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Items: 46

1.

Cardiac Safety of Ozanimod, a Novel Sphingosine-1-Phosphate Receptor Modulator: Results of a Thorough QT/QTc Study.

Tran JQ, Hartung JP, Olson AD, Mendzelevski B, Timony GA, Boehm MF, Peach RJ, Gujrathi S, Frohna PA.

Clin Pharmacol Drug Dev. 2018 Mar;7(3):263-276. doi: 10.1002/cpdd.383. Epub 2017 Aug 7.

2.

Results From the First-in-Human Study With Ozanimod, a Novel, Selective Sphingosine-1-Phosphate Receptor Modulator.

Tran JQ, Hartung JP, Peach RJ, Boehm MF, Rosen H, Smith H, Brooks JL, Timony GA, Olson AD, Gujrathi S, Frohna PA.

J Clin Pharmacol. 2017 Aug;57(8):988-996. doi: 10.1002/jcph.887. Epub 2017 Apr 11.

3.

Ozanimod (RPC1063) is a potent sphingosine-1-phosphate receptor-1 (S1P1 ) and receptor-5 (S1P5 ) agonist with autoimmune disease-modifying activity.

Scott FL, Clemons B, Brooks J, Brahmachary E, Powell R, Dedman H, Desale HG, Timony GA, Martinborough E, Rosen H, Roberts E, Boehm MF, Peach RJ.

Br J Pharmacol. 2016 Jun;173(11):1778-92. doi: 10.1111/bph.13476. Epub 2016 Apr 28.

4.

EC144 is a potent inhibitor of the heat shock protein 90.

Shi J, Van de Water R, Hong K, Lamer RB, Weichert KW, Sandoval CM, Kasibhatla SR, Boehm MF, Chao J, Lundgren K, Timple N, Lough R, Ibanez G, Boykin C, Burrows FJ, Kehry MR, Yun TJ, Harning EK, Ambrose C, Thompson J, Bixler SA, Dunah A, Snodgrass-Belt P, Arndt J, Enyedy IJ, Li P, Hong VS, McKenzie A, Biamonte MA.

J Med Chem. 2012 Sep 13;55(17):7786-95. doi: 10.1021/jm300810x. Epub 2012 Aug 31.

PMID:
22938030
5.

BIIB021, an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90.

Lundgren K, Zhang H, Brekken J, Huser N, Powell RE, Timple N, Busch DJ, Neely L, Sensintaffar JL, Yang YC, McKenzie A, Friedman J, Scannevin R, Kamal A, Hong K, Kasibhatla SR, Boehm MF, Burrows FJ.

Mol Cancer Ther. 2009 Apr;8(4):921-9. doi: 10.1158/1535-7163.MCT-08-0758.

6.

Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity.

Kasibhatla SR, Hong K, Biamonte MA, Busch DJ, Karjian PL, Sensintaffar JL, Kamal A, Lough RE, Brekken J, Lundgren K, Grecko R, Timony GA, Ran Y, Mansfield R, Fritz LC, Ulm E, Burrows FJ, Boehm MF.

J Med Chem. 2007 Jun 14;50(12):2767-78. Epub 2007 May 8.

PMID:
17488003
7.

7'-substituted benzothiazolothio- and pyridinothiazolothio-purines as potent heat shock protein 90 inhibitors.

Zhang L, Fan J, Vu K, Hong K, Le Brazidec JY, Shi J, Biamonte M, Busch DJ, Lough RE, Grecko R, Ran Y, Sensintaffar JL, Kamal A, Lundgren K, Burrows FJ, Mansfield R, Timony GA, Ulm EH, Kasibhatla SR, Boehm MF.

J Med Chem. 2006 Aug 24;49(17):5352-62.

PMID:
16913725
8.

Orally active purine-based inhibitors of the heat shock protein 90.

Biamonte MA, Shi J, Hong K, Hurst DC, Zhang L, Fan J, Busch DJ, Karjian PL, Maldonado AA, Sensintaffar JL, Yang YC, Kamal A, Lough RE, Lundgren K, Burrows FJ, Timony GA, Boehm MF, Kasibhatla SR.

J Med Chem. 2006 Jan 26;49(2):817-28.

PMID:
16420067
9.

Stereoselective synthesis of the C1-C13 fragment of 2,3-dihydrodorrigocin A.

Le Brazidec JY, Gilson CA 3rd, Boehm MF.

J Org Chem. 2005 Sep 30;70(20):8212-5.

PMID:
16277352
10.

Biological characterization of a heterodimer-selective retinoid X receptor modulator: potential benefits for the treatment of type 2 diabetes.

Leibowitz MD, Ardecky RJ, Boehm MF, Broderick CL, Carfagna MA, Crombie DL, D'Arrigo J, Etgen GJ, Faul MM, Grese TA, Havel H, Hein NI, Heyman RA, Jolley D, Klausing K, Liu S, Mais DE, Mapes CM, Marschke KB, Michellys PY, Montrose-Rafizadeh C, Ogilvie KM, Pascual B, Rungta D, Tyhonas JS, Urcan MS, Wardlow M, Yumibe N, Reifel-Miller A.

Endocrinology. 2006 Feb;147(2):1044-53. Epub 2005 Nov 3.

PMID:
16269450
11.

Preparation of 8-(arylsulfanyl)adenines with diazonium salts under mild, aerobic conditions.

Biamonte MA, Shi J, Hurst D, Hong K, Boehm MF, Kasibhatla SR.

J Org Chem. 2005 Jan 21;70(2):717-20.

PMID:
15651828
12.

Synthesis and biological evaluation of a new class of geldanamycin derivatives as potent inhibitors of Hsp90.

Le Brazidec JY, Kamal A, Busch D, Thao L, Zhang L, Timony G, Grecko R, Trent K, Lough R, Salazar T, Khan S, Burrows F, Boehm MF.

J Med Chem. 2004 Jul 15;47(15):3865-73.

PMID:
15239664
13.

Therapeutic and diagnostic implications of Hsp90 activation.

Kamal A, Boehm MF, Burrows FJ.

Trends Mol Med. 2004 Jun;10(6):283-90. Review.

PMID:
15177193
14.

Design and synthesis of benzofused heterocyclic RXR modulators.

Gernert DL, Neel DA, Boehm MF, Leibowitz MD, Mais DA, Michellys PY, Rungta D, Reifel-Miller A, Grese TA.

Bioorg Med Chem Lett. 2004 Jun 7;14(11):2759-63.

PMID:
15125928
15.

Design, synthesis and structure-activity relationship of novel RXR-selective modulators.

Michellys PY, D'Arrigo J, Grese TA, Karanewsky DS, Leibowitz MD, Mais DA, Mapes CM, Reifel-Miller A, Rungta D, Boehm MF.

Bioorg Med Chem Lett. 2004 Mar 22;14(6):1593-8.

PMID:
15006411
16.

Design and synthesis of novel RXR-selective modulators with improved pharmacological profile.

Michellys PY, Boehm MF, Chen JH, Grese TA, Karanewsky DS, Leibowitz MD, Liu S, Mais DA, Mapes CM, Reifel-Miller A, Ogilvie KM, Rungta D, Thompson AW, Tyhonas JS, Yumibe N, Ardecky RJ.

Bioorg Med Chem Lett. 2003 Nov 17;13(22):4071-5.

PMID:
14592510
17.

A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors.

Kamal A, Thao L, Sensintaffar J, Zhang L, Boehm MF, Fritz LC, Burrows FJ.

Nature. 2003 Sep 25;425(6956):407-10.

18.

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.

Michellys PY, Ardecky RJ, Chen JH, D'Arrigo J, Grese TA, Karanewsky DS, Leibowitz MD, Liu S, Mais DA, Mapes CM, Montrose-Rafizadeh C, Ogilvie KM, Reifel-Miller A, Rungta D, Thompson AW, Tyhonas JS, Boehm MF.

J Med Chem. 2003 Sep 11;46(19):4087-103.

PMID:
12954061
19.

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.

Michellys PY, Ardecky RJ, Chen JH, Crombie DL, Etgen GJ, Faul MM, Faulkner AL, Grese TA, Heyman RA, Karanewsky DS, Klausing K, Leibowitz MD, Liu S, Mais DA, Mapes CM, Marschke KB, Reifel-Miller A, Ogilvie KM, Rungta D, Thompson AW, Tyhonas JS, Boehm MF.

J Med Chem. 2003 Jun 19;46(13):2683-96.

PMID:
12801232
20.

Novel nonsecosteroidal vitamin D receptor modulator inhibits the growth of LNCaP xenograft tumors in athymic mice without increased serum calcium.

Polek TC, Murthy S, Blutt SE, Boehm MF, Zou A, Weigel NL, Allegretto EA.

Prostate. 2001 Nov 1;49(3):224-33.

PMID:
11746268
21.

Engineering orthogonal ligand-receptor pairs from "near drugs".

Doyle DF, Braasch DA, Jackson LK, Weiss HE, Boehm MF, Mangelsdorf DJ, Corey DR.

J Am Chem Soc. 2001 Nov 21;123(46):11367-71.

PMID:
11707111
22.

Synthesis and Characterization of a Highly Potent and Selective Isotopically Labeled Retinoic Acid Receptor Ligand, ALRT1550.

Bennani YL, Marron KS, Mais DE, Flatten K, Nadzan AM, Boehm MF.

J Org Chem. 1998 Feb 6;63(3):543-550.

PMID:
11672043
23.

Vitamin D analogs: mechanism of action and therapeutic applications.

Nagpal S, Lu J, Boehm MF.

Curr Med Chem. 2001 Nov;8(13):1661-79. Review.

PMID:
11562285
24.

Novel nonsecosteroidal vitamin D mimics exert VDR-modulating activities with less calcium mobilization than 1,25-dihydroxyvitamin D3.

Boehm MF, Fitzgerald P, Zou A, Elgort MG, Bischoff ED, Mere L, Mais DE, Bissonnette RP, Heyman RA, Nadzan AM, Reichman M, Allegretto EA.

Chem Biol. 1999 May;6(5):265-75.

25.

Synthesis of retinoid X receptor-specific ligands that are potent inducers of adipogenesis in 3T3-L1 cells.

Canan Koch SS, Dardashti LJ, Cesario RM, Croston GE, Boehm MF, Heyman RA, Nadzan AM.

J Med Chem. 1999 Feb 25;42(4):742-50.

PMID:
10052980
26.

Synthesis and characterization of heteroarotinoids demonstrate structure specificity relationships.

Benbrook DM, Subramanian S, Gale JB, Liu S, Brown CW, Boehm MF, Berlin KD.

J Med Chem. 1998 Sep 10;41(19):3753-7.

PMID:
9733501
27.

Trypanosoma brucei: effects of methoprene and other isoprenoid compounds on procyclic and bloodstream forms in vitro and in mice.

Harmon MA, Scott TC, Li Y, Boehm MF, Phillips MA, Mangelsdorf DJ.

Exp Parasitol. 1997 Nov;87(3):229-36.

PMID:
9371088
28.

Sensitization of diabetic and obese mice to insulin by retinoid X receptor agonists.

Mukherjee R, Davies PJ, Crombie DL, Bischoff ED, Cesario RM, Jow L, Hamann LG, Boehm MF, Mondon CE, Nadzan AM, Paterniti JR Jr, Heyman RA.

Nature. 1997 Mar 27;386(6623):407-10.

PMID:
9121558
29.

A novel retinoic acid receptor-selective retinoid, ALRT1550, has potent antitumor activity against human oral squamous carcinoma xenografts in nude mice.

Shalinsky DR, Bischoff ED, Lamph WW, Zhang L, Boehm MF, Davies PJ, Nadzan AM, Heyman RA.

Cancer Res. 1997 Jan 1;57(1):162-8.

30.

Retinoid-induced hypertriglyceridemia in rats is mediated by retinoic acid receptors.

Standeven AM, Beard RL, Johnson AT, Boehm MF, Escobar M, Heyman RA, Chandraratna RA.

Fundam Appl Toxicol. 1996 Oct;33(2):264-71.

PMID:
8921345
31.

Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells.

Zhang L, Nadzan AM, Heyman RA, Love DL, Mais DE, Croston G, Lamph WW, Boehm MF.

J Med Chem. 1996 Jul 5;39(14):2659-63.

PMID:
8709094
32.

Oxidative and reductive metabolism of 9-cis-retinoic acid in the rat. Identification of 13,14-dihydro-9-cis-retinoic acid and its taurine conjugate.

Shirley MA, Bennani YL, Boehm MF, Breau AP, Pathirana C, Ulm EH.

Drug Metab Dispos. 1996 Mar;24(3):293-302.

PMID:
8820419
33.

Retinoid X receptor acts as a hormone receptor in vivo to induce a key metabolic enzyme for 1,25-dihydroxyvitamin D3.

Allegretto EA, Shevde N, Zou A, Howell SR, Boehm MF, Hollis BW, Pike JW.

J Biol Chem. 1995 Oct 13;270(41):23906-9.

34.
35.

Photoaffinity labeling of rhodopsin and bacteriorhodopsin.

Nakanishi K, Zhang H, Lerro KA, Takekuma S, Yamamoto T, Lien TH, Sastry L, Baek DJ, Moquin-Pattey C, Boehm MF, et al.

Biophys Chem. 1995 Sep-Oct;56(1-2):13-22. Review.

PMID:
7662862
36.

Design and synthesis of potent retinoid X receptor selective ligands that induce apoptosis in leukemia cells.

Boehm MF, Zhang L, Zhi L, McClurg MR, Berger E, Wagoner M, Mais DE, Suto CM, Davies JA, Heyman RA, et al.

J Med Chem. 1995 Aug 4;38(16):3146-55.

PMID:
7636877
37.

Activation of mammalian retinoid X receptors by the insect growth regulator methoprene.

Harmon MA, Boehm MF, Heyman RA, Mangelsdorf DJ.

Proc Natl Acad Sci U S A. 1995 Jun 20;92(13):6157-60.

39.

Synthesis and structure-activity relationships of novel retinoid X receptor-selective retinoids.

Boehm MF, Zhang L, Badea BA, White SK, Mais DE, Berger E, Suto CM, Goldman ME, Heyman RA.

J Med Chem. 1994 Sep 2;37(18):2930-41.

PMID:
8071941
40.

Synthesis of high specific activity [3H]-9-cis-retinoic acid and its application for identifying retinoids with unusual binding properties.

Boehm MF, McClurg MR, Pathirana C, Mangelsdorf D, White SK, Hebert J, Winn D, Goldman ME, Heyman RA.

J Med Chem. 1994 Feb 4;37(3):408-14.

PMID:
8308867
41.

Transactivation properties of retinoic acid and retinoid X receptors in mammalian cells and yeast. Correlation with hormone binding and effects of metabolism.

Allegretto EA, McClurg MR, Lazarchik SB, Clemm DL, Kerner SA, Elgort MG, Boehm MF, White SK, Pike JW, Heyman RA.

J Biol Chem. 1993 Dec 15;268(35):26625-33. Erratum in: J Biol Chem 1994 Mar 11;269(10):7834.

42.

Cloning and expression of goldfish opsin sequences.

Johnson RL, Grant KB, Zankel TC, Boehm MF, Merbs SL, Nathans J, Nakanishi K.

Biochemistry. 1993 Jan 12;32(1):208-14.

PMID:
8418840
43.

Juvenile hormone receptors in insect larval epidermis: identification by photoaffinity labeling.

Palli SR, Osir EO, Eng W, Boehm MF, Edwards M, Kulcsar P, Ujvary I, Hiruma K, Prestwich GD, Riddiford LM.

Proc Natl Acad Sci U S A. 1990 Jan;87(2):796-800.

44.
45.
46.

Investigations of in vivo methionine racemization in mammalian tissues.

Boehm MF, Bada JL.

Biochem Int. 1984 May;8(5):603-8.

PMID:
6477622

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