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Items: 1 to 50 of 168

1.

Selection and progression of unimolecular agonists at the GIP, GLP-1, and glucagon receptors as drug candidates.

Knerr PJ, Mowery SA, Finan B, Perez-Tilve D, Tschöp MH, DiMarchi RD.

Peptides. 2019 Nov 28:170225. doi: 10.1016/j.peptides.2019.170225. [Epub ahead of print] Review.

PMID:
31786282
2.

The Structural Refinement of Glucagon for Therapeutic Use.

Chabenne J, Mroz PA, Mayer JP, DiMarchi RD.

J Med Chem. 2019 Nov 27. doi: 10.1021/acs.jmedchem.9b01493. [Epub ahead of print]

PMID:
31774682
3.

Glucagon-like peptide 1 (GLP-1).

Müller TD, Finan B, Bloom SR, D'Alessio D, Drucker DJ, Flatt PR, Fritsche A, Gribble F, Grill HJ, Habener JF, Holst JJ, Langhans W, Meier JJ, Nauck MA, Perez-Tilve D, Pocai A, Reimann F, Sandoval DA, Schwartz TW, Seeley RJ, Stemmer K, Tang-Christensen M, Woods SC, DiMarchi RD, Tschöp MH.

Mol Metab. 2019 Dec;30:72-130. doi: 10.1016/j.molmet.2019.09.010. Epub 2019 Sep 30. Review.

4.

Neurotrophic and neuroprotective effects of a monomeric GLP-1/GIP/Gcg receptor triagonist in cellular and rodent models of mild traumatic brain injury.

Li Y, Glotfelty EJ, Namdar I, Tweedie D, Olson L, Hoffer BJ, DiMarchi RD, Pick CG, Greig NH.

Exp Neurol. 2019 Nov 12;324:113113. doi: 10.1016/j.expneurol.2019.113113. [Epub ahead of print]

PMID:
31730763
5.

Glucagon-Receptor Signaling Reverses Hepatic Steatosis Independent of Leptin Receptor Expression.

Nason SR, Kim T, Antipenko JP, Finan B, DiMarchi R, Hunter CS, Habegger KM.

Endocrinology. 2019 Nov 1. pii: bqz013. doi: 10.1210/endocr/bqz013. [Epub ahead of print]

PMID:
31673703
6.

CNS-targeting pharmacological interventions for the metabolic syndrome.

Stemmer K, Müller TD, DiMarchi RD, Pfluger PT, Tschöp MH.

J Clin Invest. 2019 Aug 5;130:4058-4071. doi: 10.1172/JCI129195. eCollection 2019 Aug 5. Review.

7.

Insulin-like peptide 5 fails to improve metabolism or body weight in obese mice.

Zaykov AN, Gelfanov VM, Perez-Tilve D, Finan B, DiMarchi RD.

Peptides. 2019 Oct;120:170116. doi: 10.1016/j.peptides.2019.170116. Epub 2019 Jul 23.

PMID:
31348991
8.

A Disulfide Scan of Insulin by [3 + 1] Methodology Exhibits Site-Specific Influence on Bioactivity.

Brunel FM, Mayer JP, Gelfanov VM, Zaykov AN, Finan B, Perez-Tilve D, DiMarchi RD.

ACS Chem Biol. 2019 Aug 16;14(8):1829-1835. doi: 10.1021/acschembio.9b00420. Epub 2019 Aug 6.

PMID:
31343157
9.

A Brain-Melanocortin-Vagus Axis Mediates Adipose Tissue Expansion Independently of Energy Intake.

Holland J, Sorrell J, Yates E, Smith K, Arbabi S, Arnold M, Rivir M, Morano R, Chen J, Zhang X, Dimarchi R, Woods SC, Sanchez-Gurmaches J, Wohleb E, Perez-Tilve D.

Cell Rep. 2019 May 21;27(8):2399-2410.e6. doi: 10.1016/j.celrep.2019.04.089.

10.

Peptide Conjugates with Small Molecules Designed to Enhance Efficacy and Safety.

He R, Finan B, Mayer JP, DiMarchi RD.

Molecules. 2019 May 14;24(10). pii: E1855. doi: 10.3390/molecules24101855. Review.

11.

GLP-1/dexamethasone inhibits food reward without inducing mood and memory deficits in mice.

Décarie-Spain L, Fisette A, Zhu Z, Yang B, DiMarchi RD, Tschöp MH, Finan B, Fulton S, Clemmensen C.

Neuropharmacology. 2019 Jun;151:55-63. doi: 10.1016/j.neuropharm.2019.03.035. Epub 2019 Apr 1.

PMID:
30946847
12.

Long-Acting Neurotensin Synergizes With Liraglutide to Reverse Obesity Through a Melanocortin-Dependent Pathway.

Ratner C, He Z, Grunddal KV, Skov LJ, Hartmann B, Zhang F, Feuchtinger A, Bjerregaard A, Christoffersen C, Tschöp MH, Finan B, DiMarchi RD, Leinninger GM, Williams KW, Clemmensen C, Holst B.

Diabetes. 2019 Jun;68(6):1329-1340. doi: 10.2337/db18-1009. Epub 2019 Apr 1.

13.

The islet-expressed Lhx1 transcription factor interacts with Islet-1 and contributes to glucose homeostasis.

Bethea M, Liu Y, Wade AK, Mullen R, Gupta R, Gelfanov V, DiMarchi R, Bhatnagar S, Behringer R, Habegger KM, Hunter CS.

Am J Physiol Endocrinol Metab. 2019 Mar 1;316(3):E397-E409. doi: 10.1152/ajpendo.00235.2018. Epub 2019 Jan 8.

PMID:
30620636
14.

Optimized GIP analogs promote body weight lowering in mice through GIPR agonism not antagonism.

Mroz PA, Finan B, Gelfanov V, Yang B, Tschöp MH, DiMarchi RD, Perez-Tilve D.

Mol Metab. 2019 Feb;20:51-62. doi: 10.1016/j.molmet.2018.12.001. Epub 2018 Dec 5.

15.

Emerging hormonal-based combination pharmacotherapies for the treatment of metabolic diseases.

Clemmensen C, Finan B, Müller TD, DiMarchi RD, Tschöp MH, Hofmann SM.

Nat Rev Endocrinol. 2019 Feb;15(2):90-104. doi: 10.1038/s41574-018-0118-x. Review.

PMID:
30446744
16.

Structurally Constrained Insulin Analogs by Directed Stepwise Crosslinking.

Zhang F, Mayer JP, Gelfanov V, Liu F, DiMarchi RD.

Protein Pept Lett. 2018;25(12):1149-1154. doi: 10.2174/0929866525666181101103500.

PMID:
30381053
17.

"Let's Stay Together"; GIP and GLP-1 dual agonism in the treatment of metabolic disease.

DiMarchi RD.

Mol Metab. 2018 Dec;18:1-2. doi: 10.1016/j.molmet.2018.10.004. Epub 2018 Oct 12. No abstract available.

18.

Peptide-based multi-agonists: a new paradigm in metabolic pharmacology.

Brandt SJ, Müller TD, DiMarchi RD, Tschöp MH, Stemmer K.

J Intern Med. 2018 Dec;284(6):581-602. doi: 10.1111/joim.12837. Epub 2018 Oct 23. Review.

PMID:
30230640
19.

Deletion of the glucagon receptor gene before and after experimental diabetes reveals differential protection from hyperglycemia.

Rivero-Gutierrez B, Haller A, Holland J, Yates E, Khrisna R, Habegger K, Dimarchi R, D'Alessio D, Perez-Tilve D.

Mol Metab. 2018 Nov;17:28-38. doi: 10.1016/j.molmet.2018.07.012. Epub 2018 Aug 20.

20.

Hepatic Glucagon Receptor Signaling Enhances Insulin-Stimulated Glucose Disposal in Rodents.

Kim T, Holleman CL, Nason S, Arble DM, Ottaway N, Chabenne J, Loyd C, Kim JA, Sandoval D, Drucker DJ, DiMarchi R, Perez-Tilve D, Habegger KM.

Diabetes. 2018 Nov;67(11):2157-2166. doi: 10.2337/db18-0068. Epub 2018 Aug 27.

21.

Anti-Obesity Therapy: from Rainbow Pills to Polyagonists.

Müller TD, Clemmensen C, Finan B, DiMarchi RD, Tschöp MH.

Pharmacol Rev. 2018 Oct;70(4):712-746. doi: 10.1124/pr.117.014803. Review.

PMID:
30087160
22.

An incretin-based tri-agonist promotes superior insulin secretion from murine pancreatic islets via PLC activation.

Khajavi N, Finan B, Kluth O, Müller TD, Mergler S, Schulz A, Kleinau G, Scheerer P, Schürmann A, Gudermann T, Tschöp MH, Krude H, DiMarchi RD, Biebermann H.

Cell Signal. 2018 Nov;51:13-22. doi: 10.1016/j.cellsig.2018.07.006. Epub 2018 Jul 25.

PMID:
30055232
23.

Metabolic syndrome and extensive adipose tissue inflammation in morbidly obese Göttingen minipigs.

Renner S, Blutke A, Dobenecker B, Dhom G, Müller TD, Finan B, Clemmensen C, Bernau M, Novak I, Rathkolb B, Senf S, Zöls S, Roth M, Götz A, Hofmann SM, Hrabĕ de Angelis M, Wanke R, Kienzle E, Scholz AM, DiMarchi R, Ritzmann M, Tschöp MH, Wolf E.

Mol Metab. 2018 Oct;16:180-190. doi: 10.1016/j.molmet.2018.06.015. Epub 2018 Jun 28.

24.

Glucagon Receptor Signaling Regulates Energy Metabolism via Hepatic Farnesoid X Receptor and Fibroblast Growth Factor 21.

Kim T, Nason S, Holleman C, Pepin M, Wilson L, Berryhill TF, Wende AR, Steele C, Young ME, Barnes S, Drucker DJ, Finan B, DiMarchi R, Perez-Tilve D, Tschöp M, Habegger KM.

Diabetes. 2018 Sep;67(9):1773-1782. doi: 10.2337/db17-1502. Epub 2018 Jun 20.

25.

Targeting the Incretin/Glucagon System With Triagonists to Treat Diabetes.

Capozzi ME, DiMarchi RD, Tschöp MH, Finan B, Campbell JE.

Endocr Rev. 2018 Oct 1;39(5):719-738. doi: 10.1210/er.2018-00117. Review.

PMID:
29905825
26.

High-Yield Synthesis of Human Insulin-Like Peptide 5 Employing a Nonconventional Strategy.

Zaykov AN, Gelfanov VM, Liu F, DiMarchi RD.

Org Lett. 2018 Jun 15;20(12):3695-3699. doi: 10.1021/acs.orglett.8b01501. Epub 2018 Jun 6.

PMID:
29874090
27.

Molecular elements in FGF19 and FGF21 defining KLB/FGFR activity and specificity.

Agrawal A, Parlee S, Perez-Tilve D, Li P, Pan J, Mroz PA, Kruse Hansen AM, Andersen B, Finan B, Kharitonenkov A, DiMarchi RD.

Mol Metab. 2018 Jul;13:45-55. doi: 10.1016/j.molmet.2018.05.003. Epub 2018 May 11.

28.

Viral insulin-like peptides activate human insulin and IGF-1 receptor signaling: A paradigm shift for host-microbe interactions.

Altindis E, Cai W, Sakaguchi M, Zhang F, GuoXiao W, Liu F, De Meyts P, Gelfanov V, Pan H, DiMarchi R, Kahn CR.

Proc Natl Acad Sci U S A. 2018 Mar 6;115(10):2461-2466. doi: 10.1073/pnas.1721117115. Epub 2018 Feb 21.

29.

Synthesis and Characterization of the R27S Genetic Variant of Insulin-like Peptide 5.

Zaykov AN, Gelfanov VM, Liu F, DiMarchi RD.

ChemMedChem. 2018 Apr 23;13(8):852-859. doi: 10.1002/cmdc.201800057. Epub 2018 Mar 23.

PMID:
29466617
30.

Controlled intramolecular antagonism as a regulator of insulin receptor maximal activity.

Brandt SJ, Mayer JP, Ford J, Gelfanov VM, DiMarchi RD.

Peptides. 2018 Feb;100:18-23. doi: 10.1016/j.peptides.2017.11.022.

PMID:
29412818
31.

Max Bergmann award lecture:Macromolecular medicinal chemistry as applied to metabolic diseases.

DiMarchi RD, Mayer JP, Gelfanov VM, Tschöp M.

J Pept Sci. 2018 Jan;24(1). doi: 10.1002/psc.3056. Review.

PMID:
29322647
32.

Optimization of peptide-based polyagonists for treatment of diabetes and obesity.

Knerr PJ, Finan B, Gelfanov V, Perez-Tilve D, Tschöp MH, DiMarchi RD.

Bioorg Med Chem. 2018 Jun 1;26(10):2873-2881. doi: 10.1016/j.bmc.2017.10.047. Epub 2017 Nov 2. Review. No abstract available.

PMID:
29153547
33.

Gαs regulates Glucagon-Like Peptide 1 Receptor-mediated cyclic AMP generation at Rab5 endosomal compartment.

Girada SB, Kuna RS, Bele S, Zhu Z, Chakravarthi NR, DiMarchi RD, Mitra P.

Mol Metab. 2017 Oct;6(10):1173-1185. doi: 10.1016/j.molmet.2017.08.002. Epub 2017 Aug 10.

34.

Emerging Poly-Agonists for Obesity and Type 2 Diabetes.

Kleinert M, Clemmensen C, Stemmer K, Müller TD, DiMarchi RD, Tschöp MH.

Obesity (Silver Spring). 2017 Oct;25(10):1647-1649. doi: 10.1002/oby.21932. No abstract available.

35.

Molecular Integration of Incretin and Glucocorticoid Action Reverses Immunometabolic Dysfunction and Obesity.

Quarta C, Clemmensen C, Zhu Z, Yang B, Joseph SS, Lutter D, Yi CX, Graf E, García-Cáceres C, Legutko B, Fischer K, Brommage R, Zizzari P, Franklin BS, Krueger M, Koch M, Vettorazzi S, Li P, Hofmann SM, Bakhti M, Bastidas-Ponce A, Lickert H, Strom TM, Gailus-Durner V, Bechmann I, Perez-Tilve D, Tuckermann J, Hrabě de Angelis M, Sandoval D, Cota D, Latz E, Seeley RJ, Müller TD, DiMarchi RD, Finan B, Tschöp MH.

Cell Metab. 2017 Oct 3;26(4):620-632.e6. doi: 10.1016/j.cmet.2017.08.023. Epub 2017 Sep 21.

36.

Treatment of Diabetes and Obesity by Rationally Designed Peptide Agonists Functioning at Multiple Metabolic Receptors.

Khajavi N, Biebermann H, Tschöp M, DiMarchi R.

Endocr Dev. 2017;32:165-182. doi: 10.1159/000475737. Epub 2017 Aug 15.

PMID:
28873389
37.

Synthetic Advances in Insulin-like Peptides Enable Novel Bioactivity.

Liu F, Li P, Gelfanov V, Mayer J, DiMarchi R.

Acc Chem Res. 2017 Aug 15;50(8):1855-1865. doi: 10.1021/acs.accounts.7b00227. Epub 2017 Aug 3.

PMID:
28771323
38.

The Sustained Effects of a Dual GIP/GLP-1 Receptor Agonist, NNC0090-2746, in Patients with Type 2 Diabetes.

Frias JP, Bastyr EJ 3rd, Vignati L, Tschöp MH, Schmitt C, Owen K, Christensen RH, DiMarchi RD.

Cell Metab. 2017 Aug 1;26(2):343-352.e2. doi: 10.1016/j.cmet.2017.07.011.

39.

Once Blind, Now We See GLP-1 Molecular Action.

Mayer JP, Tschöp MH, DiMarchi RD.

Cell Metab. 2017 Aug 1;26(2):289-291. doi: 10.1016/j.cmet.2017.07.014.

40.
41.

GLP-1/glucagon receptor co-agonism for treatment of obesity.

Sánchez-Garrido MA, Brandt SJ, Clemmensen C, Müller TD, DiMarchi RD, Tschöp MH.

Diabetologia. 2017 Oct;60(10):1851-1861. doi: 10.1007/s00125-017-4354-8. Epub 2017 Jul 21. Review.

42.

Pharmacodynamics, pharmacokinetics and safety of multiple ascending doses of the novel dual glucose-dependent insulinotropic polypeptide/glucagon-like peptide-1 agonist RG7697 in people with type 2 diabetes mellitus.

Schmitt C, Portron A, Jadidi S, Sarkar N, DiMarchi R.

Diabetes Obes Metab. 2017 Oct;19(10):1436-1445. doi: 10.1111/dom.13024. Epub 2017 Jul 20.

PMID:
28730694
43.

Single-Molecule Combinatorial Therapeutics for Treating Obesity and Diabetes.

Tschöp M, DiMarchi R.

Diabetes. 2017 Jul;66(7):1766-1769. doi: 10.2337/dbi16-0068. Epub 2017 Jun 11. No abstract available.

44.

Synthesis of relaxin-2 and insulin-like peptide 5 enabled by novel tethering and traceless chemical excision.

Thalluri K, Kou B, Yang X, Zaykov AN, Mayer JP, Gelfanov VM, Liu F, DiMarchi RD.

J Pept Sci. 2017 Jun;23(6):455-465. doi: 10.1002/psc.3010. Epub 2017 May 3.

PMID:
28466571
45.

Monomeric GLP-1/GIP/glucagon triagonism corrects obesity, hepatosteatosis, and dyslipidemia in female mice.

Jall S, Sachs S, Clemmensen C, Finan B, Neff F, DiMarchi RD, Tschöp MH, Müller TD, Hofmann SM.

Mol Metab. 2017 Mar 1;6(5):440-446. doi: 10.1016/j.molmet.2017.02.002. eCollection 2017 May.

46.

Synthesis of Four-Disulfide Insulin Analogs via Sequential Disulfide Bond Formation.

Wu F, Mayer JP, Gelfanov VM, Liu F, DiMarchi RD.

J Org Chem. 2017 Apr 7;82(7):3506-3512. doi: 10.1021/acs.joc.6b03078. Epub 2017 Mar 27.

PMID:
28319665
47.

The New Biology and Pharmacology of Glucagon.

Müller TD, Finan B, Clemmensen C, DiMarchi RD, Tschöp MH.

Physiol Rev. 2017 Apr;97(2):721-766. doi: 10.1152/physrev.00025.2016. Review.

48.

Biomimetic Synthesis of Insulin Enabled by Oxime Ligation and Traceless "C-Peptide" Chemical Excision.

Thalluri K, Kou B, Gelfanov V, Mayer JP, Liu F, DiMarchi RD.

Org Lett. 2017 Feb 3;19(3):706-709. doi: 10.1021/acs.orglett.6b03876. Epub 2017 Jan 26.

PMID:
28124920
49.

Fibroblast growth factor 21 night watch: advances and uncertainties in the field.

Kharitonenkov A, DiMarchi R.

J Intern Med. 2017 Mar;281(3):233-246. doi: 10.1111/joim.12580. Epub 2016 Nov 22. Review.

50.

Novel GLP-1R/GIPR co-agonist "twincretin" is neuroprotective in cell and rodent models of mild traumatic brain injury.

Tamargo IA, Bader M, Li Y, Yu SJ, Wang Y, Talbot K, DiMarchi RD, Pick CG, Greig NH.

Exp Neurol. 2017 Feb;288:176-186. doi: 10.1016/j.expneurol.2016.11.005. Epub 2016 Nov 11.

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