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Page 1
Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist.
Palucki BL, Park MK, Nargund RP, Ye Z, Sebhat IK, Pollard PG, Kalyani RN, Tang R, Macneil T, Weinberg DH, Vongs A, Rosenblum CI, Doss GA, Miller RR, Stearns RA, Peng Q, Tamvakopoulos C, McGowan E, Martin WJ, Metzger JM, Shepherd CA, Strack AM, Macintyre DE, Van der Ploeg LH, Patchett AA. Palucki BL, et al. Among authors: vongs a. Bioorg Med Chem Lett. 2005 Jan 3;15(1):171-5. doi: 10.1016/j.bmcl.2004.10.020. Bioorg Med Chem Lett. 2005. PMID: 15582434
2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists.
Palucki BL, Park MK, Nargund RP, Tang R, MacNeil T, Weinberg DH, Vongs A, Rosenblum CI, Doss GA, Miller RR, Stearns RA, Peng Q, Tamvakopoulos C, Van der Ploeg LH, Patchett AA. Palucki BL, et al. Among authors: vongs a. Bioorg Med Chem Lett. 2005 Apr 15;15(8):1993-6. doi: 10.1016/j.bmcl.2005.02.068. Bioorg Med Chem Lett. 2005. PMID: 15808454
Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist.
Ye Z, Guo L, Barakat KJ, Pollard PG, Palucki BL, Sebhat IK, Bakshi RK, Tang R, Kalyani RN, Vongs A, Chen AS, Chen HY, Rosenblum CI, MacNeil T, Weinberg DH, Peng Q, Tamvakopoulos C, Miller RR, Stearns RA, Cashen DE, Martin WJ, Metzger JM, Strack AM, MacIntyre DE, Van der Ploeg LH, Patchett AA, Wyvratt MJ, Nargund RP. Ye Z, et al. Among authors: vongs a. Bioorg Med Chem Lett. 2005 Aug 1;15(15):3501-5. doi: 10.1016/j.bmcl.2005.05.109. Bioorg Med Chem Lett. 2005. PMID: 15982875
Melanocortin subtype 4 receptor agonists: structure-activity relationships about the 4-alkyl piperidine core.
Sebhat IK, Lai Y, Barakat K, Ye Z, Tang R, Kalyani RN, Vongs A, Macneil T, Weinberg DH, Cabello MA, Maroto M, Teran A, Fong TM, Van der Ploeg LH, Patchett AA, Nargund RP. Sebhat IK, et al. Among authors: vongs a. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5720-3. doi: 10.1016/j.bmcl.2006.11.084. Epub 2006 Dec 3. Bioorg Med Chem Lett. 2007. PMID: 17768046
Optimization of privileged structures for selective and potent melanocortin subtype-4 receptor ligands.
Hong Q, Bakshi RK, Dellureficio J, He S, Ye Z, Dobbelaar PH, Sebhat IK, Guo L, Liu J, Jian T, Tang R, Kalyani RN, Macneil T, Vongs A, Rosenblum CI, Weinberg DH, Peng Q, Tamvakopoulos C, Miller RR, Stearns RA, Cashen D, Martin WJ, Chen AS, Metzger JM, Chen HY, Strack AM, Fong TM, Maclntyre E, Van der Ploeg LH, Wyvratt MJ, Nargund RP. Hong Q, et al. Among authors: vongs a. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4483-6. doi: 10.1016/j.bmcl.2010.06.038. Epub 2010 Jun 10. Bioorg Med Chem Lett. 2010. PMID: 20598533
A role for the melanocortin 4 receptor in sexual function.
Van der Ploeg LH, Martin WJ, Howard AD, Nargund RP, Austin CP, Guan X, Drisko J, Cashen D, Sebhat I, Patchett AA, Figueroa DJ, DiLella AG, Connolly BM, Weinberg DH, Tan CP, Palyha OC, Pong SS, MacNeil T, Rosenblum C, Vongs A, Tang R, Yu H, Sailer AW, Fong TM, Huang C, Tota MR, Chang RS, Stearns R, Tamvakopoulos C, Christ G, Drazen DL, Spar BD, Nelson RJ, MacIntyre DE. Van der Ploeg LH, et al. Among authors: vongs a. Proc Natl Acad Sci U S A. 2002 Aug 20;99(17):11381-6. doi: 10.1073/pnas.172378699. Epub 2002 Aug 9. Proc Natl Acad Sci U S A. 2002. PMID: 12172010 Free PMC article.
Inactivation of the mouse melanocortin-3 receptor results in increased fat mass and reduced lean body mass.
Chen AS, Marsh DJ, Trumbauer ME, Frazier EG, Guan XM, Yu H, Rosenblum CI, Vongs A, Feng Y, Cao L, Metzger JM, Strack AM, Camacho RE, Mellin TN, Nunes CN, Min W, Fisher J, Gopal-Truter S, MacIntyre DE, Chen HY, Van der Ploeg LH. Chen AS, et al. Among authors: vongs a. Nat Genet. 2000 Sep;26(1):97-102. doi: 10.1038/79254. Nat Genet. 2000. PMID: 10973258
Production of leptin in Escherichia coli: a comparison of methods.
Varnerin JP, Smith T, Rosenblum CI, Vongs A, Murphy BA, Nunes C, Mellin TN, King JJ, Burgess BW, Junker B, Chou M, Hey P, Frazier E, MacIntyre DE, Van der Ploeg LH, Tota MR. Varnerin JP, et al. Among authors: vongs a. Protein Expr Purif. 1998 Dec;14(3):335-42. doi: 10.1006/prep.1998.0978. Protein Expr Purif. 1998. PMID: 9882567
16 results