M. Cai

发表

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

V. Hruby, H. Kessler, M. Cai, 2017, Biochemistry.

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.

V. Hruby, M. Cai, J. Dai, 2018, European journal of medicinal chemistry.

Design and microwave-assisted synthesis of novel macrocyclic peptides active at melanocortin receptors: discovery of potent and selective hMC5R receptor antagonists.

E. Novellino, P. Grieco, V. Hruby, 2008, Journal of medicinal chemistry.

Novel approaches to the design of bioavailable melanotropins

M. Cai, Yang Zhou, Minying Cai, 2017, Expert opinion on drug discovery.

Cell Signaling and Trafficking of Human Melanocortin Receptors in Real Time Using Two‐photon Fluorescence and Confocal Laser Microscopy: Differentiation of Agonists and Antagonists

M. Staňková, V. Hruby, M. Cai, 2006, Chemical biology & drug design.

Approaches to the rational design of selective melanocortin receptor antagonists

V. Hruby, M. Cai, Joel Nyberg, 2011, Expert opinion on drug discovery.

Design of novel melanotropin agonists and antagonists with high potency and selectivity for human melanocortin receptors

M. Staňková, Jinfa Ying, V. Hruby, 2005, Peptides.

Characterization of TCP-1 probes for molecular imaging of colon cancer.

A. Rouse, A. Gmitro, B. Banerjee, 2016, Journal of controlled release : official journal of the Controlled Release Society.

Structure−Activity Relationships of Novel Cyclic α-MSH/β-MSH Hybrid Analogues That Lead to Potent and Selective Ligands for the Human MC3R and Human MC5R

P. Grieco, V. Hruby, M. Cai, 2003 .

Effects of Macrocycle Size and Rigidity on Melanocortin Receptor‐1 and ‐5 Selectivity in Cyclic Lactam α‐Melanocyte‐Stimulating Hormone Analogs

V. Hruby, So-Yeop Han, M. Cai, 2006, Chemical biology & drug design.

Structure–activity studies of new melanocortin peptides containing an aromatic amino acid at the N-terminal position

P. Grieco, V. Hruby, M. Cai, 2006, Peptides.

Biological and conformational study of beta-substituted prolines in MT-II template: steric effects leading to human MC5 receptor selectivity.

C. Xiong, V. Hruby, M. Cai, 2004, The journal of peptide research : official journal of the American Peptide Society.

Exploring the Stereostructural Requirements of Peptide Ligands for the Melanocortin Receptors

P. Grieco, V. Hruby, M. Cai, 2003, Annals of the New York Academy of Sciences.

Design, synthesis and biological evaluation of ligands selective for the melanocortin-3 receptor.

James P. Cain, V. Hruby, M. Cai, 2007, Current topics in medicinal chemistry.

An Unusual Conformation of MSH Analogues Leads to a Selective Human Melanocortin 1 Receptor Antagonist for Targeting Melanoma Cells

M. Staňková, V. Hruby, M. Cai, 2013 .

Plasmon-waveguide resonance studies of ligand binding to integral proteins in membrane fragments derived from bacterial and mammalian cells.

Z. Salamon, G. Tollin, E. Navratilova, 2009, Analytical biochemistry.

New paradigms and tools in drug design for pain and addiction

I. Alves, Z. Salamon, G. Tollin, 2006, The AAPS Journal.

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

E. Novellino, P. Grieco, V. Hruby, 2018, Journal of medicinal chemistry.

Melanocortin 1 receptor regulates cholesterol and bile acid metabolism in the liver

B. Ghimire, M. Cai, E. Savontaus, 2022, bioRxiv.

Design of novel melanocortin receptor ligands: multiple receptors, complex pharmacology, the challenge.

James P. Cain, V. Hruby, M. Cai, 2011, European journal of pharmacology.

Solid-phase peptide head-to-side chain cyclodimerization: Discovery of C2-symmetric cyclic lactam hybrid α-melanocyte-stimulating hormone (MSH)/agouti-signaling protein (ASIP) analogues with potent activities at the human melanocortin receptors

James P. Cain, V. Hruby, M. Cai, 2010, Peptides.

Novel selective human melanocortin-3 receptor ligands: use of the 4-amino-1,2,4,5-tetrahydro-2-benzazepin-3-one (Aba) scaffold.

V. Hruby, M. Cai, A. Misicka, 2007, Bioorganic & medicinal chemistry letters.

Melanotropins as drugs for the treatment of obesity and other feeding disorders: potential and problems.

V. Hruby, M. Cai, Joel Nyberg, 2009, Current topics in medicinal chemistry.

Design and synthesis of novel χ2-constrained phenylalanine, naphthylalanine, and tryptophan analogues and their use in biologically active melanotropin peptides

Wei Wang, C. Xiong, V. Hruby, 2002 .

Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor.

Jinfa Ying, V. Hruby, M. Cai, 2006, Journal of medicinal chemistry.

Multiple N-methylation of MT-II backbone amide bonds leads to melanocortin receptor subtype hMC1R selectivity: pharmacological and conformational studies.

V. Hruby, H. Kessler, M. Cai, 2010, Journal of the American Chemical Society.

Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors.

V. Hruby, M. Cai, H. Wang, 2006, Bioorganic & medicinal chemistry letters.

Utilize conjugated melanotropins for the earlier diagnosis and treatment of melanoma.

V. Hruby, Zhonglin Liu, M. Cai, 2011, European journal of pharmacology.

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

V. Hruby, M. Cai, Saghar Mowlazadeh Haghighi, 2017, Journal of medicinal chemistry.

Development of N-Acetylated Dipalmitoyl-S-Glyceryl Cysteine Analogs as Efficient TLR2/TLR6 Agonists

V. Hruby, M. Cai, Yang Zhou, 2019, Molecules.

Design of peptide and peptidomimetic ligands with novel pharmacological activity profiles.

V. Hruby, M. Cai, Victor J Hruby, 2013, Annual review of pharmacology and toxicology.

The Melanocortin Receptor System: A Target for Multiple Degenerative Diseases.

V. Hruby, M. Cai, 2016, Current protein & peptide science.

Opioid and melanocortin receptors: Do they have overlapping pharmacophores?

James P. Cain, V. Hruby, M. Cai, 2008, Biopolymers.

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

V. Hruby, M. Cai, Katja Kaipio, 2020, European journal of pharmacology.

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

Philipp M. Cromm, A. Plowright, D. Craik, 2018, Journal of medicinal chemistry.

Melanocortin 1 Receptor Signaling Regulates Cholesterol Transport in Macrophages

T. Lehtimäki, V. Hruby, C. Weber, 2017, Circulation.

α-Melanocyte-stimulating hormone regulates vascular NO availability and protects against endothelial dysfunction.

V. Hruby, A. Saraste, M. Cai, 2013, Cardiovascular research.

Novel cyclic templates of alpha-MSH give highly selective and potent antagonists/agonists for human melanocortin-3/4 receptors.

Paolo Grieco, Jinfa Ying, Jinfa Ying, 2002, Journal of medicinal chemistry.

Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor.

P. Grieco, V. Hruby, M. Cai, 2009, Journal of medicinal chemistry.

CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists.

V. Hruby, A. Mollica, M. Cai, 2022, Journal of medicinal chemistry.

An unusual conformation of γ-melanocyte-stimulating hormone analogues leads to a selective human melanocortin 1 receptor antagonist for targeting melanoma cells.

M. Staňková, V. Hruby, M. Cai, 2013, Biochemistry.

Effects of selective modulation of the central melanocortin-3-receptor on food intake and hypothalamic POMC expression

V. Hruby, M. Cai, S. Wardlaw, 2008, Peptides.

Contribution of the Conserved Amino Acids of the Melanocortin-4 Receptor in d-[Nle4,Phe7]-α-Melanocyte-stimulating Hormone Binding and Signaling*

V. Hruby, M. Cai, K. Georgeson, 2007, Journal of Biological Chemistry.

Contribution of the conserved amino acids of the melanocortin-4 receptor in [corrected] [Nle4,D-Phe7]-alpha-melanocyte-stimulating [corrected] hormone binding and signaling.

V. Hruby, M. Cai, K. Georgeson, 2007, The Journal of biological chemistry.

Multiple Applications of a Novel Biarsenical Imaging Probe in Fluorescence and PET Imaging of Melanoma

V. Hruby, A. Takano, M. Cai, 2021, Bioconjugate chemistry.

Further structure–activity studies of lactam derivatives of MT-II and SHU-9119: Their activity and selectivity at human melanocortin receptors 3, 4, and 5

E. Novellino, P. Grieco, V. Hruby, 2007, Peptides.

Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.

James P. Cain, V. Hruby, M. Cai, 2008, Journal of medicinal chemistry.

Novel binding motif of ACTH analogues at the melanocortin receptors.

V. Hruby, C. Crasto, M. Cai, 2009, Biochemistry.

Sex-specific Mediation of Opioid-induced Hyperalgesia by the Melanocortin-1 Receptor

M. Staňková, A. Dahan, V. Hruby, 2010, Anesthesiology.

α-Melanocyte-Stimulating Hormone Regulates Pathological Cardiac Remodeling by Activating Melanocortin 5 Receptor in Cardiomyocytes

B. Ghimire, M. Cai, E. Savontaus, 2023, bioRxiv.

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

D. Craik, V. Hruby, Q. Kaas, 2020 .

Ψ and χ Angle Constrains at the C-Terminus Trp Position of the Melanotropin Tetrapeptide Ac-His-d-Phe-Arg-Trp-NH2 Lead to Potent and Selective Agonists at hMC1R and hMC4R.

V. Hruby, M. Cai, Saghar Mowlazadeh Haghighi, 2023, Journal of medicinal chemistry.

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

V. Hruby, M. Cai, Saghar Mowlazadeh Haghighi, 2020, ACS pharmacology & translational science.

Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor.

E. Novellino, P. Grieco, V. Hruby, 2015, Journal of medicinal chemistry.

Systematic Backbone Conformational Constraints on a Cyclic Melanotropin Ligand Leads to Highly Selective Ligands for Multiple Melanocortin Receptors.

V. Hruby, H. Kessler, M. Cai, 2015, Journal of medicinal chemistry.

Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist.

V. Hruby, S. Schwartz, M. Cai, 2015, ACS medicinal chemistry letters.

Novel 3D Pharmacophore of α-MSH/γ-MSH Hybrids Leads to Selective Human MC1R and MC3R Analogues†

M. Staňková, V. Hruby, M. Cai, 2005 .

Structure-activity relationships of gamma-MSH analogues at the human melanocortin MC3, MC4, and MC5 receptors. Discovery of highly selective hMC3R, hMC4R, and hMC5R analogues.

Paolo Grieco, P. Grieco, V. Hruby, 2003, Journal of medicinal chemistry.

Design of cyclized selective melanotropins

V. Hruby, M. Cai, 2016, Biopolymers.

Contribution of the transmembrane domain 6 of melanocortin-4 receptor to peptide [Pro5, DNal (2')8]-gamma-MSH selectivity.

V. Hruby, M. Cai, D. McPherson, 2009, Biochemical pharmacology.

Structure-activity studies of the melanocortin peptides: discovery of potent and selective affinity antagonists for the hMC3 and hMC4 receptors.

Paolo Grieco, Antonio Lavecchia, P. Grieco, 2002, Journal of medicinal chemistry.

Key amino acid residues in the melanocortin-4 receptor for nonpeptide THIQ specific binding and signaling

V. Hruby, M. Cai, Hongchang Qu, 2009, Regulatory Peptides.

Peptide and non-peptide mimetics utilize different pathways for signal transduction.

V. Hruby, M. Cai, G. Tsaprailis, 2009, Advances in Experimental Medicine and Biology.

Real time differentiation of G-protein coupled receptor (GPCR) agonist and antagonist by two photon fluorescence laser microscopy.

M. Staňková, V. Hruby, M. Cai, 2004, Journal of the American Chemical Society.

Aged Brains Express Less Melanocortin Receptors, Which Correlates with Age-Related Decline of Cognitive Functions

C. Barnes, M. Chawla, V. Hruby, 2021, Molecules.

Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.

M. Staňková, V. Hruby, M. Cai, 2005, Journal of medicinal chemistry.

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

V. Hruby, M. Cai, L. Vähätalo, 2018, The Journal of endocrinology.

Cyclic lactam hybrid α-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors.

James P. Cain, V. Hruby, M. Cai, 2011, Bioorganic & medicinal chemistry letters.

Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.

V. Hruby, M. Cai, K. Chandler, 2006, Journal of medicinal chemistry.

Design and parallel synthesis of new bicyclic small molecules for targeting the melanocortin receptors.

V. Hruby, M. Cai, A. Mayorov, 2009, Advances in experimental medicine and biology.

Design, Synthesis, and Evaluation of Piperazine-Based Small Molecule Peptide Mimetics Targeting the Melanocortin Receptors

Jinfa Ying, V. Hruby, M. Cai, 2006 .

Novel MTII/AGRP Hybrid Analogs that Lead to Selective Ligands for the Human Melanocortin Receptors

V. Hruby, M. Cai, K. Chandler, 2006 .

Design and Synthesis of Novel α-MSH Peptide Analogs Highly Selective for the hMC4R

Jinfa Ying, V. Hruby, M. Cai, 2006 .

MC1R Peptide Agonist Self-Assembles into a Hydrogel That Promotes Skin Pigmentation for Treating Vitiligo.

M. Cai, Dan Yuan, Jiaying Wei, 2023, ACS Nano.

Novel and Highly Selective Antagonist Scaffold for Human Melanocortin 3 Receptor: Computer-Aided Design and Biological Evaluation

V. Hruby, M. Cai, K. Chandler, 2006 .

Contribution of regional brain melanocortin receptor subtypes to elevated activity energy expenditure in lean, active rats

M. Bednarek, V. Hruby, L. Koch, 2015, Neuroscience.