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• 2020

  Development of Ligand-Drug Conjugates Targeting Melanoma through the Overexpressed Melanocortin 1 Receptor

  Zhou, Y., Mowlazadeh Haghighi, S., Liu, Z., Wang, L., Hruby, V. J. & Cai, M., Oct 9 2020, In: ACS Pharmacology and Translational Science. 3, 5, p. 921-930 10 p.

  Research output: Contribution to journal › Article › peer-review

  • melanotan-II
  • Receptor, Melanocortin, Type 1
  • Drug Delivery Systems
  • Melanoma
  • Ligands

• Development of novel frog-skin peptide scaffolds with selectivity towards melanocortin receptor subtypes

  Malik, U., Chan, L. Y., Cai, M., Hruby, V. J., Kaas, Q., Daly, N. L. & Craik, D. J., 2020, (Accepted/In press) In: Peptide Science.

  Research output: Contribution to journal › Article › peer-review

  • ranacyclin T
  • Melanocortin Receptors
  • Ligands
  • Peptides
  • Scaffolds

• Melanocortin 3 receptor activation with [D-Trp8]-γ-MSH suppresses inflammation in apolipoprotein E deficient mice

  Kadiri, J. J., Thapa, K., Kaipio, K., Cai, M., Hruby, V. J. & Rinne, P., Aug 5 2020, In: European Journal of Pharmacology. 880, 173186.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  • Receptor, Melanocortin, Type 3
  • Melanocyte-Stimulating Hormones
  • Apolipoproteins E
  • Melanocortin Receptors
  • Aorta
• 2019

  Development of N-acetylated dipalmitoyl-S-glyceryl cysteine analogs as efficient TLR2/TLR6 agonists

  Zhou, Y., Banday, A. H., Hruby, V. J. & Cai, M., Sep 27 2019, In: Molecules. 24, 19, 3512.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  • S-(2,3-bis(palmitoyloxy)propyl)cysteine
  • vaccines
  • cysteine
  • analogs
  • Synthetic Vaccines
  1 Scopus citations

• Multivalent peptide and peptidomimetic ligands for the treatment of pain without toxicities and addiction

  Hruby, V. J., Jun 1 2019, In: Peptides. 116, p. 63-67 5 p.

  Research output: Contribution to journal › Review article › peer-review

  • Peptidomimetics
  • Toxicity
  • Ligands
  • Bioactivity
  • Peptides
  4 Scopus citations

• Toward a Universal μ-Agonist Template for Template-Based Alignment Modeling of Opioid Ligands

  Wu, Z. & Hruby, V. J., Oct 22 2019, In: ACS Omega. 4, 17, p. 17457-17476 20 p.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  • Ligands
  • Opioid Analgesics
  • Scaffolds
  • G-Protein-Coupled Receptors
  • Morphine
  2 Scopus citations
• 2018

  Correction: Design of MC1R Selective γ-MSH Analogues with Canonical Amino Acids Leads to Potency and Pigmentation (Journal of Medicinal Chemistry (2017) 60 (9320-9329) DOI: 10.1021/acs.jmedchem.7b01295)

  Zhou, Y., Mowlazadeh Haghighi, S., Zoi, I., Sawyer, J. R., Hruby, V. J. & Cai, M., Oct 11 2018, In: Journal of Medicinal Chemistry. 61, 19, p. 8945 1 p.

  Research output: Contribution to journal › Comment/debate › peer-review

  • Melanocyte-Stimulating Hormones
  • Pharmaceutical Chemistry
  • Lizards
  • Pigmentation
  • Ether

• Cyclic biphalin analogues with a novel linker lead to potent agonist activities at mu, delta, and kappa opioid receptors

  Remesic, M., Macedonio, G., Mollica, A., Porreca, F., Hruby, V. & Lee, Y. S., Jul 23 2018, In: Bioorganic and Medicinal Chemistry. 26, 12, p. 3664-3667 4 p.

  Research output: Contribution to journal › Article › peer-review

  • biphalin
  • kappa Opioid Receptor
  • delta Opioid Receptor
  • mu Opioid Receptor
  • Opioid Receptors
  3 Scopus citations

• Development of Macrocyclic Peptidomimetics Containing Constrained α,α-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors

  Merlino, F., Zhou, Y., Cai, M., Carotenuto, A., Yousif, A. M., Brancaccio, D., Di Maro, S., Zappavigna, S., Limatola, A., Novellino, E., Grieco, P. & Hruby, V. J., May 10 2018, In: Journal of Medicinal Chemistry. 61, 9, p. 4263-4269 7 p.

  Research output: Contribution to journal › Article › peer-review

  • Melanocortin Receptors
  • Peptidomimetics
  • Melanocortins
  • amino acids
  • Human Activities
  3 Scopus citations

• Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1

  Durek, T., Cromm, P. M., White, A. M., Schroeder, C. I., Kaas, Q., Weidmann, J., Ahmad Fuaad, A., Cheneval, O., Harvey, P. J., Daly, N. L., Zhou, Y., Dellsén, A., Österlund, T., Larsson, N., Knerr, L., Bauer, U., Kessler, H., Cai, M., Hruby, V. J., Plowright, A. T. & 1 others, Craik, D. J., Apr 26 2018, In: Journal of Medicinal Chemistry. 61, 8, p. 3674-3684 11 p.

  Research output: Contribution to journal › Article › peer-review

  • sunflower SFTI-1 peptide
  • Melanocortin Receptors
  • Cyclic Peptides
  • Methylation
  • Peptides
  12 Scopus citations

• Genetic and pharmacological antagonism of NK₁ receptor prevents opiate abuse potential

  Sandweiss, A. J., McIntosh, M. I., Moutal, A., Davidson-Knapp, R., Hu, J., Giri, A. K., Yamamoto, T., Hruby, V. J., Khanna, R., Largent-Milnes, T. M. & Vanderah, T. W., Aug 1 2018, In: Molecular Psychiatry. 23, 8, p. 1745-1755 11 p.

  Research output: Contribution to journal › Article › peer-review

  • Ventral Tegmental Area
  • Opioid-Related Disorders
  • Substance P
  • Morphine
  • Analgesics
  11 Scopus citations

• Hypothalamic γ-melanocyte stimulating hormone gene delivery reduces fat mass in male mice

  Eerola, K., Virtanen, S., Vähätalo, L., Ailanen, L., Cai, M., Hruby, V., Savontaus, M. & Savontaus, E., Oct 1 2018, In: Journal of Endocrinology. 239, 1, p. 19-31 13 p.

  Research output: Contribution to journal › Article › peer-review

  • Melanocyte-Stimulating Hormones
  • Arcuate Nucleus of Hypothalamus
  • Receptor, Melanocortin, Type 3
  • Western Diet
  • Fats
  2 Scopus citations

• Protection against β-amyloid neurotoxicity by a non-toxic endogenous N-terminal β-amyloid fragment and its active hexapeptide core sequence

  Forest, K. H., Alfulaij, N., Arora, K., Taketa, R., Sherrin, T., Todorovic, C., Lawrence, J. L. M., Yoshikawa, G. T., Ng, H. L., Hruby, V. J. & Nichols, R. A., Jan 2018, In: Journal of neurochemistry. 144, 2, p. 201-217 17 p.

  Research output: Contribution to journal › Article › peer-review

  • Oligomers
  • Memory Disorders
  • Cells
  • Amyloid
  • Fear
  8 Scopus citations

• Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH₂, leads to hMC1R selectivity and pigmentation

  Mowlazadeh Haghighi, S., Zhou, Y., Dai, J., Sawyer, J. R., Hruby, V. J. & Cai, M., May 10 2018, In: European journal of medicinal chemistry. 151, p. 815-823 9 p.

  Research output: Contribution to journal › Article › peer-review

  • acetyl-histidyl-phenylalanyl-arginyl-tryptophanamide
  • Melanocyte-Stimulating Hormones
  • Pigmentation
  • Skin Neoplasms
  • Skin
  5 Scopus citations

• Synthesis and Evaluation of a Novel Bivalent Selective Antagonist for the Mu-Delta Opioid Receptor Heterodimer that Reduces Morphine Withdrawal in Mice

  Olson, K. M., Keresztes, A., Tashiro, J. K., Daconta, L. V., Hruby, V. J. & Streicher, J. M., Jul 26 2018, In: Journal of Medicinal Chemistry. 61, 14, p. 6075-6086 12 p.

  Research output: Contribution to journal › Article › peer-review

  • delta Opioid Receptor
  • mu Opioid Receptor
  • Morphine
  • CYM51010
  • enkephalin, Ser(2), Leu(5), Thr(6)-
  13 Scopus citations
• 2017

  Design of MC1R Selective γ-MSH Analogues with Canonical Amino Acids Leads to Potency and Pigmentation

  Zhou, Y., Mowlazadeh Haghighi, S., Zoi, I., Sawyer, J. R., Hruby, V. J. & Cai, M., Nov 22 2017, In: Journal of Medicinal Chemistry. 60, 22, p. 9320-9329 10 p.

  Research output: Contribution to journal › Article › peer-review

  • Receptor, Melanocortin, Type 1
  • Melanocyte-Stimulating Hormones
  • Pigmentation
  • Amino Acids
  • Melanoma
  9 Scopus citations

• Fluorescent-labeled bioconjugates of the opioid peptides biphalin and DPDPE incorporating fluorescein-maleimide linkers

  Stefanucci, A., Lei, W., Hruby, V. J., Macedonio, G., Luisi, G., Carradori, S., Streicher, J. M. & Mollica, A., Jun 1 2017, In: Future Medicinal Chemistry. 9, 9, p. 859-869 11 p.

  Research output: Contribution to journal › Article › peer-review

  • biphalin
  • fluorescein 5-maleimide
  • D-Penicillamine (2,5)-Enkephalin
  • Opioid Peptides
  • Enkephalins
  14 Scopus citations

• Melanocortin 1 Receptor Signaling Regulates Cholesterol Transport in Macrophages

  Rinne, P., Rami, M., Nuutinen, S., Santovito, D., Van Der Vorst, E. P. C., Guillamat-Prats, R., Lyytikäinen, L. P., Raitoharju, E., Oksala, N., Ring, L., Cai, M., Hruby, V. J., Lehtimäki, T., Weber, C. & Steffens, S., Jul 4 2017, In: Circulation. 136, 1, p. 83-97 15 p.

  Research output: Contribution to journal › Article › peer-review

  • Receptor, Melanocortin, Type 1
  • Cholesterol
  • Macrophages
  • Melanocyte-Stimulating Hormones
  • Foam Cells
  18 Scopus citations

• Recent Advances in the Realm of Allosteric Modulators for Opioid Receptors for Future Therapeutics

  Remesic, M., Hruby, V. J., Porreca, F. & Lee, Y. S., Jun 21 2017, In: ACS Chemical Neuroscience. 8, 6, p. 1147-1158 12 p.

  Research output: Contribution to journal › Review article › peer-review

  • Opioid Receptors
  • Modulators
  • Opioid Analgesics
  • Ligands
  • Allosteric Site
  20 Scopus citations

• Reversed-phase high-performance liquid chromatography for the separation of peptide diastereoisomers

  Hruby, V. J., Kawasaki, A. & Toth, G., Jan 1 2017, High-Performance Liquid Chromatography of Peptides and Proteins: Separation, Analysis, and Conformation. CRC Press, p. 379-388 10 p.

  Research output: Chapter in Book/Report/Conference proceeding › Chapter

  • High performance liquid chromatography
  • Peptides
  • Reverse-Phase Chromatography
  • High Pressure Liquid Chromatography
  • Amino acids
  1 Scopus citations

• Structural Insights into Selective Ligand-Receptor Interactions Leading to Receptor Inactivation Utilizing Selective Melanocortin 3 Receptor Antagonists

  Cai, M., Marelli, U. K., Mertz, B., Beck, J. G., Opperer, F., Rechenmacher, F., Kessler, H. & Hruby, V. J., Aug 15 2017, In: Biochemistry. 56, 32, p. 4201-4209 9 p.

  Research output: Contribution to journal › Article › peer-review

  • Receptor, Melanocortin, Type 3
  • Melanocortin Receptors
  • SHU 9119
  • Ligands
  • Peptides
  3 Scopus citations

• Synthesis and Investigation of Mixed μ-Opioid and δ-Opioid Agonists as Possible Bivalent Ligands for Treatment of Pain

  Vardanyan, R. S., Cain, J. P., Haghighi, S. M., Kumirov, V. K., McIntosh, M. I., Sandweiss, A. J., Porreca, F. & Hruby, V. J., 2017, In: Journal of Heterocyclic Chemistry. 54, 2, p. 1228-1235 8 p.

  Research output: Contribution to journal › Article › peer-review

  • Opioid Receptors
  • Opioid Analgesics
  • Analgesics
  • Ligands
  • Enkephalins
  4 Scopus citations
• 2016

  Cyclic non-opioid dynorphin A analogues for the bradykinin receptors

  Lee, Y. S., Remesic, M., Ramos-Colon, C., Hall, S. M., Kuzmin, A., Rankin, D., Porreca, F., Lai, J. & Hruby, V. J., 2016, In: Bioorganic and Medicinal Chemistry Letters. 26, 22, p. 5513-5516 4 p.

  Research output: Contribution to journal › Article › peer-review

  • Bradykinin Receptors
  • Dynorphins
  • Ligands
  • Scaffolds
  • Narcotic Antagonists
  4 Scopus citations

• Cyclic opioid peptides

  Remesic, M., Lee, Y. S. & Hruby, V. J., Apr 1 2016, In: Current medicinal chemistry. 23, 13, p. 1288-1303 16 p.

  Research output: Contribution to journal › Review article › peer-review

  • Cyclic Peptides
  • Opioid Peptides
  • Cyclization
  • Opioid Receptors
  • Biological Availability
  20 Scopus citations

• Design of cyclic peptides with biological activities from biologically active peptides: the case of peptide modulators of melanocortin receptors

  Hruby, V. J., Nov 1 2016, In: Biopolymers. 106, 6, p. 884-888 5 p.

  Research output: Contribution to journal › Article › peer-review

  • Cyclic Peptides
  • Melanocortin Receptors
  • Bioactivity
  • Peptides
  • Modulators
  11 Scopus citations

• Design of cyclized selective melanotropins

  Cai, M. & Hruby, V. J., Nov 1 2016, In: Biopolymers. 106, 6, p. 876-883 8 p.

  Research output: Contribution to journal › Review article › peer-review

  • Melanocyte-Stimulating Hormones
  • Peptides
  • Cyclic Peptides
  • Ligands
  • ACTH (6-9)
  12 Scopus citations

• Design synthesis and structure-activity relationship of 5-substituted (tetrahydronaphthalen-2yl)methyl with N-phenyl-N-(piperidin-2-yl)propionamide derivatives as opioid ligands

  Deekonda, S., Rankin, D., Davis, P., Lai, J., Vanderah, T. W., Porecca, F. & Hruby, V. J., Jan 15 2016, In: Bioorganic and Medicinal Chemistry. 24, 2, p. 85-91 7 p.

  Research output: Contribution to journal › Article › peer-review

  • propionamide
  • Structure-Activity Relationship
  • Opioid Analgesics
  • Derivatives
  • Assays
  2 Scopus citations

• Discovery of Stable Non-opioid Dynorphin A Analogues Interacting at the Bradykinin Receptors for the Treatment of Neuropathic Pain

  Hall, S. M., LeBaron, L., Ramos-Colon, C., Qu, C., Xie, J. Y., Porreca, F., Lai, J., Lee, Y. S. & Hruby, V. J., Dec 21 2016, In: ACS Chemical Neuroscience. 7, 12, p. 1746-1752 7 p.

  Research output: Contribution to journal › Article › peer-review

  • Bradykinin Receptors
  • Dynorphins
  • Neuralgia
  • Rats
  • Isomers
  5 Scopus citations

• Dynorphin A analogs for the treatment of chronic neuropathic pain

  Hall, S. M., Lee, Y. S. & Hruby, V. J., Feb 2016, In: Future Medicinal Chemistry. 8, 2, p. 165-177 13 p.

  Research output: Contribution to journal › Review article › peer-review

  • Dynorphins
  • Neuralgia
  • Chronic Pain
  • Pain
  • Peptides
  6 Scopus citations

• Enkephalin analogues with N-phenyl-N-(piperidin-2-ylmethyl)propionamide derivatives: Synthesis and biological evaluations

  Deekonda, S., Cole, J., Sunna, S., Rankin, D., Largent-Milnes, T. M., Davis, P., Bassirirad, N. M., Lai, J., Vanderah, T. W., Porecca, F. & Hruby, V. J., Jan 1 2016, In: Bioorganic and Medicinal Chemistry Letters. 26, 1, p. 222-227 6 p.

  Research output: Contribution to journal › Article › peer-review

  • propionamide
  • Enkephalins
  • Derivatives
  • Ligands
  • Molecules
  3 Scopus citations

• Enkephalin-fentanyl multifunctional opioids as potential neuroprotectants for ischemic stroke treatment

  Islam, M. R., Yang, L., Lee, Y. S., Hruby, V. J., Karamyan, V. T. & Abbruscato, T. J., Nov 1 2016, In: Current Pharmaceutical Design. 22, 42, p. 6459-6468 10 p.

  Research output: Contribution to journal › Article › peer-review

  • biphalin
  • Enkephalins
  • Fentanyl
  • Neuroprotective Agents
  • Opioid Analgesics
  9 Scopus citations

• Structure-Activity Relationships of [des-Arg⁷]Dynorphin A Analogues at the ΰ Opioid Receptor

  Ramos-Colon, C. N., Lee, Y. S., Remesic, M., Hall, S. M., Lavigne, J., Davis, P., Sandweiss, A. J., McIntosh, M. I., Hanson, J., Largent-Milnes, T. M., Vanderah, T. W., Streicher, J., Porreca, F. & Hruby, V. J., Nov 23 2016, In: Journal of Medicinal Chemistry. 59, 22, p. 10291-10298 8 p.

  Research output: Contribution to journal › Article › peer-review

  • Dynorphins
  • Structure-Activity Relationship
  • Opioid Receptors
  • D-phenylalanyl-D-phenylalanyl-D-norleucyl-N-(4-pyridinylmethyl)-d-argininamide
  • dynorphin A (1-9)
  5 Scopus citations

• The melanocortin receptor system: A target for multiple degenerative diseases

  Cai, M. & Hruby, V. J., Aug 1 2016, In: Current Protein and Peptide Science. 17, 5, p. 488-496 9 p.

  Research output: Contribution to journal › Article › peer-review

  • Melanocortin Receptors
  • Pro-Opiomelanocortin
  • Melanocyte-Stimulating Hormones
  • Ligands
  • Peptides
  16 Scopus citations

• Tumor Targeting and Pharmacokinetics of a Near-Infrared Fluorescent-Labeled δ-Opioid Receptor Antagonist Agent, Dmt-Tic-Cy5

  Huynh, A. S., Estrella, V., Stark, V. E., Cohen, A. S., Chen, T., Casagni, T. J., Josan, J. S., Lloyd, M. C., Johnson, J., Kim, J., Hruby, V. J., Vagner, J. & Morse, D. L., Feb 1 2016, In: Molecular Pharmaceutics. 13, 2, p. 534-544 11 p.

  Research output: Contribution to journal › Article › peer-review

  • 2',6'-dimethyltyrosyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid
  • cyanine dye 5
  • Narcotic Antagonists
  • Pharmacokinetics
  • Opioid Receptors
  9 Scopus citations

• Various modifications of the amphipathic dynorphin A pharmacophore for rat brain bradykinin receptors

  Lee, Y. S., Kupp, R., Remesic, M. V., Ramos-Colon, C., Hall, SM., Chan, C., Rankin, D., Lai, J., Porreca, F. & Hruby, V. J., Oct 1 2016, In: Chemical Biology and Drug Design. p. 615-619 5 p.

  Research output: Contribution to journal › Letter › peer-review

  • Bradykinin Receptors
  • Dynorphins
  • Rats
  • Brain
  • Chronic Pain
  2 Scopus citations