Search

Your search keyword '"Linnanen, Tero"' showing total 23 results
Start Over Author "Linnanen, Tero"
23 results on '"Linnanen, Tero"'

2. Supplementary Table S1 and Figures S1-S7 from ODM-203, a Selective Inhibitor of FGFR and VEGFR, Shows Strong Antitumor Activity, and Induces Antitumor Immunity

Author

Holmström, Tim H., primary, Moilanen, Anu-Maarit, primary, Ikonen, Tarja, primary, Björkman, Mari L., primary, Linnanen, Tero, primary, Wohlfahrt, Gerd, primary, Karlsson, Stefan, primary, Oksala, Riikka, primary, Korjamo, Timo, primary, Samajdar, Susanta, primary, Rajagopalan, Srinivasan, primary, Chelur, Shekar, primary, Narayanan, Kishore, primary, Ramachandra, Raghuveer K., primary, Mani, Jiju, primary, Nair, Rashmi, primary, Gowda, Nagaraj, primary, Anthony, Thomas, primary, Dhodheri, Samiulla, primary, Mukherjee, Subhendu, primary, Ujjinamatada, Ravi K., primary, Srinivas, Nanduri, primary, Ramachandra, Murali, primary, and Kallio, Pekka J., primary

Published
2023
Full Text
View/download PDF

3. Data from ODM-203, a Selective Inhibitor of FGFR and VEGFR, Shows Strong Antitumor Activity, and Induces Antitumor Immunity

Author

Holmström, Tim H., primary, Moilanen, Anu-Maarit, primary, Ikonen, Tarja, primary, Björkman, Mari L., primary, Linnanen, Tero, primary, Wohlfahrt, Gerd, primary, Karlsson, Stefan, primary, Oksala, Riikka, primary, Korjamo, Timo, primary, Samajdar, Susanta, primary, Rajagopalan, Srinivasan, primary, Chelur, Shekar, primary, Narayanan, Kishore, primary, Ramachandra, Raghuveer K., primary, Mani, Jiju, primary, Nair, Rashmi, primary, Gowda, Nagaraj, primary, Anthony, Thomas, primary, Dhodheri, Samiulla, primary, Mukherjee, Subhendu, primary, Ujjinamatada, Ravi K., primary, Srinivas, Nanduri, primary, Ramachandra, Murali, primary, and Kallio, Pekka J., primary

Published
2023
Full Text
View/download PDF

4. Novel Selective Estrogen Receptor Modulator Ameliorates Murine Colitis

Author

Polari, Lauri, Anttila, Santeri, Helenius, Terhi, Wiklund, Anu, Linnanen, Tero, Toivola, Diana M., and Määttä, Jorma

Subjects
Male, Selective Estrogen Receptor Modulators, Colon, colitis, Dextran Sulfate, selective estrogen receptor modulator, Article, Monocytes, progesterone receptor, macrophages, lcsh:Chemistry, Disease Models, Animal, Mice, lcsh:Biology (General), lcsh:QD1-999, inflammation, Animals, Cytokines, lcsh:QH301-705.5, estrogen receptor
Abstract

Estrogen-receptor-mediated signaling has been suggested to decrease the inflammatory response in monocyte macrophages. Previously, we showed that a novel selective estrogen receptor modulator (SERM2) promotes anti-inflammatory phenotype of monocytes in vitro. In this study, we demonstrate the potential of SERM2 in amelioration of colitis. We utilized a dextran sodium sulfate (DSS)-induced colitis model in FVB/n mice to demonstrate the effects of orally administered SERM2 on the clinical status of the mice and the histopathological changes in the colon, as well as proportion of Mrc-1 positive macrophages. SERM2 nuclear receptor affinities were measured by radioligand binding assays. Orally administered, this compound significantly alleviated DSS-induced colitis in male mice and induced local estrogen receptor activation in the inflamed colon, as well as promoting anti-inflammatory cytokine expression and infiltration of anti-inflammatory monocytes. We show that this novel drug candidate has an affinity to estrogen receptors &alpha, and &beta, and progesterone receptors, but not to glucocorticoid receptor, thus expressing unique binding properties compared to other sex steroid receptor ligands. These results indicate that novel drug candidates to alleviate inflammatory conditions of the colon could be found among sex steroid receptor activating compounds.

Published
2019
Full Text
View/download PDF

6. ODM-203, a Selective Inhibitor of FGFR and VEGFR, Shows Strong Antitumor Activity, and Induces Antitumor Immunity

Author

Holmström, Tim H., primary, Moilanen, Anu-Maarit, additional, Ikonen, Tarja, additional, Björkman, Mari L., additional, Linnanen, Tero, additional, Wohlfahrt, Gerd, additional, Karlsson, Stefan, additional, Oksala, Riikka, additional, Korjamo, Timo, additional, Samajdar, Susanta, additional, Rajagopalan, Srinivasan, additional, Chelur, Shekar, additional, Narayanan, Kishore, additional, Ramachandra, Raghuveer K., additional, Mani, Jiju, additional, Nair, Rashmi, additional, Gowda, Nagaraj, additional, Anthony, Thomas, additional, Dhodheri, Samiulla, additional, Mukherjee, Subhendu, additional, Ujjinamatada, Ravi K., additional, Srinivas, Nanduri, additional, Ramachandra, Murali, additional, and Kallio, Pekka J., additional

Published
2019
Full Text
View/download PDF

9. Intracrine Regulation of Estrogen and Other Sex Steroid Levels in Endometrium and Non-gynecological Tissues; Pathology, Physiology, and Drug Discovery

Author

Konings, Gonda, Brentjens, Linda, Delvoux, Bert, Linnanen, Tero, Cornel, Karlijn, Koskimies, Pasi, Bongers, Marlies, Kruitwagen, Roy, Xanthoulea, Sofia, Romano, Andrea, Konings, Gonda, Brentjens, Linda, Delvoux, Bert, Linnanen, Tero, Cornel, Karlijn, Koskimies, Pasi, Bongers, Marlies, Kruitwagen, Roy, Xanthoulea, Sofia, and Romano, Andrea

Abstract

Our understanding of the intracrine (or local) regulation of estrogen and other steroid synthesis and degradation expanded in the last decades, also thanks to recent technological advances in chromatography mass-spectrometry. Estrogen responsive tissues and organs are not passive receivers of the pool of steroids present in the blood but they can actively modify the intra-tissue steroid concentrations. This allows fine-tuning the exposure of responsive tissues and organs to estrogens and other steroids in order to best respond to the physiological needs of each specific organ. Deviations in such intracrine control can lead to unbalanced steroid hormone exposure and disturbances. Through a systematic bibliographic search on the expression of the intracrine enzymes in various tissues, this review gives an up-to-date view of the intracrine estrogen metabolisms, and to a lesser extent that of progestogens and androgens, in the lower female genital tract, including the physiological control of endometrial functions, receptivity, menopausal status and related pathological conditions. An overview of the intracrine regulation in extra gynecological tissues such as the lungs, gastrointestinal tract, brain, colon and bone is given. Current therapeutic approaches aimed at interfering with these metabolisms and future perspectives are discussed.

Published
2018

11. Abstract 4133: ODM-203, a novel, selective and balanced FGFR and VEGFR inhibitor with strong activity on primary and metastatic tumor growth in FGFR-dependent and angiogenic cancer models

Author

Holmström, Tim, primary, Moilanen, Anu, additional, Björkman, Mari, additional, Linnanen, Tero, additional, Wohlfahrt, Gerd, additional, Karlsson, Stefan, additional, Oksala, Riikka, additional, Korjamo, Timo, additional, Samajdar, Susanta, additional, Rajagopalan, Srinivasan, additional, Chelur, Shekar, additional, Narayan, Kishore, additional, Ramachandra, Raghuveer, additional, Anthony, Thomas, additional, DS, Samiulla, additional, Ramachandra, Murali, additional, and Kallio, Pekka, additional

Published
2015
Full Text
View/download PDF

13. Increasing Selectivity of CC Chemokine Receptor 8 Antagonists by Engineering Nondesolvation Related Interactions with the Intended and Off-Target Binding Sites

Author

Shamovsky, Igor, primary, de Graaf, Chris, additional, Alderin, Lisa, additional, Bengtsson, Malena, additional, Bladh, Håkan, additional, Börjesson, Lena, additional, Connolly, Stephen, additional, Dyke, Hazel J., additional, van den Heuvel, Marco, additional, Johansson, Henrik, additional, Josefsson, Bo-Göran, additional, Kristoffersson, Anna, additional, Linnanen, Tero, additional, Lisius, Annea, additional, Männikkö, Roope, additional, Nordén, Bo, additional, Price, Steve, additional, Ripa, Lena, additional, Rognan, Didier, additional, Rosendahl, Alexander, additional, Skrinjar, Marco, additional, and Urbahns, Klaus, additional

Published
2009
Full Text
View/download PDF

14. Serotonergic aporphine derivatives : Synthesis and structure-activity relationships

Author

Linnanen, Tero and Linnanen, Tero

Abstract

Novel series of well-characterized and stereochemically pure 11-substituted (R)-aporphine derivatives have been prepared and their interaction with serotonin 5-HT7 and 5-HT1A receptors and dopamine D2A and D1 receptors have been studied. Efficient palladium catalyzed reactions were utilized for the diastereoselective synthesis of atropisomers as well as for the synthesis of several of the other (R)-aporphine derivatives. A number of 11-arylated (R)-aporphines displayed high affinity for 5-HT7 and 5-HT1A receptors and derivatives with selectivity for either 5-HT7 or 5-HT1A receptors were obtained by chosing the proper substituents on the 11-phenyl ring. Simultaneous substitution of the 2' and 6' positions of (R)-11-phenylaporphine afforded derivatives, including some atropisomers, with increased 5-HT7 selectivity and several of these analogues were characterized as selective 5-HT7 receptor antagonists. Introduction of substituents in the other positions of the 11-phenyl group resulted in derivatives with selectivity for 5-HT1A receptors. In addition, new series of novel pentacyclic (R)-aporphines were synthesized either by the introduction of a methylene group between carbon atoms C1 and C11 in the (R)-aporphine skeleton or by ring expansion reactions of (R)-1,11-carbonylaporphine. These series of derivatives afforded the possibility to introduce substituents/functional groups below, above and in the plane of the ring system thereby allowing for structural extensions into previously unexplored areas of receptor binding sites. Compounds with various affinities for the serotonin and dopamine receptors were obtained and novel 5-HT7 receptor antagonists were identified. The identification of selective serotonin 5-HT7 receptor antagonists is of particular interest since only a few putatively selective 5-HT7 receptor antagonistic ligands have been reported.

Published
2000

Catalog

Books, media, physical & digital resources
See catalog results