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Items: 1 to 50 of 105

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.

Structural Refinement of Glucagon for Therapeutic Use.

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

J Med Chem. 2019 Dec 18. 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. 2020 Feb;324:113113. doi: 10.1016/j.expneurol.2019.113113. Epub 2019 Nov 12.

PMID:
31730763
5.

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.

6.

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
7.

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
8.

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.

9.

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
10.

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.

11.

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.

12.

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
13.

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
14.

"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.

15.

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
16.

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
17.

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
18.

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
19.

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
20.

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.

21.

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
22.

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
23.

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
24.

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
25.

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.

26.

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.

27.

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.

28.

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.

29.

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.

30.

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.

31.

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
32.

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.

33.

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
34.

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.

35.

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
36.

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.

37.

Native Design of Soluble, Aggregation-Resistant Bioactive Peptides: Chemical Evolution of Human Glucagon.

Mroz PA, Perez-Tilve D, Liu F, Mayer JP, DiMarchi RD.

ACS Chem Biol. 2016 Dec 16;11(12):3412-3420. Epub 2016 Nov 8.

PMID:
27797473
38.

Fibroblast activation protein (FAP) as a novel metabolic target.

Sánchez-Garrido MA, Habegger KM, Clemmensen C, Holleman C, Müller TD, Perez-Tilve D, Li P, Agrawal AS, Finan B, Drucker DJ, Tschöp MH, DiMarchi RD, Kharitonenkov A.

Mol Metab. 2016 Jul 16;5(10):1015-1024. doi: 10.1016/j.molmet.2016.07.003. eCollection 2016 Oct.

39.

Pyridyl-alanine as a Hydrophilic, Aromatic Element in Peptide Structural Optimization.

Mroz PA, Perez-Tilve D, Liu F, Gelfanov V, DiMarchi RD, Mayer JP.

J Med Chem. 2016 Sep 8;59(17):8061-7. doi: 10.1021/acs.jmedchem.6b00840. Epub 2016 Aug 25.

PMID:
27509198
40.

GLP-1 and estrogen conjugate acts in the supramammillary nucleus to reduce food-reward and body weight.

Vogel H, Wolf S, Rabasa C, Rodriguez-Pacheco F, Babaei CS, Stöber F, Goldschmidt J, DiMarchi RD, Finan B, Tschöp MH, Dickson SL, Schürmann A, Skibicka KP.

Neuropharmacology. 2016 Nov;110(Pt A):396-406. doi: 10.1016/j.neuropharm.2016.07.039. Epub 2016 Aug 2.

41.

Unimolecular Polypharmacy for Treatment of Diabetes and Obesity.

Tschöp MH, Finan B, Clemmensen C, Gelfanov V, Perez-Tilve D, Müller TD, DiMarchi RD.

Cell Metab. 2016 Jul 12;24(1):51-62. doi: 10.1016/j.cmet.2016.06.021. Review.

42.

Chemical Synthesis of Human Insulin-Like Peptide-6.

Wu F, Mayer JP, Zaykov AN, Zhang F, Liu F, DiMarchi RD.

Chemistry. 2016 Jul 4;22(28):9777-83. doi: 10.1002/chem.201601410. Epub 2016 Jun 3.

PMID:
27259101
43.

Reappraisal of GIP Pharmacology for Metabolic Diseases.

Finan B, Müller TD, Clemmensen C, Perez-Tilve D, DiMarchi RD, Tschöp MH.

Trends Mol Med. 2016 May;22(5):359-376. doi: 10.1016/j.molmed.2016.03.005. Epub 2016 Mar 30. Review.

PMID:
27038883
44.

Pursuit of a perfect insulin.

Zaykov AN, Mayer JP, DiMarchi RD.

Nat Rev Drug Discov. 2016 Jun;15(6):425-39. doi: 10.1038/nrd.2015.36. Epub 2016 Mar 18. Review.

PMID:
26988411
45.

Chemical synthesis of peptides within the insulin superfamily.

Liu F, Zaykov AN, Levy JJ, DiMarchi RD, Mayer JP.

J Pept Sci. 2016 May;22(5):260-70. doi: 10.1002/psc.2863. Epub 2016 Feb 22. Review.

PMID:
26910514
46.

A new quorum-sensing system (TprA/PhrA) for Streptococcus pneumoniae D39 that regulates a lantibiotic biosynthesis gene cluster.

Hoover SE, Perez AJ, Tsui HC, Sinha D, Smiley DL, DiMarchi RD, Winkler ME, Lazazzera BA.

Mol Microbiol. 2015 Jul;97(2):229-43. doi: 10.1111/mmi.13029. Epub 2015 May 26.

47.

Three-chain insulin analogs demonstrate the importance of insulin secondary structure to bioactivity.

Wu F, Chabenne JR, Gelfanov VM, Mayer JP, DiMarchi RD.

J Pept Sci. 2015 Mar;21(3):223-30. doi: 10.1002/psc.2744. Epub 2015 Feb 9.

PMID:
25665061
48.

GLP-1-oestrogen attenuates hyperphagia and protects from beta cell failure in diabetes-prone New Zealand obese (NZO) mice.

Schwenk RW, Baumeier C, Finan B, Kluth O, Brauer C, Joost HG, DiMarchi RD, Tschöp MH, Schürmann A.

Diabetologia. 2015 Mar;58(3):604-14. doi: 10.1007/s00125-014-3478-3. Epub 2014 Dec 20.

49.

A rationally designed monomeric peptide triagonist corrects obesity and diabetes in rodents.

Finan B, Yang B, Ottaway N, Smiley DL, Ma T, Clemmensen C, Chabenne J, Zhang L, Habegger KM, Fischer K, Campbell JE, Sandoval D, Seeley RJ, Bleicher K, Uhles S, Riboulet W, Funk J, Hertel C, Belli S, Sebokova E, Conde-Knape K, Konkar A, Drucker DJ, Gelfanov V, Pfluger PT, Müller TD, Perez-Tilve D, DiMarchi RD, Tschöp MH.

Nat Med. 2015 Jan;21(1):27-36. doi: 10.1038/nm.3761. Epub 2014 Dec 8.

PMID:
25485909
50.

Chemical synthesis of insulin analogs through a novel precursor.

Zaykov AN, Mayer JP, Gelfanov VM, DiMarchi RD.

ACS Chem Biol. 2014 Mar 21;9(3):683-91. doi: 10.1021/cb400792s. Epub 2014 Jan 2.

PMID:
24328449

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