(S)-N-Methylnaltrexone
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Lack of Influence of Substrate on Ligand Interaction with the Human Multidrug
Downloaded from molpharm.aspetjournals.org at ASPET Journals on September 23, 2021 page 1 nd Interaction with the Human Multidrug Multidrug Human the with nd Interaction This article has not been copyedited and formatted. The final version may differ from this version. This article has not been copyedited and formatted. The final version may differ from this version. This article has not been copyedited and formatted. The final version may differ from this version. This article has not been copyedited and formatted. The final version may differ from this version. This article has not been copyedited and formatted. The final version may differ from this version. This article has not been copyedited and formatted. The final version may differ from this version. This article has not been copyedited and formatted. The final version may differ from this version. This article has not been copyedited and formatted. The final version may differ from this version. This article has not been copyedited and formatted. The final version may differ from this version. This article has not been copyedited and formatted. The final version may differ from this version. This article has not been copyedited and formatted. The final version may differ from this version. This article has not been copyedited and formatted. The final version may differ from this version. This article has not been copyedited and formatted. The final version may differ from this version. This article has not been copyedited and formatted. The final version may differ from this version. This article has not been copyedited and formatted. The final version may differ from this version. -
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 -
United States Patent (10) Patent No.: US 8,916,581 B2 Boyd Et Al
USOO891 6581 B2 (12) United States Patent (10) Patent No.: US 8,916,581 B2 Boyd et al. (45) Date of Patent: *Dec. 23, 2014 (54) (S)-N-METHYLNALTREXONE 4,194,045 A 3, 1980 Adelstein 4,203,920 A 5, 1980 Diamond et al. (75) Inventors: Thomas A. Boyd, Grandview, NY (US); 4,241,066 A 12, 1980 Kobylecki et al. H OW d Wagoner,goner, Warwick,s NY (US);s 4,311,833.4,277,605 A T.1/1982 1981 NamikoshiBuyniski et etal. al. Suketu P. Sanghvi, Kendall Park, NJ 4.322,426 A 3/1982 Hermann et al. (US); Christopher Verbicky, 4.326,074 A 4, 1982 Diamond et al. Broadalbin, NY (US); Stephen 4.326,075 A 4, 1982 Diamond et al. “. s 4,377.568 A 3/1983 Chopra et al. Andruski, Clifton Park, NY (US) 4.385,078 A 5/1983 Onda et al. 4.427,676 A 1/1984 White et al. (73) Assignee: Progenics Pharmaceuticals, Inc., 4,430,327 A 2, 1984 Frederickson et al. Tarrytown, NY (US) 4,452,775 A 6/1984 Kent 4,457,907 A 7/1984 Porteret al. (*) Notice: Subject to any disclaimer, the term of this 4,462.839 A 7/1984 McGinley et al. patent is extended or adjusted under 35 4,518.4334,466,968 A 5/19858, 1984 McGinleyBernstein et al. U.S.C. 154(b) by 344 days. 4,533,739 A 8/1985 Pitzele et al. This patent is Subject to a terminal dis- 4,606,9094,556,552 A 12/19858/1986 PorterBechgaard et al. -
Genl:VE 1970 © World Health Organization 1970
Nathan B. Eddy, Hans Friebel, Klaus-Jiirgen Hahn & Hans Halbach WORLD HEALTH ORGANIZATION ORGANISATION .MONDIALE DE LA SANT~ GENl:VE 1970 © World Health Organization 1970 Publications of the World Health Organization enjoy copyright protection in accordance with the provisions of Protocol 2 of the Universal Copyright Convention. Nevertheless governmental agencies or learned and professional societies may reproduce data or excerpts or illustrations from them without requesting an authorization from the World Health Organization. For rights of reproduction or translation of WHO publications in toto, application should be made to the Division of Editorial and Reference Services, World Health Organization, Geneva, Switzerland. The World Health Organization welcomes such applications. Authors alone are responsible for views expressed in signed articles. The designations employed and the presentation of the material in this publication do not imply the expression of any opinion whatsoever on the part of the Director-General of the World Health Organization concerning the legal status of any country or territory or of its authorities, or concerning the delimitation of its frontiers. Errors and omissions excepted, the names of proprietary products are distinguished by initial capital letters. © Organisation mondiale de la Sante 1970 Les publications de l'Organisation mondiale de la Sante beneficient de la protection prevue par les dispositions du Protocole n° 2 de la Convention universelle pour la Protection du Droit d'Auteur. Les institutions gouvernementales et les societes savantes ou professionnelles peuvent, toutefois, reproduire des donnees, des extraits ou des illustrations provenant de ces publications, sans en demander l'autorisation a l'Organisation mondiale de la Sante. Pour toute reproduction ou traduction integrate, une autorisation doit etre demandee a la Division des Services d'Edition et de Documentation, Organisation mondiale de la Sante, Geneve, Suisse. -
Pharmacy and Poisons (Third and Fourth Schedule Amendment) Order 2017
Q UO N T FA R U T A F E BERMUDA PHARMACY AND POISONS (THIRD AND FOURTH SCHEDULE AMENDMENT) ORDER 2017 BR 111 / 2017 The Minister responsible for health, in exercise of the power conferred by section 48A(1) of the Pharmacy and Poisons Act 1979, makes the following Order: Citation 1 This Order may be cited as the Pharmacy and Poisons (Third and Fourth Schedule Amendment) Order 2017. Repeals and replaces the Third and Fourth Schedule of the Pharmacy and Poisons Act 1979 2 The Third and Fourth Schedules to the Pharmacy and Poisons Act 1979 are repealed and replaced with— “THIRD SCHEDULE (Sections 25(6); 27(1))) DRUGS OBTAINABLE ONLY ON PRESCRIPTION EXCEPT WHERE SPECIFIED IN THE FOURTH SCHEDULE (PART I AND PART II) Note: The following annotations used in this Schedule have the following meanings: md (maximum dose) i.e. the maximum quantity of the substance contained in the amount of a medicinal product which is recommended to be taken or administered at any one time. 1 PHARMACY AND POISONS (THIRD AND FOURTH SCHEDULE AMENDMENT) ORDER 2017 mdd (maximum daily dose) i.e. the maximum quantity of the substance that is contained in the amount of a medicinal product which is recommended to be taken or administered in any period of 24 hours. mg milligram ms (maximum strength) i.e. either or, if so specified, both of the following: (a) the maximum quantity of the substance by weight or volume that is contained in the dosage unit of a medicinal product; or (b) the maximum percentage of the substance contained in a medicinal product calculated in terms of w/w, w/v, v/w, or v/v, as appropriate. -
(12) United States Patent (10) Patent No.: US 6,264,917 B1 Klaveness Et Al
USOO6264,917B1 (12) United States Patent (10) Patent No.: US 6,264,917 B1 Klaveness et al. (45) Date of Patent: Jul. 24, 2001 (54) TARGETED ULTRASOUND CONTRAST 5,733,572 3/1998 Unger et al.. AGENTS 5,780,010 7/1998 Lanza et al. 5,846,517 12/1998 Unger .................................. 424/9.52 (75) Inventors: Jo Klaveness; Pál Rongved; Dagfinn 5,849,727 12/1998 Porter et al. ......................... 514/156 Lovhaug, all of Oslo (NO) 5,910,300 6/1999 Tournier et al. .................... 424/9.34 FOREIGN PATENT DOCUMENTS (73) Assignee: Nycomed Imaging AS, Oslo (NO) 2 145 SOS 4/1994 (CA). (*) Notice: Subject to any disclaimer, the term of this 19 626 530 1/1998 (DE). patent is extended or adjusted under 35 O 727 225 8/1996 (EP). U.S.C. 154(b) by 0 days. WO91/15244 10/1991 (WO). WO 93/20802 10/1993 (WO). WO 94/07539 4/1994 (WO). (21) Appl. No.: 08/958,993 WO 94/28873 12/1994 (WO). WO 94/28874 12/1994 (WO). (22) Filed: Oct. 28, 1997 WO95/03356 2/1995 (WO). WO95/03357 2/1995 (WO). Related U.S. Application Data WO95/07072 3/1995 (WO). (60) Provisional application No. 60/049.264, filed on Jun. 7, WO95/15118 6/1995 (WO). 1997, provisional application No. 60/049,265, filed on Jun. WO 96/39149 12/1996 (WO). 7, 1997, and provisional application No. 60/049.268, filed WO 96/40277 12/1996 (WO). on Jun. 7, 1997. WO 96/40285 12/1996 (WO). (30) Foreign Application Priority Data WO 96/41647 12/1996 (WO). -
Drug Name Plate Number Well Location % Inhibition, Screen Axitinib 1 1 20 Gefitinib (ZD1839) 1 2 70 Sorafenib Tosylate 1 3 21 Cr
Drug Name Plate Number Well Location % Inhibition, Screen Axitinib 1 1 20 Gefitinib (ZD1839) 1 2 70 Sorafenib Tosylate 1 3 21 Crizotinib (PF-02341066) 1 4 55 Docetaxel 1 5 98 Anastrozole 1 6 25 Cladribine 1 7 23 Methotrexate 1 8 -187 Letrozole 1 9 65 Entecavir Hydrate 1 10 48 Roxadustat (FG-4592) 1 11 19 Imatinib Mesylate (STI571) 1 12 0 Sunitinib Malate 1 13 34 Vismodegib (GDC-0449) 1 14 64 Paclitaxel 1 15 89 Aprepitant 1 16 94 Decitabine 1 17 -79 Bendamustine HCl 1 18 19 Temozolomide 1 19 -111 Nepafenac 1 20 24 Nintedanib (BIBF 1120) 1 21 -43 Lapatinib (GW-572016) Ditosylate 1 22 88 Temsirolimus (CCI-779, NSC 683864) 1 23 96 Belinostat (PXD101) 1 24 46 Capecitabine 1 25 19 Bicalutamide 1 26 83 Dutasteride 1 27 68 Epirubicin HCl 1 28 -59 Tamoxifen 1 29 30 Rufinamide 1 30 96 Afatinib (BIBW2992) 1 31 -54 Lenalidomide (CC-5013) 1 32 19 Vorinostat (SAHA, MK0683) 1 33 38 Rucaparib (AG-014699,PF-01367338) phosphate1 34 14 Lenvatinib (E7080) 1 35 80 Fulvestrant 1 36 76 Melatonin 1 37 15 Etoposide 1 38 -69 Vincristine sulfate 1 39 61 Posaconazole 1 40 97 Bortezomib (PS-341) 1 41 71 Panobinostat (LBH589) 1 42 41 Entinostat (MS-275) 1 43 26 Cabozantinib (XL184, BMS-907351) 1 44 79 Valproic acid sodium salt (Sodium valproate) 1 45 7 Raltitrexed 1 46 39 Bisoprolol fumarate 1 47 -23 Raloxifene HCl 1 48 97 Agomelatine 1 49 35 Prasugrel 1 50 -24 Bosutinib (SKI-606) 1 51 85 Nilotinib (AMN-107) 1 52 99 Enzastaurin (LY317615) 1 53 -12 Everolimus (RAD001) 1 54 94 Regorafenib (BAY 73-4506) 1 55 24 Thalidomide 1 56 40 Tivozanib (AV-951) 1 57 86 Fludarabine -
Put Microrna Drug Discovery
Research Collection Doctoral Thesis Gene circuit based screening assays for mirna drug discovery Author(s): Häfliger, Benjamin Publication Date: 2016 Permanent Link: https://doi.org/10.3929/ethz-a-010651992 Rights / License: In Copyright - Non-Commercial Use Permitted This page was generated automatically upon download from the ETH Zurich Research Collection. For more information please consult the Terms of use. ETH Library DISS. ETH NO. 23325 GENE CIRCUIT BASED SCREENING ASSAYS FOR MIRNA DRUG DISCOVERY A thesis submitted to attain the degree of DOCTOR OF SCIENCES of ETH ZURICH (Dr. sc. ETH Zurich) presented by BENJAMIN HÄFLIGER MSc ETH Biotech, ETH Zurich born on 25.02.1988 citizen of Fischbach, LU accepted on the recommendation of Prof. Dr. Yaakov Benenson Prof. Dr. Sven Panke Dr. Helge Grosshans 2016 ii Abstract Drug discovery is the process of identifying potential new medicines. A key step in this process is high throughput screening (HTS), whereby active compounds are identified from a large library of up to one million candidate molecules. Through minia- turization and automation, such libraries can nowadays be tested in a single week. Despite this impressive performance, about 50% of the screening campaigns fail to provide the desired hits, or the emerging lead compounds do not perform as expected in clinical settings, mostly due to toxicity from off-target interactions. To overcome this issue, novel HTS assays should provide more detailed information on the underlying biology and the relevant off-targets. Multiplexed assays based on liquid chromatog- raphy-mass spectroscopy or deep sequencing could deliver this information; yet, their throughput is comparably low. -
Trabajo De Diploma
Facultad de Química-Farmacia Departamento de Farmacia Trabajo de diploma Título: Evaluación experimental “in vivo” de nuevos compuestos con actividad analgésica seleccionados a través del tamizaje virtual. Autor: Yulier León Mederos Tutores: Dr. Yovani Marrero Ponce MSc. Arelis López Sacerio 2009-2010 Exergo Todos y cada uno de nosotros paga puntualmente su cuota de sacrificio consciente de recibir el premio en la satisfacción del deber cumplido, conscientes de avanzar con todos hacia el Hombre Nuevo que se vislumbra en el horizonte... Che Yulier León Mederos Evaluación experimental “in vivo” de nuevos compuestos con actividad analgésica seleccionados a través del tamizaje virtual Dedicatoria A alguien que se lo merece, por su ayuda y su apoyo durante esta larga carrera como estudiante universitario, mi madre la cual confió siempre en mí y por ver esperado con paciencia esta gran hazaña. Elisa Jorge por verse convertido en mi madre y por su apoyo incondicional cada día que transcurrió en esta escuela. A mis hermanos por estar siempre a mí lado cuando más yo los necesitaba, a mi abuela que no pudo disfrutar esta gran victoria junto a mí, pero allá donde ella está le llegará este lindo regalo. Yulier León Mederos Evaluación experimental “in vivo” de nuevos compuestos con actividad analgésica seleccionados a través del tamizaje virtual Agradecimientos Esta página está dedicada a todas aquellas personas que de un modo u otro hicieron posible la realización de esta tesis. Quisiera agradecer en primer lugar a mi madre que siempre depositó todo su amor y confianza en mí, sobre todo en los momentos difíciles a lo largo de mi carrera A mis hermanos ya que sus consejos siempre fueron buenos y por el aprecio que siento hacia ellos. -
Neuropathic Pain: Delving Into the Oxidative Origin and the Possible Implication of Transient Receptor Potential Channels
REVIEW published: 14 February 2018 doi: 10.3389/fphys.2018.00095 Neuropathic Pain: Delving into the Oxidative Origin and the Possible Implication of Transient Receptor Potential Channels Cristina Carrasco 1*, Mustafa Nazirogluˇ 2, Ana B. Rodríguez 1 and José A. Pariente 1 1 Department of Physiology, Faculty of Sciences, University of Extremadura, Badajoz, Spain, 2 Neuroscience Research Center, Suleyman Demirel University, Isparta, Turkey Currently, neuropathic pain is an underestimated socioeconomic health problem affecting millions of people worldwide, which incidence may increase in the next years due to chronification of several diseases, such as cancer and diabetes. Growing evidence links neuropathic pain present in several disorders [i.e., spinal cord injury (SCI), cancer, diabetes and alcoholism] to central sensitization, as a global result of mitochondrial dysfunction induced by oxidative and nitrosative stress. Additionally, inflammatory signals Edited by: and the overload in intracellular calcium ion could be also implicated in this complex Ali Mobasheri, network that has not yet been elucidated. Recently, calcium channels namely transient University of Surrey, United Kingdom receptor potential (TRP) superfamily, including members of the subfamilies A (TRAP1), M Reviewed by: Felipe Simon, (TRPM2 and 7), and V (TRPV1 and 4), have demonstrated to play a role in the nociception Universidad Andrés Bello, Chile mediated by sensory neurons. Therefore, as neuropathic pain could be a consequence of Enrique Soto, the imbalance between reactive oxygen species and endogen antioxidants, antioxidant Benemérita Universidad Autónoma de Puebla, Mexico supplementation may be a treatment option. This kind of therapy would exert its beneficial *Correspondence: action through antioxidant and immunoregulatory functions, optimizing mitochondrial Cristina Carrasco function and even increasing the biogenesis of this vital organelle; on balance, antioxidant [email protected] supplementation would improve the patient’s quality of life. -