Search Results - "Freeman, Katie T."
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Neuroplasticity of sensory and sympathetic nerve fibers in a mouse model of a painful arthritic joint
Published in Arthritis & rheumatology (Hoboken, N.J.) (01-07-2012)“…Objective Many forms of arthritis are accompanied by significant chronic joint pain. This study was undertaken to investigate whether there is significant…”
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2
Pathological sprouting of adult nociceptors in chronic prostate cancer-induced bone pain
Published in The Journal of neuroscience (03-11-2010)“…Pain frequently accompanies cancer. What remains unclear is why this pain frequently becomes more severe and difficult to control with disease progression…”
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3
The Parallel Structure-Activity Relationship Screening of Three Compounds Identifies the Common Agonist Pharmacophore of Pyrrolidine Bis-Cyclic Guanidine Melanocortin-3 Receptor (MC3R) Small-Molecule Ligands
Published in International journal of molecular sciences (14-06-2023)“…The melanocortin receptors are involved in numerous physiological pathways, including appetite, skin and hair pigmentation, and steroidogenesis. In particular,…”
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4
Breast cancer-induced bone remodeling, skeletal pain, and sprouting of sensory nerve fibers
Published in The journal of pain (01-06-2011)“…Breast cancer metastasis to bone is frequently accompanied by pain. What remains unclear is why this pain tends to become more severe and difficult to control…”
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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
Published in Molecules (Basel, Switzerland) (13-04-2019)“…The five melanocortin receptors (MC1R–MC5R) are involved in numerous biological pathways, including steroidogenesis, pigmentation, and food intake. In…”
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Administration of a Tropomyosin Receptor Kinase Inhibitor Attenuates Sarcoma-Induced Nerve Sprouting, Neuroma Formation and Bone Cancer Pain
Published in Molecular pain (07-12-2010)“…Pain often accompanies cancer and most current therapies for treating cancer pain have significant unwanted side effects. Targeting nerve growth factor (NGF)…”
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7
Nerve growth factor sequestering therapy attenuates non-malignant skeletal pain following fracture
Published in Pain (Amsterdam) (15-12-2007)“…Current therapies to treat skeletal fracture pain are extremely limited. Some non-steroidal anti-inflammatory drugs have been shown to inhibit bone healing and…”
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Effects of a Monoclonal Antibody Raised Against Nerve Growth Factor on Skeletal Pain and Bone Healing After Fracture of the C57BL/6J Mouse Femur
Published in Journal of bone and mineral research (01-11-2007)“…A closed femur fracture pain model was developed in the C57BL/6J mouse. One day after fracture, a monoclonal antibody raised against nerve growth factor…”
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9
Development of hMC1R Selective Small Agonists for Sunless Tanning and Prevention of Genotoxicity of UV in Melanocytes
Published in Journal of investigative dermatology (01-07-2021)“…Activation of the human melanocortin 1 receptor (hMC1R) expressed on melanocytes by α-melanocortin plays a central role in regulating human pigmentation and…”
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10
Discovery of a Pan-Melanocortin Receptor Antagonist [Ac-DPhe(pI)-Arg-Nal(2′)-Orn-NH2] at the MC1R, MC3R, MC4R, and MC5R that Mediates an Increased Feeding Response in Mice and a 40-Fold Selective MC1R Antagonist [Ac-DPhe(pI)-DArg-Nal(2′)-Arg-NH2]
Published in Journal of medicinal chemistry (22-06-2023)“…Discovery of pan-antagonist ligands for the melanocortin receptors will help identify the physiological activities controlled by these receptors. The…”
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Synergistic Multiresidue Substitutions of a Macrocyclic c[Pro-Arg-Phe-Phe-Asn-Ala-Phe‑dPro] Agouti-Related Protein (AGRP) Scaffold Yield Potent and >600-Fold MC4R versus MC3R Selective Melanocortin Receptor Antagonists
Published in Journal of medicinal chemistry (13-09-2018)“…Antagonist ligands of the melanocortin-3 and -4 receptors (MC3R, MC4R), including agouti-related protein (AGRP), are postulated to be targets for the treatment…”
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An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers
Published in Journal of medicinal chemistry (14-04-2016)“…Pharmacological probes for the melanocortin receptors have been utilized for studying various disease states including cancer, sexual function disorders,…”
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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
Published in Journal of medicinal chemistry (10-01-2019)“…Understanding the functional relevance of G protein-coupled receptor (GPCR) homodimerization has been limited by the insufficient tools to assess asymmetric…”
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14
Structure–Activity Relationship Studies on a Macrocyclic Agouti-Related Protein (AGRP) Scaffold Reveal Agouti Signaling Protein (ASP) Residue Substitutions Maintain Melanocortin‑4 Receptor Antagonist Potency and Result in Inverse Agonist Pharmacology at the Melanocortin‑5 Receptor
Published in Journal of medicinal chemistry (12-10-2017)“…The melanocortin system consists of five reported receptors, agonists from the proopiomelanocortin gene transcript, and two antagonists, agouti-signaling…”
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15
A fragment of the Escherichia coli ClpB heat-shock protein is a micromolar melanocortin 1 receptor agonist
Published in Bioorganic & medicinal chemistry letters (15-11-2015)“…[Display omitted] The melanocortin system consists of five receptor subtypes (MC1–5R), endogenous agonists derived from the proopiomelanocortin gene…”
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Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe‑dPro] Decreases Melanocortin‑4 Receptor Antagonist Potency and Results in the Discovery of Melanocortin‑5 Receptor Antagonists
Published in Journal of medicinal chemistry (12-03-2020)“…While the melanocortin receptors (MCRs) are known to be involved in numerous biological pathways, the potential roles of the MC5R have not been clearly…”
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17
Peptoid NPhe4 in AGRP-Based c[Pro1‑Arg2‑Phe3‑Phe4‑Xxx5‑Ala6‑Phe7‑DPro8] Scaffolds Maintain Mouse MC4R Antagonist Potency
Published in ACS medicinal chemistry letters (08-10-2020)“…The melanocortin receptors are involved in numerous physiological functions and are regulated by agonists derived from the proopiomelanocortin gene transcript…”
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18
Functional Mixture-Based Positional Scan Identifies a Library of Antagonist Tetrapeptide Sequences (LAtTeS) with Nanomolar Potency for the Melanocortin‑4 Receptor and Equipotent with the Endogenous AGRP(86-132) Antagonist
Published in Journal of medicinal chemistry (14-10-2021)“…The melanocortin-4 receptor (MC4R) plays an important role in appetite. Agonist ligands that stimulate the MC4R decrease appetite, while antagonist compounds…”
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A Macrocyclic Agouti-Related Protein/[Nle4,DPhe7]α-Melanocyte Stimulating Hormone Chimeric Scaffold Produces Subnanomolar Melanocortin Receptor Ligands
Published in Journal of medicinal chemistry (26-01-2017)“…The melanocortin system consists of five receptor subtypes, endogenous agonists, and naturally occurring antagonists. These receptors and ligands have been…”
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Multiresidue Tetrapeptide Substitutions Yield a 140-fold Selective Melanocortin-3 over Melanocortin-4 Receptor Agonist
Published in ACS medicinal chemistry letters (14-01-2021)“…The five melanocortin receptors regulate numerous physiological functions. Although many ligands have been developed for the melanocortin-4 receptor (MC4R),…”
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