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Review of Clinical Pharmacology and Pharmacokinetics INTERNATIONAL EDITION Review of Clinical Pharmacology and Pharmacokinetics INTERNATIONAL EDITION EDITORS-IN-CHIEF: Prof. STAVROS T. PLESSAS, M.D. and Dr CHARALAMPOS T. PLESSAS EDITORIAL BOARD Prof. FRAGISKI ANTHOULI-ANAGNOSTOPOULOU (Athens) Prof. JOHN MATSOUKAS (Patras) Assoc. Prof. EUTYCHIA ASPRODINI (Larissa) Prof. THOMAS MAVROMOUSTAKOS (Athens) Dr ANTHONY AVGERINOS (Athens) Assist. Prof. NIKOLAOS STEFANOPOULOS (Patras) Assist. Prof. FOTOULA BABATSIKOU-KOUTI (Athens) Prof. GEORGE PANAYIOTAKIS (Patras) Dr CORINNE A. BENAKIS (Geneva) Prof. MARIA PAPADIMITRIOU (Patras) Assist. Prof. EVDOKIA BILLIS (Patras) Prof. KOSTAS PAPADOPOULOS (Thessaloniki) Assoc. Prof. ANNA DELTSIDOY (Athens) Dr PAUL C. PAPADOPOULOS (Thessaloniki) Prof. YVONNE DIMOULA (Athens) Prof. PARASKEVI PAPAIOANNIDOU (Thessaloniki) Assist. Prof. MARIANNA DIOMIDOUS (Athens) Dr NIKI GEORGATOU-PAPAGEORGIOU (Athens) Prof. CHRISTODOULOS FLORDELLIS (Patras) Prof. ANDREAS PAPAPETROPOULOS (Athens) Prof. GEORGE GIOFTSOS (Lamia) Assist. Prof. PANAYOTIS PLESSAS (USA) Prof. ACHILLEAS GRAVANIS (Heraklion) Prof. AGAPIOS PETRIDIS (Athens) Prof. ANASTASIA KANELLOU (Athens) Prof. GEORGE POLICHRONOPOULOS (Athens) Prof. GEORGE KARAKIULAKIS (Thessaloniki) Prof. EVANGELIA PROTOPAPA (Athens) Prof. KONSTANTINOS KALLARAS (Thessaloniki) Prof. VASILIKI SAKELLARI (Lamia) Assoc. Prof. THEOFANIS KATOSTARAS (Athens) Prof. NΙΚOS SAKELLARIDIS (Larissa) Prof. VASSILIKI KEFALA (Athens) Prof. NIKOLAOS M. SITARAS (Athens) Prof. HELEN KINTZIOU (Athens) Prof. GREGORY SKALKEAS (Athens) Prof. MICHAEL P. KITROU (Patras) Assist. Prof. NIKOLAOS D. THALASSINOS (Athens) Prof. BASILE KOKKAS (Thessaloniki) Assoc. Prof. HELEN THEODOSOPOULOU (Athens) Prof. THEODOROS KONSTANTINIDIS (Alexandroupolis) Prof. DEMETRIOS TRICHOPOULOS (Athens) Prof. CHARILAOS KOUTIS (Athens) Prof. ASTERIOS TSIFTSOGLOU (Thessaloniki) Prof. DIMITRIOS KOUVELAS (Thessaloniki) Prof. MARIA MIRONIDOU-TZOUVELEKI (Thessaloniki) Assoc. Prof. CHARIS LIAPI (Athens) Prof. ZAMPIA VARDAKI (Athens) Prof. JOHN MANTAS (Athens) Prof. MARIA VENETIKOU (Athens) Assist. Prof. CHRISTOS MASOUROS (Chalkis) Assoc. Prof. ATHANASIOS ZISIMOPOULOS (Alexandroupo- Dr ELISABETH-ADAMANTIA MASOUROU (Athens) lis) Assoc. Prof. ANDREAS YIACOUMETTIS (Alexandroupolis) Articles published in this Journal are Indexed or Abstracted in: ••• Chemical Abstracts ••• Elsevier' Bibliographic Databases: Scopus, EMBASE, EMBiology, Elsevier BIOBASE ••• SCImago Journal and Country Rank Factor Further informations regarding the Journal can be seen in the web address: http://pharmakonpress.gr 2 REVIEW OF CLINICAL PHARMACOLOGY AND PHARMACOKINETICS, INTERNATIONAL EDITION 2014 Review of Clinical Pharmacology and Pharmacokinetics INTERNATIONAL EDITION a Published three times a year by PHARMAKON-Press Publisher Responsible According to the Law Helen S. Plessa 9A Kanari str., GR-1532, Nea Penteli, Athens, Hellas Tel.- Fax 00302109756332 Email: splessas @otenet.gr & [email protected] Τετραµηνιαία Έκδοση από την ΦΑΡΜΑΚΟΝ-Τύπος Ιδιοκτήτης-Υπεύθυνος κατά το Νόµο Ελένη Πλέσσα του Σταύρου Κανάρη 9Α, GR-15232, Νέα Πεντέλη, Αθήνα, Ελλάς Τηλ.- Fax 00302109756332 Email: splessas @otenet.gr & [email protected] a EDITORS-IN-CHIEF Professor Stavros T. Plessas MD, Tel./Fax 00302107700663 Email: splessas @otenet.gr & [email protected] Dr Charalampos T. Plessas, Tel. 00302107778101 Email: lplessas @otenet.gr & [email protected] ΕΚ∆ΟΤΕΣ Καθηγ. Ιατρός: Σταύρος Τ. Πλέσσας, Τηλ.-Fax 0030 2107700663 Email: splessas @otenet.gr & [email protected] ∆ρ Χαράλαµπος Τ. Πλέσσας: Τηλ. 00302107778101 Email: lplessas @otenet.gr & [email protected] a Original Papers, Review Articles, as well as short preliminary communications will be considered for publication and should be send to the Editors-in Chief Πρωτότυπες Ερευνητικές Εργασίες, Άρθρα Επισκόπησης και Ενηµέρωσης, καθώς και Κλινικές Μελέτες µε άµεση σχέση το Φάρµακο και τη Θεραπευτική πρέπει να αποστέλ- λονται στους Εκδότες a Online ISSN 1011-6583 Articles published in this Journal are Indexed or Abstracted in: ••• Chemical Abstracts ••• Elsevier’s Bibliographic Databases: Scopus, EMBASE, EMBiology, Elsevier BIOBASE ••• SCImago Journal and Coun- try Rank Factor 15 th CONFERENCE MEDICINAL CHEMISTRY: DRUG DISCOVERY AND DESIGN, PATRAS, HELLAS 3 VOLUME 28 a 2014 No 1 CONTENTS J. MATSOUKAS…………………………………....8 Drug: Membrane interactions and drug discovery Letter from the Guest Editor A. CHATZIKONSTANTINOU, M. CHATZIATHA- NASSIADOU, N. SAYYAD, A. PRIMIKIRI, E. GIANNOPOULOU, H. KALOFONOS, J. MAT- Forewords SOUKAS, H. STAMATIS, I.P. GEROTHANAS- SIS, A.G. TZAKOS……………………………….17 J. MATSOUKAS……………………………………9 th The Smallest on line bioreactor: Drug develop- 15 Medicinal Chemistry Conference, Official ment in the NMR tube Opening: Introduction I. MARGIOLAKI…………………………………...18 A.V. SCHALLY……………………………………..9 Macromolecular micro-crystallography: Perspec- tives in drug discovery Abstracts Lectures G. RASSIAS, R.A. WARD, N.G. STEVENSON, K.M.P. WHEELHOUSE, K.L. LLEWELLYN, A. OCHEN, C.W. JONES, E.C. HOOK……………18 H. zur HAUSEN, E.-M. DE VILLIERS………….11 Trametinib: The first approved MEK inhibitor for Contributions of Infections to human carcino- the treatment of cancer genesis - Mechanisms and perspectives S.K. HADJIKAKOU……………………………….19 V. APOSTOLOPOULOS…………………………11 Design and development of new silver, organotin, Development of a breast and an ovarian cancer and antimony metallo-drugs which bind to lipoxy- vaccine: What have we achieved in 20 years? genase and DNA, modulating their function and C.A. GOGOS AND K. AKINOSOGLOU………..12 inducing apoptosis Sepsis syndrome: From research to clinical prac- tice Abstracts Posters K. BARLOS AND D. GATOS……………………13 Single chain insulins: Novel high tech products S. VASILAKAKI, T. MAVROMOUSTAKOS, G. V. TSEVELEKI, T. TSELIOS, I. KANISTRAS, O. KOKOTOS………………………………………...21 KOUTSONI, I. FRILIGOU, V. APOSTOLOPOU- Docking studies on coumarin and quinolinone LOS, E. DOTSIKA, J. MATSOUKAS, H. LASS- derivatives as sPLA 2 GIIA inhibitors MANN, L. PROBERT…………………………….14 Immunotherapy of experimental autoimmune K. KATSIKANI, G. STATHOPOULOS………….21 encephalomyelitis using APC-targeted myelin Study for the effect of p68, RNA-helicase on the peptides as prophylactic and therapeutic vac- growth of different types of cancer in vitro and in cines vivo J. MATSOUKAS, M.-E. ANDROUTSOU………14 M. KOSMA, M. RODI, E. PASMATZI, A. MO- Elmyelin, a novel potential vaccine in the treat- NASTIRLI, D. TSAMBAOS, A. MOUZAKI……..22 ment of multiple sclerosis: Preparation of IND File In vitro study of the effects of imiquimodin iso- towards phase I clinical investigation lated peripheral blood cell populations (PBMC) of patients with recurrent herpes labialis and healthy M.D. VLAHAKOS, A. DRAKOU…………………15 controls Hepcidin: A new peptide modulator of erythropoi- esis A.-M. KARAGIANNI, M.-E. ANDROUTSOU, M. MICHALATOU, M. ANTONOPOULOS, G. AGE- T. CHRISTOPOULOS……………………………16 LIS, T. TSELIOS, J. MATSOUKAS……………..22 Biosensors: Progress and prospective Comparative in vitro evaluation using full skin and stratum corneum in the transdermal delivery of G. PATRINOS…………………………………….16 losartan for the treatment of hypertension From the DNA structure to gene and to Genetic Medicine C. APOSTOLOPOULOU, A. MARAZIOTI, A. MOUSTAKI, T. AGALIOTI, A. GIANNOU, G. T. MAVROMOUSTAKOS………………………..17 STATHOPOULOS………………………………..23 4 REVIEW OF CLINICAL PHARMACOLOGY AND PHARMACOKINETICS, INTERNATIONAL EDITION 2014 Role of KRAS mutations in neoplasmatic activa- D. DIAMANTOPOULOU, A. BEKATOROU, M. tion of nuclear factor-kappa B KALLIS, M. KANELLAKI, A. VLAMIS…………..29 Preparation and study of formulations based on C.N. BANTI, A.D. GIANNOULIS, N. KOURK- pistacia terebinthus l. resin and probiotic sac- OUMELIS, A.M. OWCZARZAK, M. KUBICKI, S.K. charomyces boulardii cells for medical uses HADJIKAKOU……………………………………..24 Interactions of novel metallo-drugs of silver(I) E. FOTOU, A. TSILIGIANNI, S. ZEVGITI, C. complex towards intracellular molecules PAPADOPOULOS, E. PANOU-POMONIS, G. PANAGIARIS, M. SAKARELLOS-DAITSIO- C. TRIANTIS, A. SHEGANI, C. RAPTOPOULOU, TIS………………………………………………….30 A. TERZIS, M. PELECANOU, I. PIRMETTIS, M. Keratin and collagen polypeptide models as a PAPADOPOULOS………………………………..24 means for assessing the deterioration of organic Synthesis and characterization of new Fac- 1 materials of cultural heritage [M(Νο)(L )(Co) 3] mixed ligand complexes E. VRONTAKI, G. MELAGRAKI, T. MAVRO- C. TRIANTIS, A. LAZOPOULOS, M. SAGNOU, MOUSTAKOS, A. AFANTITIS…………………..31 M. PELECANOU, I. PIRMETTIS, M. PAPA- Exploiting ChEMBL database to identify indole DOPOULOS......................................................25 analogues as HCV replication inhibitors Synthesis, characterization and biodistribution of 1 new fac-[M(ΝΟ)(L )(CO) 3] mixed ligand comple- E.Ι. GKANIATSOU, C.Ν. BANTI, N. KOURKOU- xes for imaging of Alzheimer’s Disease MELIS, S. SKOULIKA, S.K. HADJIKAKOU……31 Synthesis, characterisation and bioactivity of he- C. SEMIDALAS, I. TSERTOU, P. GENNAIOU, A. xadecyltrimethyl-ammonium bromide-silver com- TZANI, M. ROUSSAKI, C. NIXARLIDIS, A. plex micelles in aqueous media DETSI, P. ZOUMPOULAKIS……………………25 Novel hydroxytyrosol (HT) analogues as potential E. GIANNOPOULOU, C.-S. KITSOU, C. PETRO- antioxidants and COX-2 inhibitors POULOS, J. SLANINOVÁ, Η.P. KALOFONOS, P. CORDOPATIS, V. MAGAFA…………………….32 C. BAKAVOS, C. ATHANASSOPOULOS, D. Studies of οxytocin analogues on breast cancer PEPE, A. NAPOLI, F. MAZZOTTI, G. SIN- cells proliferation DONA………………………………………………26 N-Hydroxysuccinimidyl p-methoxybenzoate as E. KRITSI, C. POTAMITIS,
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