Carrie Haskell-Luevano

1994 …2021

Research output per year

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Research Output

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Article
2020

Single Nucleotide Polymorphisms in the Melanocortin His-Phe-Arg-Trp Sequences Decrease Tetrapeptide Potency and Efficacy

Winget, M. D., Ericson, M. D., Freeman, K. T. & Haskell-Luevano, C., Mar 12 2020, In : ACS Medicinal Chemistry Letters. 11, 3, p. 272-277 6 p.

Research output: Contribution to journalArticle

2019

Developing a Biased Unmatched Bivalent Ligand (BUmBL) Design Strategy to Target the GPCR Homodimer Allosteric Signaling (cAMP over β-Arrestin 2 Recruitment) Within the Melanocortin Receptors

Lensing, C. J., Freeman, K. T., Schnell, S. M., Speth, R. C., Zarth, A. T. & Haskell-Luevano, C., Jan 10 2019, In : Journal of medicinal chemistry. 62, 1, p. 144-158 15 p.

Research output: Contribution to journalArticle

Open Access
4 Scopus citations

Discovery of Polypharmacological Melanocortin-3 and -4 Receptor Probes and Identification of a 100-Fold Selective nM MC3R Agonist versus a μm MC4R Partial Agonist

Fleming, K. A., Freeman, K. T., Powers, M. D., Santos, R. G., Debevec, G., Giulianotti, M. A., Houghten, R. A., Doering, S. R., Pinilla, C. & Haskell-Luevano, C., Mar 14 2019, In : Journal of medicinal chemistry. 62, 5, p. 2738-2749 12 p.

Research output: Contribution to journalArticle

1 Scopus citations

Structure–activity relationships of the tetrapeptide Ac-His-Arg-(Pi)Dphe-TiC-NH2 at the mouse melanocortin receptors: Modification at the (PI)DPhe position leads to MMC3R versus MMC4R selective ligands

Schlasner, K. N., Ericson, M. D., Doering, S. R., Freeman, K. T., Weinrich, M. & Haskell-Luevano, C., Apr 13 2019, In : Molecules. 24, 8, 1463.

Research output: Contribution to journalArticle

Open Access
2018

1,2,3-Triazole Rings as a Disulfide Bond Mimetic in Chimeric AGRP-Melanocortin Peptides: Design, Synthesis, and Functional Characterization

Tala, S. R., Singh, A., Lensing, C. J., Schnell, S. M., Freeman, K. T., Rocca, J. R. & Haskell-Luevano, C., May 16 2018, In : ACS Chemical Neuroscience. 9, 5, p. 1001-1013 13 p.

Research output: Contribution to journalArticle

Open Access
8 Scopus citations
Open Access
1 Scopus citations

Comparative in Vivo Investigation of Intrathecal and Intracerebroventricular Administration with Melanocortin Ligands MTII and AGRP into Mice

Adank, D. N., Lunzer, M. M., Lensing, C. J., Wilber, S. L., Gancarz, A. M. & Haskell-Luevano, C., Feb 21 2018, In : ACS Chemical Neuroscience. 9, 2, p. 320-327 8 p.

Research output: Contribution to journalArticle

Open Access
5 Scopus citations

Discovery of Melanocortin Ligands via a Double Simultaneous Substitution Strategy Based on the Ac-His-DPhe-Arg-Trp-NH2 Template

Todorovic, A., Lensing, C. J., Holder, J. R., Scott, J. W., Sorensen, N. B. & Haskell-Luevano, C., Nov 21 2018, In : ACS Chemical Neuroscience. 9, 11, p. 2753-2766 14 p.

Research output: Contribution to journalArticle

Open Access

Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors

Ericson, M. D., Singh, A., Tala, S. R., Haslach, E. M., Dirain, M. L. S., Schaub, J. W., Flores, V., Eick, N., Lensing, C. J., Freeman, K. T., Smeester, B. A., Adank, D. N., Wilber, S. L., Speth, R. & Haskell-Luevano, C., Apr 26 2018, In : Journal of Medicinal Chemistry. 61, 8, p. 3738-3744 7 p.

Research output: Contribution to journalArticle

Open Access
1 Scopus citations
Open Access
7 Scopus citations
Open Access
1 Scopus citations
2017

A Direct in Vivo Comparison of the Melanocortin Monovalent Agonist Ac-His-DPhe-Arg-Trp-NH2 versus the Bivalent Agonist Ac-His-DPhe-Arg-Trp-PEDG20-His-DPhe-Arg-Trp-NH2: A Bivalent Advantage

Lensing, C. J., Adank, D. N., Wilber, S. L., Freeman, K. T., Schnell, S. M., Speth, R. C., Zarth, A. T. & Haskell-Luevano, C., Jun 21 2017, In : ACS Chemical Neuroscience. 8, 6, p. 1262-1278 17 p.

Research output: Contribution to journalArticle

Open Access
6 Scopus citations

A macrocyclic agouti-related protein/[Nle4,DPhe7]α-melanocyte stimulating hormone chimeric scaffold produces subnanomolar melanocortin receptor ligands

Ericson, M. D., Freeman, K. T., Schnell, S. M. & Haskell-Luevano, C., Jan 26 2017, In : Journal of Medicinal Chemistry. 60, 2, p. 805-813 9 p.

Research output: Contribution to journalArticle

Open Access
4 Scopus citations

Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa1-Arg-(pI)DPhe-Xaa4-NH2

Doering, S. R., Freeman, K. T., Schnell, S. M., Haslach, E. M., Dirain, M., Debevec, G., Geer, P., Santos, R. G., Giulianotti, M. A., Pinilla, C., Appel, J. R., Speth, R. C., Houghten, R. A. & Haskell-Luevano, C., May 25 2017, In : Journal of medicinal chemistry. 60, 10, p. 4342-4357 16 p.

Research output: Contribution to journalArticle

Open Access
4 Scopus citations
Open Access
5 Scopus citations
2016

Ac-Trp-DPhe(p-I)-Arg-Trp-NH2, a 250-Fold Selective Melanocortin-4 Receptor (MC4R) Antagonist over the Melanocortin-3 Receptor (MC3R), Affects Energy Homeostasis in Male and Female Mice Differently

Lensing, C. J., Adank, D. N., Doering, S. R., Wilber, S. L., Andreasen, A., Schaub, J. W., Xiang, Z. & Haskell-Luevano, C., Sep 21 2016, In : ACS Chemical Neuroscience. 7, 9, p. 1283-1291 9 p.

Research output: Contribution to journalArticle

14 Scopus citations

An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers

Lensing, C. J., Freeman, K. T., Schnell, S. M., Adank, D. N., Speth, R. C. & Haskell-Luevano, C., Apr 28 2016, In : Journal of medicinal chemistry. 59, 7, p. 3112-3128 17 p.

Research output: Contribution to journalArticle

21 Scopus citations

Comparative Functional Alanine Positional Scanning of the α-Melanocyte Stimulating Hormone and NDP-Melanocyte Stimulating Hormone Demonstrates Differential Structure-Activity Relationships at the Mouse Melanocortin Receptors

Todorovic, A., Ericson, M. D., Palusak, R. D., Sorensen, N. B., Wood, M. S., Xiang, Z. & Haskell-Luevano, C., Jul 20 2016, In : ACS Chemical Neuroscience. 7, 7, p. 984-994 11 p.

Research output: Contribution to journalArticle

3 Scopus citations

Synthesis and Structure-Activity Relationships of Substituted Urea Derivatives on Mouse Melanocortin Receptors

Singh, A., Kast, J., Dirain, M. L. S., Huang, H. & Haskell-Luevano, C., Feb 17 2016, In : ACS Chemical Neuroscience. 7, 2, p. 196-205 10 p.

Research output: Contribution to journalArticle

2 Scopus citations
2015

A fragment of the Escherichia coli ClpB heat-shock protein is a micromolar melanocortin 1 receptor agonist

Ericson, M. D., Schnell, S. M., Freeman, K. T. & Haskell-Luevano, C., Nov 15 2015, In : Bioorganic and Medicinal Chemistry Letters. 25, 22, p. 5306-5308 3 p.

Research output: Contribution to journalArticle

19 Scopus citations

Csf2 and Ptgs2 epigenetic dysregulation in diabetesprone bicongenic B6.NODC11bxC1tb mice

Garrigan, E., Belkin, N. S., Seydel, F., Han, Z., Carter, J., McDuffie, M., Morel, L., Peck, A. B., Clare-Salzler, M. J., Atkinson, M., Wasserfall, C., Davoodi-Semiromi, A., Shi, J. D., Haskell-Luevano, C., Yang, L. J., Alexander, J. J., Cdebaca, A., Piliant, T., Riggs, C., Amick, M. & 2 others, Litherland, S. A. & Bober, R., Jan 1 2015, In : Genetics and Epigenetics. 1, 7, p. 5-17 13 p.

Research output: Contribution to journalArticle

1 Scopus citations
17 Scopus citations

Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor

Doering, S. R., Todorovic, A. & Haskell-Luevano, C., Feb 12 2015, In : ACS Medicinal Chemistry Letters. 6, 2, p. 123-127 5 p.

Research output: Contribution to journalArticle

12 Scopus citations

Microwave-assisted solid-phase synthesis of side-chain to side-chain lactam-bridge cyclic peptides

Tala, S. R., Schnell, S. M. & Haskell-Luevano, C., Dec 15 2015, In : Bioorganic and Medicinal Chemistry Letters. 25, 24, p. 5708-5711 4 p.

Research output: Contribution to journalArticle

17 Scopus citations

Synthesis and pharmacology of α/β3-peptides based on the melanocortin agonist Ac-His-d Phe-Arg-Trp-NH2 sequence

Singh, A., Tala, S. R., Flores, V., Freeman, K. & Haskell-Luevano, C., May 14 2015, In : ACS Medicinal Chemistry Letters. 6, 5, p. 568-572 5 p.

Research output: Contribution to journalArticle

16 Scopus citations
2014

1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: Design, synthesis, conformational analysis, and biological activity

Testa, C., Scrima, M., Grimaldi, M., D'Ursi, A. M., Dirain, M. L., Lubin-Germain, N., Singh, A., Haskell-Luevano, C., Chorev, M., Rovero, P. & Papini, A. M., Nov 26 2014, In : Journal of medicinal chemistry. 57, 22, p. 9424-9434 11 p.

Research output: Contribution to journalArticle

28 Scopus citations

Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R Human Melanocortin-4 Polymorphic Receptors (hMC4Rs)

Haslach, E. M., Huang, H., Dirain, M., Debevec, G., Geer, P., Santos, R. G., Giulianotti, M. A., Pinilla, C., Appel, J. R., Doering, S. R., Walters, M. A., Houghten, R. A. & Haskell-Luevano, C., Jun 12 2014, In : Journal of medicinal chemistry. 57, 11, p. 4615-4628 14 p.

Research output: Contribution to journalArticle

13 Scopus citations
10 Scopus citations
2013
7 Scopus citations
2011

Incorporation of a bioactive reverse-turn heterocycle into a peptide template using solid-phase synthesis to probe melanocortin receptor selectivity and ligand conformations by 2D 1H NMR

Singh, A., Wilczynski, A., Holder, J. R., Witek, R. M., Dirain, M. L., Xiang, Z., Edison, A. S. & Haskell-Luevano, C., Mar 10 2011, In : Journal of Medicinal Chemistry. 54, 5, p. 1379-1390 12 p.

Research output: Contribution to journalArticle

14 Scopus citations

Use of chimeric melanocortin-2 and -4 receptors to identify regions responsible for ligand specificity and dependence on melanocortin 2 receptor accessory protein

Hinkle, P. M., Serasinghe, M. N., Jakabowski, A., Sebag, J. A., Wilson, K. R. & Haskell-Luevano, C., Jun 11 2011, In : European Journal of Pharmacology. 660, 1, p. 94-102 9 p.

Research output: Contribution to journalArticle

13 Scopus citations
2010

Effect of MTII on food intake and brain c-Fos in melanocortin-3, melanocortin-4, and double MC3 and MC4 receptor knockout mice

Rowland, N. E., Schaub, J. W., Robertson, K. L., Andreasen, A. & Haskell-Luevano, C., Dec 1 2010, In : Peptides. 31, 12, p. 2314-2317 4 p.

Research output: Contribution to journalArticle

29 Scopus citations

Effect of serotonergic anorectics on food intake and induction of Fos in brain of mice with disruption of melanocortin 3 and/or 4 receptors

Rowland, N. E., Fakhar, K. J., Robertson, K. L. & Haskell-Luevano, C., Nov 1 2010, In : Pharmacology Biochemistry and Behavior. 97, 1, p. 107-111 5 p.

Research output: Contribution to journalArticle

12 Scopus citations

Food demand and meal size in mice with single or combined disruption of melanocortin type 3 and 4 receptors

Atalayer, D., Robertson, K. L., Haskell-Luevano, C., Andreasen, A. & Rowland, N. E., Jun 1 2010, In : American Journal of Physiology - Regulatory Integrative and Comparative Physiology. 298, 6, p. R1667-R1674

Research output: Contribution to journalArticle

37 Scopus citations
33 Scopus citations

The effect of backbone cyclization on PK/PD properties of bioactive peptide-peptoid hybrids: The melanocortin agonist paradigm

Ovadia, O., Linde, Y., Haskell-Luevano, C., Dirain, M. L., Sheynis, T., Jelinek, R., Gilon, C. & Hoffman, A., Jan 15 2010, In : Bioorganic and Medicinal Chemistry. 18, 2, p. 580-589 10 p.

Research output: Contribution to journalArticle

25 Scopus citations

γ2-Melanocyte stimulation hormone (γ2- MSH) truncation studies results in the cautionary note that γ2- MSH is not selective for the mouse MC3R over the mouse MC5R

Joseph, C. G., Yao, H., Scott, J. W., Sorensen, N. B., Marnane, R. N., Mountjoy, K. G. & Haskell-Luevano, C., Dec 1 2010, In : Peptides. 31, 12, p. 2304-2313 10 p.

Research output: Contribution to journalArticle

10 Scopus citations

Construction and characterization of melanocortin-2 and -4 receptor chimeras.

Wilson, K. R., Proneth, B., Luesch, H., Litherland, S. A. & Haskell-Luevano, C., 2009, In : Advances in experimental medicine and biology. 611, p. 301-302 2 p.

Research output: Contribution to journalArticle

Discovery of a ligand that compensates for decreased endogenous agonist potency of melanocortin-4 receptor polymorphisms identified in obese humans.

Haskell-Luevano, C., Xiang, Z., Wilczynski, A. M., Haskell, K. R., Andreasen, A. M., Litherland, S. A., Millard, W. J., Pogozheva, I. D., Mosberg, H. I. & Sorenson, N. B., 2009, In : Advances in Experimental Medicine and Biology. 611, p. 509-510 2 p.

Research output: Contribution to journalArticle

Functional characterization and structural modeling of obesity associated mutations in the melanocortin 4 receptor

Tan, K., Pogozheva, I. D., Yeo, G. S. H., Hadaschik, D., Keogh, J. M., Haskell-Leuvano, C., O'Rahilly, S., Mosberg, H. I. & Farooqi, I. S., Jan 1 2009, In : Endocrinology. 150, 1, p. 114-125 12 p.

Research output: Contribution to journalArticle

54 Scopus citations

Prevalence of pathogenetic MC4R mutations in Italian children with early Onset obesity, tall stature and familial history of obesity

Santoro, N., Cirillo, G., Xiang, Z., Tanas, R., Greggio, N., Morino, G., Iughetti, L., Vottero, A., Salvatoni, A., Di Pietro, M., Balsamo, A., Crinò, A., Grandone, A., Haskell-Luevano, C., Perrone, L. & del Giudice, E. M., Mar 12 2009, In : BMC medical genetics. 10, 25.

Research output: Contribution to journalArticle

21 Scopus citations

Semi-rigid tripeptide agonists of melanocortin receptors

Ruwe, A. R., Koikov, L., Abdel-Malek, Z., Haskell-Luevano, C., Dirain, M. L., Portillo, F., Xiang, Z., Wortman, M. & Knittel, J. J., Sep 1 2009, In : Bioorganic and Medicinal Chemistry Letters. 19, 17, p. 5176-5181 6 p.

Research output: Contribution to journalArticle

2 Scopus citations

Voluntary exercise prevents the obese and diabetic metabolic syndrome of the melanocortin-4 receptor knockout mouse

Haskell-Luevano, C., Schaub, J. W., Andreasen, A., Haskell, K. R., Moore, M. C., Koerper, L. M., Rouzaud, F., Baker, H. V., Millard, W. J., Walter, G., Litherland, S. A. & Xiang, Z., Feb 1 2009, In : FASEB Journal. 23, 2, p. 642-655 14 p.

Research output: Contribution to journalArticle

50 Scopus citations

α-MSH tripeptide analogs activate the melanocortin 1 receptor and reduce UV-induced DNA damage in human melanocytes

Abdel-Malek, Z. A., Ruwe, A., Kavanagh-Starner, R., Kadekaro, A. L., Swope, V., Haskell-Luevano, C., Koikov, L. & Knittel, J. J., Oct 1 2009, In : Pigment Cell and Melanoma Research. 22, 5, p. 635-644 10 p.

Research output: Contribution to journalArticle

56 Scopus citations

β-Turn secondary structure and melanocortin ligands

Haslach, E. M., Schaub, J. W. & Haskell-Luevano, C., Feb 1 2009, In : Bioorganic and Medicinal Chemistry. 17, 3, p. 952-958 7 p.

Research output: Contribution to journalArticle

7 Scopus citations
2008

Backbone cyclic peptidomimetic melanocortin-4 receptor agonist as a novel orally administrated drug lead for treating obesity

Hess, S., Linde, Y., Ovadia, O., Safrai, E., Shalev, D. E., Swed, A., Halbfinger, E., Lapidot, T., Winkler, I., Gabinet, Y., Faier, A., Yarden, D., Xiang, Z., Portillo, F. P., Haskell-Luevano, C., Gilon, C. & Hoffman, A., Feb 28 2008, In : Journal of Medicinal Chemistry. 51, 4, p. 1026-1034 9 p.

Research output: Contribution to journalArticle

65 Scopus citations

Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-Nïb modified at the para position of the benzyl side chain (DPhe): Importance for mouse melanocortin-3 receptor agonist versus antagonist activity

Proneth, B., Pogozheva, I. D., Portillo, F. P., Mosberg, H. I. & Haskell-Luevano, C., Sep 25 2008, In : Journal of Medicinal Chemistry. 51, 18, p. 5585-5593 9 p.

Research output: Contribution to journalArticle

13 Scopus citations

Structure-activity relationship and metabolic stability studies of Backbone cyclization and N-methylation of melanocortin peptides

Linde, Y., Ovadia, O., Safrai, E., Xiang, Z., Portillo, F. P., Shalev, D. E., Haskell-Luevano, C., Hoffman, A. & Gilon, C., Dec 1 2008, In : Biopolymers - Peptide Science Section. 90, 5, p. 671-682 12 p.

Research output: Contribution to journalArticle

34 Scopus citations