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Timothy Grese

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Michael G Bell; Douglas Gernert; Timothy Grese; Matthew D Belvo; Peter S Borromeo; Sally A Kelley; joseph kennedy; Stanley P Kolis; Peter A Lander; Rachel Richey; V Scott Sharp; Gregory A Stephenson; Jeffrey D Williams; Hannah Yu; Karen M Zimmerman; Mitchell I Steinberg; Prabhakar K Jadhav
(S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor.
Rieko Tanaka; Almudena Rubio; Nancy K Harn; Douglas Gernert; Timothy Grese; Jun Eishima; Mitsunobu Hara; Nobuyuki Yoda; Rui Ohashi; Takashi Kuwabara; Shiro Soga; Shiro Akinaga; Shinji Nara; Yutaka Kanda
Design and synthesis of piperidine farnesyltransferase inhibitors with reduced glucuronidation potential.
Mark D Leibowitz; Robert J Ardecky; Marcus F Boehm; Carol L Broderick; Mark A Carfagna; Diane L Crombie; Jennifer D'Arrigo; Garret J Etgen; Margaret M Faul; Timothy Grese; Henry Havel; Nancy I Hein; Richard A Heyman; Diane Jolley; Kay Klausing; Sha Liu; Dale E Mais; Christopher M Mapes; Keith B Marschke; Pierre-Yves Michellys; Chahrzad Montrose-Rafizadeh; Kathleen M Ogilvie; Bernadette Pascual; Deepa Rungta; John S Tyhonas; Mary S Urcan; Marilyn Wardlow; Nathan Yumibe; Anne Reifel-Miller
Biological characterization of a heterodimer-selective retinoid X receptor modulator: potential benefits for the treatment of type 2 diabetes.

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All Publications

2007: Michael G Bell; Douglas Gernert; Timothy Grese; Matthew D Belvo; Peter S Borromeo; Sally A Kelley; joseph kennedy; Stanley P Kolis; Peter A Lander; Rachel Richey; V Scott Sharp; Gregory A Stephenson; Jeffrey D Williams; Hannah Yu; Karen M Zimmerman; Mitchell I Steinberg; Prabhakar K Jadhav
(S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor.
Journal of medicinal chemistry 2007;50(26):6443-5.
2007: Rieko Tanaka; Almudena Rubio; Nancy K Harn; Douglas Gernert; Timothy Grese; Jun Eishima; Mitsunobu Hara; Nobuyuki Yoda; Rui Ohashi; Takashi Kuwabara; Shiro Soga; Shiro Akinaga; Shinji Nara; Yutaka Kanda
Design and synthesis of piperidine farnesyltransferase inhibitors with reduced glucuronidation potential.
Bioorganic & medicinal chemistry 2007;15(3):1363-82.
2006: Mark D Leibowitz; Robert J Ardecky; Marcus F Boehm; Carol L Broderick; Mark A Carfagna; Diane L Crombie; Jennifer D'Arrigo; Garret J Etgen; Margaret M Faul; Timothy Grese; Henry Havel; Nancy I Hein; Richard A Heyman; Diane Jolley; Kay Klausing; Sha Liu; Dale E Mais; Christopher M Mapes; Keith B Marschke; Pierre-Yves Michellys; Chahrzad Montrose-Rafizadeh; Kathleen M Ogilvie; Bernadette Pascual; Deepa Rungta; John S Tyhonas; Mary S Urcan; Marilyn Wardlow; Nathan Yumibe; Anne Reifel-Miller
Biological characterization of a heterodimer-selective retinoid X receptor modulator: potential benefits for the treatment of type 2 diabetes.
Endocrinology 2006;147(2):1044-53.
2005: David A Neel; Matthew L Brown; Peter A Lander; Timothy Grese; Jean M Defauw; Robert A Doti; Todd Fields; Sally Ann Kelley; Stephon Smith; Karen M Zimmerman; Mitchell I Steinberg; Prabhakar K Jadhav
3,3-Bisaryloxindoles as mineralocorticoid receptor antagonists.
Bioorganic & medicinal chemistry letters 2005;15(10):2553-7.
2005: Leah M Helvering; Mary D Adrian; Andrew G Geiser; Shawn T Estrem; Tao Wei; Shuguang Huang; Peining Chen; Ernst Dow; J N Calley; Jeffrey A Dodge; Timothy Grese; Scott A Jones; David L Halladay; Rebecca R Miles; Jude E Onyia; Yanfei L Ma; Masahiko Sato; Henry Bryant
Differential effects of estrogen and raloxifene on messenger RNA and matrix metalloproteinase 2 activity in the rat uterus.
Biology of reproduction 2005;72(4):830-41.
2004: Douglas Gernert; David A Neel; Marcus F Boehm; Mark D Leibowitz; Dale A Mais; Pierre-Yves Michellys; Deepa Rungta; Anne Reifel-Miller; Timothy Grese
Design and synthesis of benzofused heterocyclic RXR modulators.
Bioorganic & medicinal chemistry letters 2004;14(11):2759-63.
2004: Pierre-Yves Michellys; Jennifer D'Arrigo; Timothy Grese; Donald S Karanewsky; Mark D Leibowitz; Dale A Mais; Christopher M Mapes; Anne Reifel-Miller; Deepa Rungta; Marcus F Boehm
Design, synthesis and structure-activity relationship of novel RXR-selective modulators.
Bioorganic & medicinal chemistry letters 2004;14(6):1593-8.
2003: Pierre-Yves Michellys; Marcus F Boehm; Jyun-Hung Chen; Timothy Grese; Donald S Karanewsky; Mark D Leibowitz; Sha Liu; Dale A Mais; Christopher M Mapes; Anne Reifel-Miller; Kathleen M Ogilvie; Deepa Rungta; Anthony W Thompson; John S Tyhonas; Nathan Yumibe; Robert J Ardecky
Design and synthesis of novel RXR-selective modulators with improved pharmacological profile.
Bioorganic & medicinal chemistry letters 2003;13(22):4071-5.
2003: Douglas Gernert; R Ajamie; R A Ardecky; Michael G Bell; Mark D Leibowitz; Dale A Mais; Christopher M Mapes; Pierre-Yves Michellys; Deepa Rungta; Anne Reifel-Miller; John S Tyhonas; Nathan Yumibe; Timothy Grese
Design and synthesis of fluorinated RXR modulators.
Bioorganic & medicinal chemistry letters 2003;13(19):3191-5.
2003: Pierre-Yves Michellys; Robert J Ardecky; Jyun-Hung Chen; Jennifer D'Arrigo; Timothy Grese; Donald S Karanewsky; Mark D Leibowitz; Sha Liu; Dale A Mais; Christopher M Mapes; Chahrzad Montrose-Rafizadeh; Kathleen M Ogilvie; Anne Reifel-Miller; Deepa Rungta; Anthony W Thompson; John S Tyhonas; Marcus F Boehm
Design, synthesis, and structure-activity relationship studies of novel 6,7-locked-[7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta]-2,4,6-trienoic acids.
Journal of medicinal chemistry 2003;46(19):4087-103.
2003: Pierre-Yves Michellys; Robert J Ardecky; Jyun-Hung Chen; Diane L Crombie; Garret J Etgen; Margaret M Faul; A L Faulkner; Timothy Grese; Richard A Heyman; Donald S Karanewsky; Kay Klausing; Mark D Leibowitz; Sha Liu; Dale A Mais; Christopher M Mapes; Keith B Marschke; Anne Reifel-Miller; Kathleen M Ogilvie; Deepa Rungta; Anthony W Thompson; John S Tyhonas; Marcus F Boehm
Novel (2E,4E,6Z)-7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta-2,4,6-trienoic acid retinoid X receptor modulators are active in models of type 2 diabetes.
Journal of medicinal chemistry 2003;46(13):2683-96.
2003: Jeffrey Thomas; Kelli S Bramlett; Chahrzad Montrose; Patricia Foxworthy; Patrick I Eacho; Denis McCann; Guoqing Cao; Anton Kiefer; Jeff McCowan; Kuo-Long Yu; Timothy Grese; William W Chin; Burris thomas; Laura F Michael
A chemical switch regulates fibrate specificity for peroxisome proliferator-activated receptor alpha (PPARalpha ) versus liver X receptor.
The Journal of biological chemistry 2003;278(4):2403-10.
2002: Margaret M Faul; Timothy Grese
Selective RXR modulators for the treatment of type II diabetes.
Current opinion in drug discovery & development 2002;5(6):974-85.
2002: Nanjoo Suh; William W Lamph; Andrew Glasebrook; Timothy Grese; Alan D Palkowitz; Charlotte R Williams; Renee Risingsong; M Rendi Farris; Richard A Heyman; Michael B. Sporn
Prevention and treatment of experimental breast cancer with the combination of a new selective estrogen receptor modulator, arzoxifene, and a new rexinoid, LG 100268.
Clinical cancer research : an official journal of the American Association for Cancer Research 2002;8(10):3270-5.
2001: Timothy Grese; Mary D Adrian; DL Phillips; Pamela K Shetler; LL Short; Andrew Glasebrook; Henry Bryant
Photochemical synthesis of N-arylbenzophenanthridine selective estrogen receptor modulators (serms).
Journal of medicinal chemistry 2001;44(17):2857-60.
2001: SR Howell; MA Shirley; Timothy Grese; David A Neel; K E Wells; E H Ulm
Bexarotene metabolism in rat, dog, and human, synthesis of oxidative metabolites, and in vitro activity at retinoid receptors.
Drug metabolism and disposition: the biological fate of chemicals 2001;29(7):990-8.
1999: Masahiko Sato; Timothy Grese; Jeffrey A Dodge; Henry Bryant; C H Turner
Emerging therapies for the prevention or treatment of postmenopausal osteoporosis.
Journal of medicinal chemistry 1999;42(1):1-24.
1998: Timothy Grese; L D Pennington; James Sluka; Mary D Adrian; Harlan W Cole; Tina Fuson; David Magee; DL Phillips; ER Rowley; Pamela K Shetler; LL Short; M Venugopalan; NN Yang; Masahiko Sato; Andrew Glasebrook; Henry Bryant
Synthesis and pharmacology of conformationally restricted raloxifene analogues: highly potent selective estrogen receptor modulators.
Journal of medicinal chemistry 1998;41(8):1272-83.
1998: Timothy Grese; Jeffrey A Dodge
Selective estrogen receptor modulators (SERMs).
Current pharmaceutical design 1998;4(1):71-92.
1997: Timothy Grese; James Sluka; Henry Bryant; GJ Cullinan; Andrew Glasebrook; C D Jones; K Matsumoto; Alan D Palkowitz; Masahiko Sato; J D Termine; Mark A Winter; NN Yang; Jeffrey A Dodge
Molecular determinants of tissue selectivity in estrogen receptor modulators.
Proceedings of the National Academy of Sciences of the United States of America 1997;94(25):14105-10.
1997: Timothy Grese; S Cho; Don R Finley; A G Godfrey; C D Jones; Charles W Lugar; M J Martin; K Matsumoto; L D Pennington; Mark A Winter; Mary D Adrian; Harlan W Cole; David Magee; DL Phillips; ER Rowley; LL Short; Andrew Glasebrook; Henry Bryant
Structure-activity relationships of selective estrogen receptor modulators: modifications to the 2-arylbenzothiophene core of raloxifene.
Journal of medicinal chemistry 1997;40(2):146-67.