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Items: 1 to 50 of 76

1.

Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.

Pio B, Chobanian HR, Guo Y, Josien H, Hagmann WK, Miller M, Trujillo ME, Kirkland M, Kosinski D, Mane J, Pachanski M, Cheewatrakoolpong B, Ashley E, Orr R, Wright MJ, Bugianesi R, Souza S, Zhang X, Di Salvo J, Weinglass AB, Tschirret-Guth R, Samuel K, Chen Q, Shang J, Lamca J, Ehrhart J, Nargund R, Howard AD, Colletti SL.

Bioorg Med Chem Lett. 2019 Jul 15;29(14):1842-1848. doi: 10.1016/j.bmcl.2019.04.050. Epub 2019 May 2.

PMID:
31109791
2.

Structure-Activity Relationship of Novel and Selective Biaryl-Chroman GPR40 AgoPAMs.

Chen HY, Plummer CW, Xiao D, Chobanian HR, DeMong D, Miller M, Trujillo ME, Kirkland M, Kosinski D, Mane J, Pachanski M, Cheewatrakoolpong B, Di Salvo J, Thomas-Fowlkes B, Souza S, Tatosian DA, Chen Q, Hafey MJ, Houle R, Nolting AF, Orr R, Ehrhart J, Weinglass AB, Tschirret-Guth R, Howard AD, Colletti SL.

ACS Med Chem Lett. 2018 Jun 14;9(7):685-690. doi: 10.1021/acsmedchemlett.8b00149. eCollection 2018 Jul 12.

3.

GPR40 partial agonists and AgoPAMs: Differentiating effects on glucose and hormonal secretions in the rodent.

Pachanski MJ, Kirkland ME, Kosinski DT, Mane J, Cheewatrakoolpong B, Xue J, Szeto D, Forrest G, Miller C, Bunzel M, Plummer CW, Chobanian HR, Miller MW, Souza S, Thomas-Fowlkes BS, Ogawa AM, Weinglass AB, Di Salvo J, Li X, Feng Y, Tatosian DA, Howard AD, Colletti SL, Trujillo ME.

PLoS One. 2017 Oct 20;12(10):e0186033. doi: 10.1371/journal.pone.0186033. eCollection 2017.

4.

GPR120 suppresses adipose tissue lipolysis and synergizes with GPR40 in antidiabetic efficacy.

Satapati S, Qian Y, Wu MS, Petrov A, Dai G, Wang SP, Zhu Y, Shen X, Muise ES, Chen Y, Zycband E, Weinglass A, Di Salvo J, Debenham JS, Cox JM, Lan P, Shah V, Previs SF, Erion M, Kelley DE, Wang L, Howard AD, Shang J.

J Lipid Res. 2017 Aug;58(8):1561-1578. doi: 10.1194/jlr.M075044. Epub 2017 Jun 5.

5.

Structural basis for the cooperative allosteric activation of the free fatty acid receptor GPR40.

Lu J, Byrne N, Wang J, Bricogne G, Brown FK, Chobanian HR, Colletti SL, Di Salvo J, Thomas-Fowlkes B, Guo Y, Hall DL, Hadix J, Hastings NB, Hermes JD, Ho T, Howard AD, Josien H, Kornienko M, Lumb KJ, Miller MW, Patel SB, Pio B, Plummer CW, Sherborne BS, Sheth P, Souza S, Tummala S, Vonrhein C, Webb M, Allen SJ, Johnston JM, Weinglass AB, Sharma S, Soisson SM.

Nat Struct Mol Biol. 2017 Jul;24(7):570-577. doi: 10.1038/nsmb.3417. Epub 2017 Jun 5.

PMID:
28581512
6.

GPR40 partial agonist MK-2305 lower fasting glucose in the Goto Kakizaki rat via suppression of endogenous glucose production.

Miller C, Pachanski MJ, Kirkland ME, Kosinski DT, Mane J, Bunzel M, Cao J, Souza S, Thomas-Fowlkes B, Di Salvo J, Weinglass AB, Li X, Myers RW, Knagge K, Carrington PE, Hagmann WK, Trujillo ME.

PLoS One. 2017 May 23;12(5):e0176182. doi: 10.1371/journal.pone.0176182. eCollection 2017.

7.

GPR40 reduces food intake and body weight through GLP-1.

Gorski JN, Pachanski MJ, Mane J, Plummer CW, Souza S, Thomas-Fowlkes BS, Ogawa AM, Weinglass AB, Di Salvo J, Cheewatrakoolpong B, Howard AD, Colletti SL, Trujillo ME.

Am J Physiol Endocrinol Metab. 2017 Jul 1;313(1):E37-E47. doi: 10.1152/ajpendo.00435.2016. Epub 2017 Mar 14.

8.

Design and Synthesis of Novel, Selective GPR40 AgoPAMs.

Plummer CW, Clements MJ, Chen H, Rajagopalan M, Josien H, Hagmann WK, Miller M, Trujillo ME, Kirkland M, Kosinski D, Mane J, Pachanski M, Cheewatrakoolpong B, Nolting AF, Orr R, Christensen M, Campeau LC, Wright MJ, Bugianesi R, Souza S, Zhang X, Di Salvo J, Weinglass AB, Tschirret-Guth R, Nargund R, Howard AD, Colletti SL.

ACS Med Chem Lett. 2017 Jan 23;8(2):221-226. doi: 10.1021/acsmedchemlett.6b00443. eCollection 2017 Feb 9.

9.

Corrigendum to "Discovery of benzofuran propanoic acid GPR120 agonists: From uHTS hit to mechanism-based pharmacodynamic effects" [Bioorg. Med. Chem. Lett. 26 (2016) 5724-5728].

Lombardo M, Bender K, London C, Plotkin MA, Kirkland M, Mane J, Pachanski M, Geissler W, Cummings J, Habulihaz B, Akiyama TE, Di Salvo J, Madeira M, Pols J, Powles MA, Finley MF, Johnson E, Roussel T, Uebele VN, Crespo A, Leung D, Alleyne C, Trusca D, Lei Y, Howard AD, Ujjainwalla F, Tata JR, Sinz CJ.

Bioorg Med Chem Lett. 2017 Mar 1;27(5):1333. doi: 10.1016/j.bmcl.2017.01.082. Epub 2017 Feb 4. No abstract available.

PMID:
28169160
10.

Discovery of Chromane Propionic Acid Analogues as Selective Agonists of GPR120 with in Vivo Activity in Rodents.

Adams GL, Velazquez F, Jayne C, Shah U, Miao S, Ashley ER, Madeira M, Akiyama TE, Di Salvo J, Suzuki T, Wang N, Truong Q, Gilbert E, Zhou D, Verras A, Kirkland M, Pachanski M, Powles M, Yin W, Ujjainwalla F, Venkatraman S, Edmondson SD.

ACS Med Chem Lett. 2016 Dec 6;8(1):96-101. doi: 10.1021/acsmedchemlett.6b00394. eCollection 2017 Jan 12.

11.

Design, Synthesis, and Evaluation of Novel and Selective G-protein Coupled Receptor 120 (GPR120) Spirocyclic Agonists.

Cox JM, Chu HD, Chelliah MV, Debenham JS, Eagen K, Lan P, Lombardo M, London C, Plotkin MA, Shah U, Sun Z, Vaccaro HM, Venkatraman S, Suzuki T, Wang N, Ashley ER, Crespo A, Madeira M, Leung DH, Alleyne C, Ogawa AM, Souza S, Thomas-Fowlkes B, Di Salvo J, Weinglass A, Kirkland M, Pachanski M, Powles MA, Tozzo E, Akiyama TE, Ujjainwalla F, Tata JR, Sinz CJ.

ACS Med Chem Lett. 2016 Nov 17;8(1):49-54. doi: 10.1021/acsmedchemlett.6b00360. eCollection 2017 Jan 12.

12.

Investigation of piperazine benzamides as human β3 adrenergic receptor agonists for the treatment of overactive bladder.

Harper BH, Wang L, Zhu C, Kar NF, Li B, Moyes CR, Goble SD, Costa M, Dingley K, Di Salvo J, Ha SN, Hurley A, Li X, Miller RR, Nagabukuro H, Salituro GM, Smith S, Struthers M, Hale JJ, Edmondson SD, Berger R.

Bioorg Med Chem Lett. 2017 Feb 15;27(4):1094-1098. doi: 10.1016/j.bmcl.2016.12.033. Epub 2016 Dec 11.

PMID:
28089699
13.

Pharmacological Characterization of a Novel Beta 3 Adrenergic Agonist, Vibegron: Evaluation of Antimuscarinic Receptor Selectivity for Combination Therapy for Overactive Bladder.

Di Salvo J, Nagabukuro H, Wickham LA, Abbadie C, DeMartino JA, Fitzmaurice A, Gichuru L, Kulick A, Donnelly MJ, Jochnowitz N, Hurley AL, Pereira A, Sanfiz A, Veronin G, Villa K, Woods J, Zamlynny B, Zycband E, Salituro GM, Frenkl T, Weber AE, Edmondson SD, Struthers M.

J Pharmacol Exp Ther. 2017 Feb;360(2):346-355. doi: 10.1124/jpet.116.237313. Epub 2016 Dec 13.

PMID:
27965369
14.

Discovery of benzofuran propanoic acid GPR120 agonists: From uHTS hit to mechanism-based pharmacodynamic effects.

Lombardo M, Bender K, London C, Plotkin MA, Kirkland M, Mane J, Pachanski M, Geissler W, Cummings J, Habulihaz B, Akiyama TE, Di Salvo J, Madeira M, Pols J, Powles MA, Finley MF, Johnson E, Roussel T, Uebele VN, Crespo A, Leung D, Alleyne C, Trusca D, Lei Y, Howard AD, Ujjainwalla F, Tata JR, Sinz CJ.

Bioorg Med Chem Lett. 2016 Dec 1;26(23):5724-5728. doi: 10.1016/j.bmcl.2016.10.054. Epub 2016 Oct 24. Erratum in: Bioorg Med Chem Lett. 2017 Mar 1;27(5):1333.

PMID:
27815121
15.

Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.

Edmondson SD, Zhu C, Kar NF, Di Salvo J, Nagabukuro H, Sacre-Salem B, Dingley K, Berger R, Goble SD, Morriello G, Harper B, Moyes CR, Shen DM, Wang L, Ball R, Fitzmaurice A, Frenkl T, Gichuru LN, Ha S, Hurley AL, Jochnowitz N, Levorse D, Mistry S, Miller RR, Ormes J, Salituro GM, Sanfiz A, Stevenson AS, Villa K, Zamlynny B, Green S, Struthers M, Weber AE.

J Med Chem. 2016 Jan 28;59(2):609-23. doi: 10.1021/acs.jmedchem.5b01372. Epub 2016 Jan 8.

PMID:
26709102
16.

SPECTRON, a neutron noise measurement system in frequency domain.

de Izarra G, Jammes C, Geslot B, Di Salvo J, Destouches C.

Rev Sci Instrum. 2015 Nov;86(11):115111. doi: 10.1063/1.4935250.

PMID:
26628176
17.

Discovery of benzamides as potent human β3 adrenergic receptor agonists.

Zhu C, Kar NF, Li B, Costa M, Dingley KH, Di Salvo J, Ha SN, Hurley AL, Li X, Miller RR, Salituro GM, Struthers M, Weber AE, Hale JJ, Edmondson SD.

Bioorg Med Chem Lett. 2016 Jan 1;26(1):55-9. doi: 10.1016/j.bmcl.2015.11.030. Epub 2015 Nov 11.

PMID:
26590100
18.

GPR40 (FFAR1) - Combined Gs and Gq signaling in vitro is associated with robust incretin secretagogue action ex vivo and in vivo.

Hauge M, Vestmar MA, Husted AS, Ekberg JP, Wright MJ, Di Salvo J, Weinglass AB, Engelstoft MS, Madsen AN, Lückmann M, Miller MW, Trujillo ME, Frimurer TM, Holst B, Howard AD, Schwartz TW.

Mol Metab. 2014 Oct 24;4(1):3-14. doi: 10.1016/j.molmet.2014.10.002. eCollection 2015 Jan.

19.

A Gpr120-selective agonist improves insulin resistance and chronic inflammation in obese mice.

Oh DY, Walenta E, Akiyama TE, Lagakos WS, Lackey D, Pessentheiner AR, Sasik R, Hah N, Chi TJ, Cox JM, Powels MA, Di Salvo J, Sinz C, Watkins SM, Armando AM, Chung H, Evans RM, Quehenberger O, McNelis J, Bogner-Strauss JG, Olefsky JM.

Nat Med. 2014 Aug;20(8):942-7. doi: 10.1038/nm.3614. Epub 2014 Jul 6.

20.

Design, synthesis, and evaluation of conformationally restricted acetanilides as potent and selective β3 adrenergic receptor agonists for the treatment of overactive bladder.

Moyes CR, Berger R, Goble SD, Harper B, Shen DM, Wang L, Bansal A, Brown PN, Chen AS, Dingley KH, Di Salvo J, Fitzmaurice A, Gichuru LN, Hurley AL, Jochnowitz N, Miller RR, Mistry S, Nagabukuro H, Salituro GM, Sanfiz A, Stevenson AS, Villa K, Zamlynny B, Struthers M, Weber AE, Edmondson SD.

J Med Chem. 2014 Feb 27;57(4):1437-53. doi: 10.1021/jm4017224. Epub 2014 Feb 5.

PMID:
24437735
21.

The discovery of potent antagonists of NPBWR1 (GPR7).

Anthony Romero F, Hastings NB, Moningka R, Guo Z, Wang M, Di Salvo J, Lei Y, Trusca D, Deng Q, Tong V, Terebetski JL, Ball RG, Ujjainwalla F.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1014-8. doi: 10.1016/j.bmcl.2011.11.126. Epub 2011 Dec 8.

PMID:
22197390
22.

Design of a novel pyrrolidine scaffold utilized in the discovery of potent and selective human β3 adrenergic receptor agonists.

Morriello GJ, Wendt HR, Bansal A, Di Salvo J, Feighner S, He J, Hurley AL, Hreniuk DL, Salituro GM, Reddy MV, Galloway SM, McGettigan KK, Laws G, McKnight C, Doss GA, Tsou NN, Black RM, Morris J, Ball RG, Sanfiz AT, Streckfuss E, Struthers M, Edmondson SD.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1865-70. doi: 10.1016/j.bmcl.2010.12.087. Epub 2010 Dec 25.

PMID:
21353541
23.

Potent heteroarylpiperidine and carboxyphenylpiperidine 1-alkyl-cyclopentane carboxamide CCR2 antagonists.

Pasternak A, Goble SD, Vicario PP, Di Salvo J, Ayala JM, Struthers M, DeMartino JA, Mills SG, Yang L.

Bioorg Med Chem Lett. 2008 Feb 1;18(3):994-8. doi: 10.1016/j.bmcl.2007.12.029. Epub 2007 Dec 27.

PMID:
18164199
24.

(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]triazolo[1,5-a]-pyridin-6-ylphenyl)butanamide: a selective alpha-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Edmondson SD, Mastracchio A, Mathvink RJ, He J, Harper B, Park YJ, Beconi M, Di Salvo J, Eiermann GJ, He H, Leiting B, Leone JF, Levorse DA, Lyons K, Patel RA, Patel SB, Petrov A, Scapin G, Shang J, Roy RS, Smith A, Wu JK, Xu S, Zhu B, Thornberry NA, Weber AE.

J Med Chem. 2006 Jun 15;49(12):3614-27.

PMID:
16759103
25.

4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors.

Parmee ER, He J, Mastracchio A, Edmondson SD, Colwell L, Eiermann G, Feeney WP, Habulihaz B, He H, Kilburn R, Leiting B, Lyons K, Marsilio F, Patel RA, Petrov A, Di Salvo J, Wu JK, Thornberry NA, Weber AE.

Bioorg Med Chem Lett. 2004 Jan 5;14(1):43-6.

PMID:
14684294
26.

Comparison of the functional blockade of rat substance P (NK1) receptors by GR205171, RP67580, SR140333 and NKP-608.

Rupniak NM, Carlson EJ, Shepheard S, Bentley G, Williams AR, Hill A, Swain C, Mills SG, Di Salvo J, Kilburn R, Cascieri MA, Kurtz MM, Tsao KL, Gould SL, Chicchi GG.

Neuropharmacology. 2003 Aug;45(2):231-41.

PMID:
12842129
27.

Antibody-mediated blockade of the CXCR3 chemokine receptor results in diminished recruitment of T helper 1 cells into sites of inflammation.

Xie JH, Nomura N, Lu M, Chen SL, Koch GE, Weng Y, Rosa R, Di Salvo J, Mudgett J, Peterson LB, Wicker LS, DeMartino JA.

J Leukoc Biol. 2003 Jun;73(6):771-80.

PMID:
12773510
28.

Binding of 2-aryl-4-(piperidin-1-yl)butanamines and 1,3,4-trisubstituted pyrrolidines to human CCR5: a molecular modeling-guided mutagenesis study of the binding pocket.

Castonguay LA, Weng Y, Adolfsen W, Di Salvo J, Kilburn R, Caldwell CG, Daugherty BL, Finke PE, Hale JJ, Lynch CL, Mills SG, MacCoss M, Springer MS, DeMartino JA.

Biochemistry. 2003 Feb 18;42(6):1544-50.

PMID:
12578367
29.

4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists II.

Cooper LC, Carlson EJ, Castro JL, Chicchi GG, Dinnell K, Di Salvo J, Elliott JM, Hollingworth GJ, Kurtz MM, Ridgill MP, Rycroft W, Tsao KL, Swain CJ.

Bioorg Med Chem Lett. 2002 Jul 8;12(13):1759-62.

PMID:
12067555
30.

Combinatorial synthesis of 3-(amidoalkyl) and 3-(aminoalkyl)-2-arylindole derivatives: discovery of potent ligands for a variety of G-protein coupled receptors.

Willoughby CA, Hutchins SM, Rosauer KG, Dhar MJ, Chapman KT, Chicchi GG, Sadowski S, Weinberg DH, Patel S, Malkowitz L, Di Salvo J, Pacholok SG, Cheng K.

Bioorg Med Chem Lett. 2002 Jan 7;12(1):93-6.

PMID:
11738581
31.

Cyclic imides as potent and selective alpha-1A adrenergic receptor antagonists.

DiPardo RM, Patane MA, Newton RC, Price R, Broten TP, Chang RS, Ransom RW, Di Salvo J, Freidinger RM, Bock MG.

Bioorg Med Chem Lett. 2001 Jul 23;11(14):1959-62.

PMID:
11459670
32.

The CXCR4 agonist ligand stromal derived factor-1 maintains high affinity for receptors in both Galpha(i)-coupled and uncoupled states.

Di Salvo J, Koch GE, Johnson KE, Blake AD, Daugherty BL, DeMartino JA, Sirotina-Meisher A, Liu Y, Springer MS, Cascieri MA, Sullivan KA.

Eur J Pharmacol. 2000 Dec 8;409(2):143-54.

PMID:
11104827
33.

Phenylacetamides as selective alpha-1A adrenergic receptor antagonists.

Patane MA, DiPardo RM, Newton RC, Price RP, Broten TP, Chang RS, Ransom RW, Di Salvo J, Nagarathnam D, Forray C, Gluchowski C, Bock MG.

Bioorg Med Chem Lett. 2000 Aug 7;10(15):1621-4.

PMID:
10937709
34.

Acidic fibroblast growth factor is present in the enteric nervous system of the large intestine.

Capetandes A, Di Salvo J, Ronan JJ, Thomas KA.

J Histochem Cytochem. 2000 Mar;48(3):407-14.

PMID:
10681394
35.

Selective alpha-1a adrenergic receptor antagonists. Effects of pharmacophore regio- and stereochemistry on potency and selectivity.

Patane MA, DiPardo RM, Price RP, Chang RS, Ransom RW, O'Malley SS, Di Salvo J, Bock MG.

Bioorg Med Chem Lett. 1998 Sep 22;8(18):2495-500.

PMID:
9873568
36.

Protein kinase C: modulation of vasopressin-induced calcium influx and release in A7r5 vascular smooth muscle cells.

Kaplan-Albuquerque N, Di Salvo J.

Arch Biochem Biophys. 1998 Nov 15;359(2):209-14.

PMID:
9808762
38.

Genistein sensitivity of calcium transport pathways in serotonin-activated vascular smooth muscle cells.

Nelson SR, Chien T, Di Salvo J.

Arch Biochem Biophys. 1997 Sep 1;345(1):65-72.

PMID:
9281312
39.

Protein tyrosine phosphorylation in smooth muscle: a potential coupling mechanism between receptor activation and intracellular calcium.

Di Salvo J, Nelson SR, Kaplan N.

Proc Soc Exp Biol Med. 1997 Apr;214(4):285-301. Review.

PMID:
9111520
41.
42.

Modulation of Ca2+ sensitivity in smooth muscle by genistein and protein tyrosine phosphorylation.

Steusloff A, Paul E, Semenchuk LA, Di Salvo J, Pfitzer G.

Arch Biochem Biophys. 1995 Jul 10;320(2):236-42.

PMID:
7625829
43.

Protein tyrosine phosphorylation, cellular Ca2+, and Ca2+ sensitivity for contraction of smooth muscle.

Di Salvo J, Pfitzer G, Semenchuk LA.

Can J Physiol Pharmacol. 1994 Nov;72(11):1434-9. Review.

PMID:
7767890
44.

Vanadate-induced contraction of smooth muscle and enhanced protein tyrosine phosphorylation.

Di Salvo J, Semenchuk LA, Lauer J.

Arch Biochem Biophys. 1993 Aug 1;304(2):386-91.

PMID:
7688495
45.

Tyrosine kinase inhibitors suppress agonist-induced contraction in smooth muscle.

Di Salvo J, Steusloff A, Semenchuk L, Satoh S, Kolquist K, Pfitzer G.

Biochem Biophys Res Commun. 1993 Feb 15;190(3):968-74.

PMID:
8439345
46.

The phospholamban phosphatase associated with cardiac sarcoplasmic reticulum is a type 1 enzyme.

Steenaart NA, Ganim JR, Di Salvo J, Kranias EG.

Arch Biochem Biophys. 1992 Feb 14;293(1):17-24.

PMID:
1309982
47.

Human retinal vascular cells differ from umbilical cells in synthetic functions and their response to glucose.

Rymaszewski Z, Szymanski PT, Abplanalp WA, Myatt L, Di Salvo J, Cohen RM.

Proc Soc Exp Biol Med. 1992 Feb;199(2):183-91.

PMID:
1741410
48.

Localization of acidic fibroblast growth factor within the mouse brain using biochemical and immunocytochemical techniques.

Fallon JH, Di Salvo J, Loughlin SE, Gimenez-Gallego G, Seroogy KB, Bradshaw RA, Morrison RS, Ciofi P, Thomas KA.

Growth Factors. 1992;6(2):139-57.

PMID:
1375040
49.

Effects of modulators of myosin phosphorylation on isometric force and shortening velocity in skinned smooth muscle.

Strauss JD, Szymanski PT, Di Salvo J, Paul RJ.

Prog Clin Biol Res. 1990;327:617-22.

PMID:
2157223
50.

Stabilization by heparin of acidic fibroblast growth factor mitogenicity for human endothelial cells in vitro.

Mueller SN, Thomas KA, Di Salvo J, Levine EM.

J Cell Physiol. 1989 Sep;140(3):439-48.

PMID:
2777882

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