and new drugs Vihang S. Chawan, Abhishek M. Phatak*, Kalpesh V. Gawand, Sagar V. Badwane, Sagar S. Panchal Department of Pharmacology, TNMC and BYL Nair Ch. Hospital Mumbai, Maharashtra, India ABSTRACT Received: 10 March 2016 Epilepsy is a common neurological disorder affecting 0.5-1% of the population Accepted: 15 April 2016 in India. Majority of patients respond to currently available antiepileptic drugs (AEDs), but a small percentage of patients have shown poor and inadequate *Correspondence to: response to AEDs in addition to various side effects and drug interactions while Dr. Abhishek Madan Phatak, on therapy. Thus there is a need to develop more effective AEDs in drug Email: abhishekphatak9288 resistant epilepsy which have a better safety profile with minimal adverse @gmail.com effects. The United States food and drug administration (USFDA) has approved eslicarbazepine acetate, ezogabine, perampanel and brivaracetam which have Copyright: © the author(s), shown a promising future as better AEDs and drugs like ganaxolone, intranasal publisher and licensee Medip diazepam, ICA- 105665, valnoctamide, VX-765, naluzotan are in the pipeline. Academy. This is an open- access article distributed under Keywords: Epilepsy, Newer antiepileptic drugs, Eslicarbazepine Acetate, the terms of the Creative Ezogabine (Retigabine), Perampanel, Brivaracetam, Naluzotan Commons Attribution Non- Commercial License, which permits unrestricted non- commercial use, distribution, and reproduction in any medium, provided the original work is properly cited. INTRODUCTION to AEDs or those patient who have suffered from recurrent seizures, may require surgery. -
WO 2015/072852 Al 21 May 2015 (21.05.2015) P O P C T
(12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2015/072852 Al 21 May 2015 (21.05.2015) P O P C T (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every A61K 36/84 (2006.01) A61K 31/5513 (2006.01) kind of national protection available): AE, AG, AL, AM, A61K 31/045 (2006.01) A61P 31/22 (2006.01) AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, A61K 31/522 (2006.01) A61K 45/06 (2006.01) BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (21) International Application Number: HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, PCT/NL20 14/050780 KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, (22) International Filing Date: MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, 13 November 2014 (13.1 1.2014) PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, (25) Filing Language: English TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (26) Publication Language: English (84) Designated States (unless otherwise indicated, for every (30) Priority Data: kind of regional protection available): ARIPO (BW, GH, 61/903,430 13 November 2013 (13. 11.2013) US GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, (71) Applicant: RJG DEVELOPMENTS B.V.