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Items: 1 to 50 of 65

1.

Discovery of small molecule splicing modulators of survival motor neuron-2 (SMN2) for the treatment of Spinal Muscular Atrophy (SMA).

Cheung AK, Hurley B, Kerrigan R, Shu L, Chin DN, Shen Y, O'Brien G, Sung MJ, Hou Y, Axford J, Cody E, Sun R, Fazal A, Tomlinson RC, Jain M, Deng L, Hoffmaster K, Song C, Van Hoosear M, Shin Y, Servais R, Towler CS, Hild M, Curtis D, Dietrich WF, Hamann LG, Briner K, Chen KS, Kobayashi D, Sivasankaran R, Dales NA.

J Med Chem. 2018 Nov 8. doi: 10.1021/acs.jmedchem.8b01291. [Epub ahead of print]

PMID:
30407821
2.

SALL4 mediates teratogenicity as a thalidomide-dependent cereblon substrate.

Matyskiela ME, Couto S, Zheng X, Lu G, Hui J, Stamp K, Drew C, Ren Y, Wang M, Carpenter A, Lee CW, Clayton T, Fang W, Lu CC, Riley M, Abdubek P, Blease K, Hartke J, Kumar G, Vessey R, Rolfe M, Hamann LG, Chamberlain PP.

Nat Chem Biol. 2018 Oct;14(10):981-987. doi: 10.1038/s41589-018-0129-x. Epub 2018 Sep 6.

PMID:
30190590
3.

Discovery of 1-((6-Aminopyridin-3-yl)Methyl)-3-(4-Bromophenyl)Urea as a Potent, Irreversible Myeloperoxidase Inhibitor.

Marro ML, Patterson AW, Lee L, Deng L, Reynolds A, Ren X, Axford L, Patnaik A, Hollis-Symynkywicz M, Casson N, Custeau D, Ames L, Loi S, Zhang L, Honda T, Blank J, Harrison TJ, Papillon JPN, Hamann LG, Marcinkeviciene J, Regard JB.

J Pharmacol Exp Ther. 2018 Oct;367(1):147-154. doi: 10.1124/jpet.118.248435. Epub 2018 Aug 3.

PMID:
30076263
4.

Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.

Tria GS, Abrams T, Baird J, Burks HE, Firestone B, Gaither LA, Hamann LG, He G, Kirby CA, Kim S, Lombardo F, Macchi KJ, McDonnell DP, Mishina Y, Norris JD, Nunez J, Springer C, Sun Y, Thomsen NM, Wang C, Wang J, Yu B, Tiong-Yip CL, Peukert S.

J Med Chem. 2018 Apr 12;61(7):2837-2864. doi: 10.1021/acs.jmedchem.7b01682. Epub 2018 Mar 22.

PMID:
29562737
5.

Design, Synthesis, and Properties of a Potent Inhibitor of Pseudomonas aeruginosa Deacetylase LpxC.

Piizzi G, Parker DT, Peng Y, Dobler M, Patnaik A, Wattanasin S, Liu E, Lenoir F, Nunez J, Kerrigan J, McKenney D, Osborne C, Yu D, Lanieri L, Bojkovic J, Dzink-Fox J, Lilly MD, Sprague ER, Lu Y, Wang H, Ranjitkar S, Xie L, Wang B, Glick M, Hamann LG, Tommasi R, Yang X, Dean CR.

J Med Chem. 2017 Jun 22;60(12):5002-5014. doi: 10.1021/acs.jmedchem.7b00377. Epub 2017 Jun 9.

PMID:
28549219
6.

Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer.

Burks HE, Abrams T, Kirby CA, Baird J, Fekete A, Hamann LG, Kim S, Lombardo F, Loo A, Lubicka D, Macchi K, McDonnell DP, Mishina Y, Norris JD, Nunez J, Saran C, Sun Y, Thomsen NM, Wang C, Wang J, Peukert S.

J Med Chem. 2017 Apr 13;60(7):2790-2818. doi: 10.1021/acs.jmedchem.6b01468. Epub 2017 Mar 15.

PMID:
28296398
7.

Accessing Drug Metabolites via Transition-Metal Catalyzed C-H Oxidation: The Liver as Synthetic Inspiration.

Genovino J, Sames D, Hamann LG, Touré BB.

Angew Chem Int Ed Engl. 2016 Nov 7;55(46):14218-14238. doi: 10.1002/anie.201602644. Epub 2016 Oct 10. Review.

PMID:
27723189
8.

Biotransformation of Daclatasvir In Vitro and in Nonclinical Species: Formation of the Main Metabolite by Pyrrolidine δ-Oxidation and Rearrangement.

Li W, Zhao W, Liu X, Huang X, Lopez OD, Leet JE, Fancher RM, Nguyen V, Goodrich J, Easter J, Hong Y, Caceres-Cortes J, Chang SY, Ma L, Belema M, Hamann LG, Gao M, Zhu M, Shu YZ, Humphreys WG, Johnson BM.

Drug Metab Dispos. 2016 Jun;44(6):809-20. doi: 10.1124/dmd.115.068866. Epub 2016 Mar 30.

PMID:
27029743
9.

Corrigendum: SMN2 splice modulators enhance U1-pre-mRNA association and rescue SMA mice.

Palacino J, Swalley SE, Song C, Cheung AK, Shu L, Zhang X, Van Hoosear M, Shin Y, Chin DN, Keller CG, Beibel M, Renaud NA, Smith TM, Salcius M, Shi X, Hild M, Servais R, Jain M, Deng L, Bullock C, McLellan M, Schuierer S, Murphy L, Blommers MJ, Blaustein C, Berenshteyn F, Lacoste A, Thomas JR, Roma G, Michaud GA, Tseng BS, Porter JA, Myer VE, Tallarico JA, Hamann LG, Curtis D, Fishman MC, Dietrich WF, Dales NA, Sivasankaran R.

Nat Chem Biol. 2016 Apr;12(4):304. doi: 10.1038/nchembio0416-304c. No abstract available.

PMID:
26991088
10.

Potent, Selective, and Orally Bioavailable Inhibitors of VPS34 Provide Chemical Tools to Modulate Autophagy in Vivo.

Honda A, Harrington E, Cornella-Taracido I, Furet P, Knapp MS, Glick M, Triantafellow E, Dowdle WE, Wiedershain D, Maniara W, Moore C, Finan PM, Hamann LG, Firestone B, Murphy LO, Keaney EP.

ACS Med Chem Lett. 2015 Nov 13;7(1):72-6. doi: 10.1021/acsmedchemlett.5b00335. eCollection 2016 Jan 14.

11.

Inhibitors of HIV-1 attachment: The discovery and structure-activity relationships of tetrahydroisoquinolines as replacements for the piperazine benzamide in the 3-glyoxylyl 6-azaindole pharmacophore.

Swidorski JJ, Liu Z, Yin Z, Wang T, Carini DJ, Rahematpura S, Zheng M, Johnson K, Zhang S, Lin PF, Parker DD, Li W, Meanwell NA, Hamann LG, Regueiro-Ren A.

Bioorg Med Chem Lett. 2016 Jan 1;26(1):160-7. doi: 10.1016/j.bmcl.2015.11.009. Epub 2015 Nov 5.

PMID:
26584882
12.

Corrigendum: SMN2 splice modulators enhance U1-pre-mRNA association and rescue SMA mice.

Palacino J, Swalley SE, Song C, Cheung AK, Shu L, Zhang X, Van Hoosear M, Shin Y, Chin DN, Keller CG, Beibel M, Renaud NA, Smith TM, Salcius M, Shi X, Hild M, Servais R, Jain M, Deng L, Bullock C, McLellan M, Schuierer S, Murphy L, Blommers MJ, Blaustein C, Berenshteyn F, Lacoste A, Thomas JR, Roma G, Michaud GA, Tseng BS, Porter JA, Myer VE, Tallarico JA, Hamann LG, Curtis D, Fishman MC, Dietrich WF, Dales NA, Sivasankaran R.

Nat Chem Biol. 2015 Sep;11(9):741. doi: 10.1038/nchembio0915-741a. No abstract available.

PMID:
26284678
13.

SMN2 splice modulators enhance U1-pre-mRNA association and rescue SMA mice.

Palacino J, Swalley SE, Song C, Cheung AK, Shu L, Zhang X, Van Hoosear M, Shin Y, Chin DN, Keller CG, Beibel M, Renaud NA, Smith TM, Salcius M, Shi X, Hild M, Servais R, Jain M, Deng L, Bullock C, McLellan M, Schuierer S, Murphy L, Blommers MJ, Blaustein C, Berenshteyn F, Lacoste A, Thomas JR, Roma G, Michaud GA, Tseng BS, Porter JA, Myer VE, Tallarico JA, Hamann LG, Curtis D, Fishman MC, Dietrich WF, Dales NA, Sivasankaran R.

Nat Chem Biol. 2015 Jul;11(7):511-7. doi: 10.1038/nchembio.1837. Epub 2015 Jun 1. Erratum in: Nat Chem Biol. 2016 Apr;12(4):304. Nat Chem Biol. 2015 Sep;11(9):741.

PMID:
26030728
14.

Non-Directed Allylic C-H Acetoxylation in the Presence of Lewis Basic Heterocycles.

Malik HA, Taylor BL, Kerrigan JR, Grob JE, Houk KN, Du Bois J, Hamann LG, Patterson AW.

Chem Sci. 2014 Jun 1;5(6):2352-2361.

15.

Late-stage C-H functionalization of complex alkaloids and drug molecules via intermolecular rhodium-carbenoid insertion.

He J, Hamann LG, Davies HM, Beckwith RE.

Nat Commun. 2015 Jan 12;6:5943. doi: 10.1038/ncomms6943.

PMID:
25581471
16.

Selective VPS34 inhibitor blocks autophagy and uncovers a role for NCOA4 in ferritin degradation and iron homeostasis in vivo.

Dowdle WE, Nyfeler B, Nagel J, Elling RA, Liu S, Triantafellow E, Menon S, Wang Z, Honda A, Pardee G, Cantwell J, Luu C, Cornella-Taracido I, Harrington E, Fekkes P, Lei H, Fang Q, Digan ME, Burdick D, Powers AF, Helliwell SB, D'Aquin S, Bastien J, Wang H, Wiederschain D, Kuerth J, Bergman P, Schwalb D, Thomas J, Ugwonali S, Harbinski F, Tallarico J, Wilson CJ, Myer VE, Porter JA, Bussiere DE, Finan PM, Labow MA, Mao X, Hamann LG, Manning BD, Valdez RA, Nicholson T, Schirle M, Knapp MS, Keaney EP, Murphy LO.

Nat Cell Biol. 2014 Nov;16(11):1069-79. doi: 10.1038/ncb3053. Epub 2014 Oct 19.

PMID:
25327288
17.

Discovery of pyridyl sulfonamide 11-beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors for the treatment of metabolic disorders.

Yoon DS, Wu SC, Seethala R, Golla R, Nayeem A, Everlof JG, Gordon DA, Hamann LG, Robl JA.

Bioorg Med Chem Lett. 2014 Nov 1;24(21):5045-9. doi: 10.1016/j.bmcl.2014.09.012. Epub 2014 Sep 16.

PMID:
25266782
18.

2-Alkyloxazoles as potent and selective PI4KIIIβ inhibitors demonstrating inhibition of HCV replication.

Keaney EP, Connolly M, Dobler M, Karki R, Honda A, Sokup S, Karur S, Britt S, Patnaik A, Raman P, Hamann LG, Wiedmann B, LaMarche MJ.

Bioorg Med Chem Lett. 2014 Aug 15;24(16):3714-8. doi: 10.1016/j.bmcl.2014.07.015. Epub 2014 Jul 12.

PMID:
25065492
19.

Synthetic strategy: natural products on demand.

Hamann LG.

Nat Chem. 2014 Jun;6(6):460-1. doi: 10.1038/nchem.1964. No abstract available.

PMID:
24848226
20.

Hepatitis C virus NS5A replication complex inhibitors: the discovery of daclatasvir.

Belema M, Nguyen VN, Bachand C, Deon DH, Goodrich JT, James CA, Lavoie R, Lopez OD, Martel A, Romine JL, Ruediger EH, Snyder LB, St Laurent DR, Yang F, Zhu J, Wong HS, Langley DR, Adams SP, Cantor GH, Chimalakonda A, Fura A, Johnson BM, Knipe JO, Parker DD, Santone KS, Fridell RA, Lemm JA, O'Boyle DR 2nd, Colonno RJ, Gao M, Meanwell NA, Hamann LG.

J Med Chem. 2014 Mar 13;57(5):2013-32. doi: 10.1021/jm401836p. Epub 2014 Feb 12.

PMID:
24521299
21.

Optimization of activity, selectivity, and liability profiles in 5-oxopyrrolopyridine DPP4 inhibitors leading to clinical candidate (Sa)-2-(3-(aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b]pyridin-6(7H)-yl)-N,N-dimethylacetamide (BMS-767778).

Devasthale P, Wang Y, Wang W, Fevig J, Feng J, Wang A, Harrity T, Egan D, Morgan N, Cap M, Fura A, Klei HE, Kish K, Weigelt C, Sun L, Levesque P, Moulin F, Li YX, Zahler R, Kirby MS, Hamann LG.

J Med Chem. 2013 Sep 26;56(18):7343-57. doi: 10.1021/jm4008906. Epub 2013 Sep 9.

PMID:
23964740
22.

Sustainable practices in medicinal chemistry: current state and future directions.

Bryan MC, Dillon B, Hamann LG, Hughes GJ, Kopach ME, Peterson EA, Pourashraf M, Raheem I, Richardson P, Richter D, Sneddon HF.

J Med Chem. 2013 Aug 8;56(15):6007-21. doi: 10.1021/jm400250p. Epub 2013 May 9. Review.

PMID:
23586692
23.

Substituted piperidinyl glycinyl 2-cyano-4,5-methano pyrrolidines as potent and stable dipeptidyl peptidase IV inhibitors.

Zhao G, Kwon C, Wang A, Robertson JG, Marcinkeviciene J, Parker RA, Kirby MS, Hamann LG.

Bioorg Med Chem Lett. 2013 Mar 15;23(6):1622-5. doi: 10.1016/j.bmcl.2013.01.104. Epub 2013 Jan 31.

PMID:
23416006
24.

One-pot C-N/C-C cross-coupling of methyliminodiacetic acid boronyl arenes enabled by protective enolization.

Grob JE, Dechantsreiter MA, Tichkule RB, Connolly MK, Honda A, Tomlinson RC, Hamann LG.

Org Lett. 2012 Nov 2;14(21):5578-81. doi: 10.1021/ol302702q. Epub 2012 Oct 23.

PMID:
23092156
25.

Regioselective synthesis and slow-release Suzuki-Miyaura cross-coupling of MIDA boronate-functionalized isoxazoles and triazoles.

Grob JE, Nunez J, Dechantsreiter MA, Hamann LG.

J Org Chem. 2011 Dec 16;76(24):10241-8. doi: 10.1021/jo201973t. Epub 2011 Nov 29.

PMID:
22047083
26.

7-Oxopyrrolopyridine-derived DPP4 inhibitors-mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site.

Wang W, Devasthale P, Wang A, Harrity T, Egan D, Morgan N, Cap M, Fura A, Klei HE, Kish K, Weigelt C, Sun L, Levesque P, Li YX, Zahler R, Kirby MS, Hamann LG.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6646-51. doi: 10.1016/j.bmcl.2011.09.074. Epub 2011 Sep 24.

PMID:
21996520
27.

The effects of NS5A inhibitors on NS5A phosphorylation, polyprotein processing and localization.

Qiu D, Lemm JA, O'Boyle DR 2nd, Sun JH, Nower PT, Nguyen V, Hamann LG, Snyder LB, Deon DH, Ruediger E, Meanwell NA, Belema M, Gao M, Fridell RA.

J Gen Virol. 2011 Nov;92(Pt 11):2502-11. doi: 10.1099/vir.0.034801-0. Epub 2011 Jul 27.

PMID:
21795470
28.

Generation of 3,8-substituted 1,2,4-triazolopyridines as potent inhibitors of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1).

Wang H, Robl JA, Hamann LG, Simpkins L, Golla R, Li YX, Seethala R, Zvyaga T, Gordon DA, Li JJ.

Bioorg Med Chem Lett. 2011 Jul 15;21(14):4146-9. doi: 10.1016/j.bmcl.2011.05.101.

PMID:
21689935
29.

One-pot reductive amination and Suzuki-Miyaura cross-coupling of formyl aryl and heteroaryl MIDA boronates in array format.

Grob JE, Nunez J, Dechantsreiter MA, Hamann LG.

J Org Chem. 2011 Jun 17;76(12):4930-40. doi: 10.1021/jo2005928. Epub 2011 May 19.

PMID:
21526832
30.

Synthesis, SAR, and atropisomerism of imidazolopyrimidine DPP4 inhibitors.

O'Connor SP, Wang Y, Simpkins LM, Brigance RP, Meng W, Wang A, Kirby MS, Weigelt CA, Hamann LG.

Bioorg Med Chem Lett. 2010 Nov 1;20(21):6273-6. doi: 10.1016/j.bmcl.2010.08.090. Epub 2010 Aug 22.

PMID:
20833042
31.

Discovery of 6-(aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as potent, selective dipeptidyl peptidase-4 (DPP4) inhibitors.

Meng W, Brigance RP, Chao HJ, Fura A, Harrity T, Marcinkeviciene J, O'Connor SP, Tamura JK, Xie D, Zhang Y, Klei HE, Kish K, Weigelt CA, Turdi H, Wang A, Zahler R, Kirby MS, Hamann LG.

J Med Chem. 2010 Aug 12;53(15):5620-8. doi: 10.1021/jm100634a.

PMID:
20684603
32.

Synthesis and SAR of azolopyrimidines as potent and selective dipeptidyl peptidase-4 (DPP4) inhibitors for type 2 diabetes.

Brigance RP, Meng W, Fura A, Harrity T, Wang A, Zahler R, Kirby MS, Hamann LG.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4395-8. doi: 10.1016/j.bmcl.2010.06.063. Epub 2010 Jun 15.

PMID:
20598534
33.

Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect.

Gao M, Nettles RE, Belema M, Snyder LB, Nguyen VN, Fridell RA, Serrano-Wu MH, Langley DR, Sun JH, O'Boyle DR 2nd, Lemm JA, Wang C, Knipe JO, Chien C, Colonno RJ, Grasela DM, Meanwell NA, Hamann LG.

Nature. 2010 May 6;465(7294):96-100. doi: 10.1038/nature08960. Epub 2010 Apr 21.

PMID:
20410884
34.

N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation.

Nirschl AA, Zou Y, Krystek SR Jr, Sutton JC, Simpkins LM, Lupisella JA, Kuhns JE, Seethala R, Golla R, Sleph PG, Beehler BC, Grover GJ, Egan D, Fura A, Vyas VP, Li YX, Sack JS, Kish KF, An Y, Bryson JA, Gougoutas JZ, DiMarco J, Zahler R, Ostrowski J, Hamann LG.

J Med Chem. 2009 May 14;52(9):2794-8. doi: 10.1021/jm801583j.

PMID:
19351168
35.

Pharmacokinetics of the dipeptidyl peptidase 4 inhibitor saxagliptin in rats, dogs, and monkeys and clinical projections.

Fura A, Khanna A, Vyas V, Koplowitz B, Chang SY, Caporuscio C, Boulton DW, Christopher LJ, Chadwick KD, Hamann LG, Humphreys WG, Kirby M.

Drug Metab Dispos. 2009 Jun;37(6):1164-71. doi: 10.1124/dmd.108.026088. Epub 2009 Feb 27.

PMID:
19251818
36.

Pyridine amides as potent and selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.

Wang H, Ruan Z, Li JJ, Simpkins LM, Smirk RA, Wu SC, Hutchins RD, Nirschl DS, Van Kirk K, Cooper CB, Sutton JC, Ma Z, Golla R, Seethala R, Salyan ME, Nayeem A, Krystek SR Jr, Sheriff S, Camac DM, Morin PE, Carpenter B, Robl JA, Zahler R, Gordon DA, Hamann LG.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3168-72. doi: 10.1016/j.bmcl.2008.04.069. Epub 2008 May 1.

PMID:
18485702
37.

Involvement of DPP-IV catalytic residues in enzyme-saxagliptin complex formation.

Metzler WJ, Yanchunas J, Weigelt C, Kish K, Klei HE, Xie D, Zhang Y, Corbett M, Tamura JK, He B, Hamann LG, Kirby MS, Marcinkeviciene J.

Protein Sci. 2008 Feb;17(2):240-50. doi: 10.1110/ps.073253208.

38.

Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors.

Simpkins LM, Bolton S, Pi Z, Sutton JC, Kwon C, Zhao G, Magnin DR, Augeri DJ, Gungor T, Rotella DP, Sun Z, Liu Y, Slusarchyk WS, Marcinkeviciene J, Robertson JG, Wang A, Robl JA, Atwal KS, Zahler RL, Parker RA, Kirby MS, Hamann LG.

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6476-80. Epub 2007 Oct 1.

PMID:
17937986
39.

Cofactor-specific modulation of 11beta-hydroxysteroid dehydrogenase 1 inhibitor potency.

Sahni-Arya B, Flynn MJ, Bergeron L, Salyan ME, Pedicord DL, Golla R, Ma Z, Wang H, Seethala R, Wu SC, Li JJ, Nayeem A, Gates C, Hamann LG, Gordon DA, Blat Y.

Biochim Biophys Acta. 2007 Sep;1774(9):1184-91. Epub 2007 Jul 19.

PMID:
17707701
40.

Synthesis and SAR of tetrahydropyrrolo[1,2-b][1,2,5]thiadiazol-2(3H)-one 1,1-dioxide analogues as highly potent selective androgen receptor modulators.

Manfredi MC, Bi Y, Nirschl AA, Sutton JC, Seethala R, Golla R, Beehler BC, Sleph PG, Grover GJ, Ostrowski J, Hamann LG.

Bioorg Med Chem Lett. 2007 Aug 15;17(16):4487-90. Epub 2007 Jun 6.

PMID:
17574413
41.

Discovery of potent and muscle selective androgen receptor modulators through scaffold modifications.

Li JJ, Sutton JC, Nirschl A, Zou Y, Wang H, Sun C, Pi Z, Johnson R, Krystek SR Jr, Seethala R, Golla R, Sleph PG, Beehler BC, Grover GJ, Fura A, Vyas VP, Li CY, Gougoutas JZ, Galella MA, Zahler R, Ostrowski J, Hamann LG.

J Med Chem. 2007 Jun 28;50(13):3015-25. Epub 2007 Jun 7.

PMID:
17552509
42.

Tandem optimization of target activity and elimination of mutagenic potential in a potent series of N-aryl bicyclic hydantoin-based selective androgen receptor modulators.

Hamann LG, Manfredi MC, Sun C, Krystek SR Jr, Huang Y, Bi Y, Augeri DJ, Wang T, Zou Y, Betebenner DA, Fura A, Seethala R, Golla R, Kuhns JE, Lupisella JA, Darienzo CJ, Custer LL, Price JL, Johnson JM, Biller SA, Zahler R, Ostrowski J.

Bioorg Med Chem Lett. 2007 Apr 1;17(7):1860-4. Epub 2007 Jan 27.

PMID:
17292608
43.

Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold.

Sun C, Robl JA, Wang TC, Huang Y, Kuhns JE, Lupisella JA, Beehler BC, Golla R, Sleph PG, Seethala R, Fura A, Krystek SR Jr, An Y, Malley MF, Sack JS, Salvati ME, Grover GJ, Ostrowski J, Hamann LG.

J Med Chem. 2006 Dec 28;49(26):7596-9.

PMID:
17181141
44.

Pharmacological and x-ray structural characterization of a novel selective androgen receptor modulator: potent hyperanabolic stimulation of skeletal muscle with hypostimulation of prostate in rats.

Ostrowski J, Kuhns JE, Lupisella JA, Manfredi MC, Beehler BC, Krystek SR Jr, Bi Y, Sun C, Seethala R, Golla R, Sleph PG, Fura A, An Y, Kish KF, Sack JS, Mookhtiar KA, Grover GJ, Hamann LG.

Endocrinology. 2007 Jan;148(1):4-12. Epub 2006 Sep 28.

PMID:
17008401
45.

Seco-prolinenitrile inhibitors of dipeptidyl peptidase IV define minimal pharmacophore requirements at P1.

Magnin DR, Taunk PC, Robertson JG, Wang A, Marcinkeviciene J, Kirby MS, Hamann LG.

Bioorg Med Chem Lett. 2006 Mar 15;16(6):1731-4. Epub 2005 Dec 20.

PMID:
16376077
46.

Mechanism of Gly-Pro-pNA cleavage catalyzed by dipeptidyl peptidase-IV and its inhibition by saxagliptin (BMS-477118).

Kim YB, Kopcho LM, Kirby MS, Hamann LG, Weigelt CA, Metzler WJ, Marcinkeviciene J.

Arch Biochem Biophys. 2006 Jan 1;445(1):9-18. Epub 2005 Dec 5.

PMID:
16364232
47.

Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors.

Zhao G, Taunk PC, Magnin DR, Simpkins LM, Robl JA, Wang A, Robertson JG, Marcinkeviciene J, Sitkoff DF, Parker RA, Kirby MS, Hamann LG.

Bioorg Med Chem Lett. 2005 Sep 15;15(18):3992-5.

PMID:
16046120
48.

Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Augeri DJ, Robl JA, Betebenner DA, Magnin DR, Khanna A, Robertson JG, Wang A, Simpkins LM, Taunk P, Huang Q, Han SP, Abboa-Offei B, Cap M, Xin L, Tao L, Tozzo E, Welzel GE, Egan DM, Marcinkeviciene J, Chang SY, Biller SA, Kirby MS, Parker RA, Hamann LG.

J Med Chem. 2005 Jul 28;48(15):5025-37.

PMID:
16033281
49.

Structure-activity relationships and sub-type selectivity in an oxabicyclic estrogen receptor alpha/beta agonist scaffold.

Hamann LG, Meyer JH, Ruppar DA, Marschke KB, Lopez FJ, Allegretto EA, Karanewsky DS.

Bioorg Med Chem Lett. 2005 Mar 1;15(5):1463-6.

PMID:
15713407
50.

Synthesis of novel potent dipeptidyl peptidase IV inhibitors with enhanced chemical stability: interplay between the N-terminal amino acid alkyl side chain and the cyclopropyl group of alpha-aminoacyl-l-cis-4,5-methanoprolinenitrile-based inhibitors.

Magnin DR, Robl JA, Sulsky RB, Augeri DJ, Huang Y, Simpkins LM, Taunk PC, Betebenner DA, Robertson JG, Abboa-Offei BE, Wang A, Cap M, Xin L, Tao L, Sitkoff DF, Malley MF, Gougoutas JZ, Khanna A, Huang Q, Han SP, Parker RA, Hamann LG.

J Med Chem. 2004 May 6;47(10):2587-98.

PMID:
15115400

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