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

DiMarchi RD.

Mol Metab. 2018 Oct 12. pii: S2212-8778(18)30972-4. doi: 10.1016/j.molmet.2018.10.004. [Epub ahead of print] No abstract available.


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

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

J Intern Med. 2018 Sep 19. doi: 10.1111/joim.12837. [Epub ahead of print]


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


Peptide lipidation stabilizes structure to enhance biological function.

Ward BP, Ottaway NL, Perez-Tilve D, Ma D, Gelfanov VM, Tschöp MH, Dimarchi RD.

Mol Metab. 2013 Sep 5;2(4):468-79. doi: 10.1016/j.molmet.2013.08.008. eCollection 2013.


A hydrophobic site on the GLP-1 receptor extracellular domain orients the peptide ligand for signal transduction.

Patterson JT, Li P, Day JW, Gelfanov VM, Dimarchi RD.

Mol Metab. 2013 Jan 16;2(2):86-91. doi: 10.1016/j.molmet.2013.01.003. eCollection 2013.


GLP-1R responsiveness predicts individual gastric bypass efficacy on glucose tolerance in rats.

Habegger KM, Heppner KM, Amburgy SE, Ottaway N, Holland J, Raver C, Bartley E, Müller TD, Pfluger PT, Berger J, Toure M, Benoit SC, Dimarchi RD, Perez-Tilve D, D'Alessio DA, Seeley RJ, Tschöp MH.

Diabetes. 2014 Feb;63(2):505-13. doi: 10.2337/db13-0511. Epub 2013 Nov 1.


Unimolecular dual incretins maximize metabolic benefits in rodents, monkeys, and humans.

Finan B, Ma T, Ottaway N, Müller TD, Habegger KM, Heppner KM, Kirchner H, Holland J, Hembree J, Raver C, Lockie SH, Smiley DL, Gelfanov V, Yang B, Hofmann S, Bruemmer D, Drucker DJ, Pfluger PT, Perez-Tilve D, Gidda J, Vignati L, Zhang L, Hauptman JB, Lau M, Brecheisen M, Uhles S, Riboulet W, Hainaut E, Sebokova E, Conde-Knape K, Konkar A, DiMarchi RD, Tschöp MH.

Sci Transl Med. 2013 Oct 30;5(209):209ra151. doi: 10.1126/scitranslmed.3007218.


GLP-1R agonism enhances adjustable gastric banding in diet-induced obese rats.

Habegger KM, Kirchner H, Yi CX, Heppner KM, Sweeney D, Ottaway N, Holland J, Amburgy S, Raver C, Krishna R, Müller TD, Perez-Tilve D, Pfluger PT, Obici S, DiMarchi RD, D'Alessio DA, Seeley RJ, Tschöp MH.

Diabetes. 2013 Sep;62(9):3261-7. doi: 10.2337/db13-0117. Epub 2013 Jun 17.


Discovery of high potency, single-chain insulin analogs with a shortened B-chain and nonpeptide linker.

Kaur ZP, Ochman AR, Mayer JP, Gelfanov VM, DiMarchi RD.

ACS Chem Biol. 2013 Aug 16;8(8):1822-9. doi: 10.1021/cb4002624. Epub 2013 Jun 18.


Glucagon-like peptide-1 receptor-mediated endosomal cAMP generation promotes glucose-stimulated insulin secretion in pancreatic β-cells.

Kuna RS, Girada SB, Asalla S, Vallentyne J, Maddika S, Patterson JT, Smiley DL, DiMarchi RD, Mitra P.

Am J Physiol Endocrinol Metab. 2013 Jul 15;305(2):E161-70. doi: 10.1152/ajpendo.00551.2012. Epub 2013 Apr 16.


Allosteric inhibition of a zinc-sensing transcriptional repressor: insights into the arsenic repressor (ArsR) family.

Campanello GC, Ma Z, Grossoehme NE, Guerra AJ, Ward BP, Dimarchi RD, Ye Y, Dann CE 3rd, Giedroc DP.

J Mol Biol. 2013 Apr 12;425(7):1143-57. doi: 10.1016/j.jmb.2013.01.018. Epub 2013 Jan 23.


Fibroblast growth factor 21 mediates specific glucagon actions.

Habegger KM, Stemmer K, Cheng C, Müller TD, Heppner KM, Ottaway N, Holland J, Hembree JL, Smiley D, Gelfanov V, Krishna R, Arafat AM, Konkar A, Belli S, Kapps M, Woods SC, Hofmann SM, D'Alessio D, Pfluger PT, Perez-Tilve D, Seeley RJ, Konishi M, Itoh N, Kharitonenkov A, Spranger J, DiMarchi RD, Tschöp MH.

Diabetes. 2013 May;62(5):1453-63. doi: 10.2337/db12-1116. Epub 2013 Jan 10.


Targeted estrogen delivery reverses the metabolic syndrome.

Finan B, Yang B, Ottaway N, Stemmer K, Müller TD, Yi CX, Habegger K, Schriever SC, García-Cáceres C, Kabra DG, Hembree J, Holland J, Raver C, Seeley RJ, Hans W, Irmler M, Beckers J, de Angelis MH, Tiano JP, Mauvais-Jarvis F, Perez-Tilve D, Pfluger P, Zhang L, Gelfanov V, DiMarchi RD, Tschöp MH.

Nat Med. 2012 Dec;18(12):1847-56. doi: 10.1038/nm.3009. Epub 2012 Nov 11.


Outstanding Scientific Achievement Award Lecture 2011: defeating diabesity: the case for personalized combinatorial therapies.

Tschöp MH, DiMarchi RD.

Diabetes. 2012 Jun;61(6):1309-14. doi: 10.2337/db12-0272. No abstract available.


FGF21 analogs of sustained action enabled by orthogonal biosynthesis demonstrate enhanced antidiabetic pharmacology in rodents.

Mu J, Pinkstaff J, Li Z, Skidmore L, Li N, Myler H, Dallas-Yang Q, Putnam AM, Yao J, Bussell S, Wu M, Norman TC, Rodriguez CG, Kimmel B, Metzger JM, Manibusan A, Lee D, Zaller DM, Zhang BB, DiMarchi RD, Berger JP, Axelrod DW.

Diabetes. 2012 Feb;61(2):505-12. doi: 10.2337/db11-0838. Epub 2011 Dec 30.


Functional association of the N-terminal residues with the central region in glucagon-related peptides.

Patterson JT, Day JW, Gelfanov VM, DiMarchi RD.

J Pept Sci. 2011 Oct;17(10):659-66. doi: 10.1002/psc.1385. Epub 2011 Jun 10.


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