Hye Jin Kang
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View article: Response kinetics as a dynamic prognostic marker in patients with multiple myeloma
Response kinetics as a dynamic prognostic marker in patients with multiple myeloma Open
While traditional risk-stratifying models based on static baseline factors have been used to predict prognosis, they may not fully capture the dynamic features of high-risk disease. In this multicenter retrospective study, we investigated …
View article: G-Protein-Coupled Receptor (GPCR) Signaling and Pharmacology in Metabolism: Physiology, Mechanisms, and Therapeutic Potential
G-Protein-Coupled Receptor (GPCR) Signaling and Pharmacology in Metabolism: Physiology, Mechanisms, and Therapeutic Potential Open
G-protein coupled receptors (GPCRs), the largest family of integral membrane proteins, enable cells to sense and appropriately respond to the environment through mediating extracellular signaling to intercellular messenger molecules. GPCRs…
View article: Comparative Analysis of Primary and Second Primary Multiple Myeloma: A Propensity Score-Matched Study
Comparative Analysis of Primary and Second Primary Multiple Myeloma: A Propensity Score-Matched Study Open
Background: With the increasing number of cancer survivors, second primary malignancies (SPMs) are attracting clinical interest. Although SPMs following multiple myeloma (MM) have been studied, data on second primary multiple myeloma (SPMM…
View article: Sequential Bruton Tyrosine Kinase Inhibitor Therapy in Relapsed or Refractory Mantle Cell Lymphoma Following Chemotherapy: Real-World Outcomes and Attrition Rates - an Updated Report from the Asia-Pacific Multinational Retrospective Registry
Sequential Bruton Tyrosine Kinase Inhibitor Therapy in Relapsed or Refractory Mantle Cell Lymphoma Following Chemotherapy: Real-World Outcomes and Attrition Rates - an Updated Report from the Asia-Pacific Multinational Retrospective Registry Open
I ntroduction We conducted a multinational, multicenter retrospective registry study to evaluate the efficacy of sequential 2L or 3L Bruton Tyrosine Kinase inhibitor (BTKi) therapy following chemotherapy in patients with MCL in the Asia-Pa…
View article: The Clinical Course of the Late Toxicity of Definitive Radiotherapy in Cervical Cancer
The Clinical Course of the Late Toxicity of Definitive Radiotherapy in Cervical Cancer Open
Background and Objectives: This study aimed to investigate the clinical course and characteristics of late toxicity over time following the completion of definitive radiotherapy (RT) in patients with cervical cancer. Materials and Methods:…
View article: Docking for EP4R antagonists active against inflammatory pain
Docking for EP4R antagonists active against inflammatory pain Open
The lipid prostaglandin E 2 (PGE 2 ) mediates inflammatory pain by activating G protein-coupled receptors, including the prostaglandin E2 receptor 4 (EP4R). Nonsteroidal anti-inflammatory drugs (NSAIDs) reduce nociception by inhibiting pro…
View article: Structure-Based Discovery of a NPFF1R Antagonist with Analgesic Activity
Structure-Based Discovery of a NPFF1R Antagonist with Analgesic Activity Open
While opioid drugs remain among the most effective analgesics for pain management, adverse effects limit their use. Molecules that synergize with opioids, increasing analgesia without increasing side effects, could prove beneficial. A pote…
View article: Initial treatment response and short-term mortality of spontaneous bacterial peritonitis in cirrhotic patients with hepatocellular carcinoma
Initial treatment response and short-term mortality of spontaneous bacterial peritonitis in cirrhotic patients with hepatocellular carcinoma Open
This study aimed to investigate the initial treatment response and short-term mortality of spontaneous bacterial peritonitis (SBP) in cirrhotic patients with hepatocellular carcinoma (HCC) compared with those without HCC. A total of 245 pa…
View article: Structural insights into the human niacin receptor HCA2-Gi signalling complex
Structural insights into the human niacin receptor HCA2-Gi signalling complex Open
The hydroxycarboxylic acid receptor 2 (HCA2) agonist niacin has been used as treatment for dyslipidemia for several decades albeit with skin flushing as a common side-effect in treated individuals. Extensive efforts have been made to ident…
View article: Darinaparsin in patients with relapsed or refractory peripheral T-cell lymphoma: results of an Asian phase 2 study
Darinaparsin in patients with relapsed or refractory peripheral T-cell lymphoma: results of an Asian phase 2 study Open
Darinaparsin is a novel organic arsenical compound of dimethylated arsenic conjugated to glutathione, with antitumor activity and a mechanism of action markedly different from other available agents. This phase 2, nonrandomized, single-arm…
View article: Neurotensin receptor allosterism revealed in complex with a biased allosteric modulator
Neurotensin receptor allosterism revealed in complex with a biased allosteric modulator Open
SUMMARY The NTSR1 neurotensin receptor (NTSR1) is a G protein coupled receptor (GPCR) found in the brain and peripheral tissues with neurotensin (NTS) being its endogenous peptide ligand. In the brain, NTS modulates dopamine neuronal activ…
View article: Design, Synthesis, and Characterization of [ <sup>18</sup> F]mG2P026 as a High-Contrast PET Imaging Ligand for Metabotropic Glutamate Receptor 2
Design, Synthesis, and Characterization of [ <sup>18</sup> F]mG2P026 as a High-Contrast PET Imaging Ligand for Metabotropic Glutamate Receptor 2 Open
An array of triazolopyridines based on JNJ-46356479 (6) were synthesized as potential positron emission tomography radiotracers for metabotropic glutamate receptor 2 (mGluR2). The selected candidates 8-10 featured enhanced positive alloste…
View article: Synthesis and Characterization of 5-(2-Fluoro-4-[ <sup>11</sup> C]methoxyphenyl)-2,2-dimethyl-3,4-dihydro-2 <i>H</i> -pyrano[2,3- <i>b</i> ]pyridine-7-carboxamide as a PET Imaging Ligand for Metabotropic Glutamate Receptor 2
Synthesis and Characterization of 5-(2-Fluoro-4-[ <sup>11</sup> C]methoxyphenyl)-2,2-dimethyl-3,4-dihydro-2 <i>H</i> -pyrano[2,3- <i>b</i> ]pyridine-7-carboxamide as a PET Imaging Ligand for Metabotropic Glutamate Receptor 2 Open
Metabotropic glutamate receptor 2 (mGluR2) is a therapeutic target for several neuropsychiatric disorders. An mGluR2 function in etiology could be unveiled by positron emission tomography (PET). In this regard, 5-(2-fluoro-4-[11C]methoxyph…
View article: Design and Discovery of a High Affinity, Selective and β-Arrestin Biased 5-HT7 Receptor Agonist
Design and Discovery of a High Affinity, Selective and β-Arrestin Biased 5-HT7 Receptor Agonist Open
Compound 1c, 2-(2-(3,4-Dihydroisoquinolin-2(1H)-yl)ethyl)-5-fluoro-2,3-dihydro-1H-inden-1-one was previously reported from our laboratory showing high affinity binding to the 5-HT7 receptor (Ki = 0.5 nM). However, compound 1c racemizes rea…
View article: A Promising Chemical Series of Positive Allosteric Modulators of the μ-Opioid Receptor that Enhance the Antinociceptive Efficacy of Opioids but not their Adverse Effects
A Promising Chemical Series of Positive Allosteric Modulators of the μ-Opioid Receptor that Enhance the Antinociceptive Efficacy of Opioids but not their Adverse Effects Open
Positive allosteric modulators (PAMs) of the µ-opioid receptor (MOR) have been proposed to exhibit therapeutic potential by maximizing the analgesic properties of clinically used opioid drugs while limiting their adverse effects or risk of…
View article: Re-exploring the N-phenylpicolinamide derivatives to develop mGlu4 ligands with improved affinity and in vitro microsomal stability
Re-exploring the N-phenylpicolinamide derivatives to develop mGlu4 ligands with improved affinity and in vitro microsomal stability Open
In recent years, mGlu4 has received great attention and research effort because of the potential benefits of mGlu4 activation in treating numerous brain disorders, such as Parkinson's disease (PD). Many positive allosteric modulators of mG…
View article: Design, Synthesis, and Characterization of Benzimidazole Derivatives as Positron Emission Tomography Imaging Ligands for Metabotropic Glutamate Receptor 2
Design, Synthesis, and Characterization of Benzimidazole Derivatives as Positron Emission Tomography Imaging Ligands for Metabotropic Glutamate Receptor 2 Open
Three benzimidazole derivatives (13-15) have been synthetized as potential positron emission tomography (PET) imaging ligands for mGluR2 in the brain. Of these compounds, 13 exhibits potent binding affinity (IC50 = 7.6 ± 0.9 nM), positive …
View article: Effects of Ketamine and Ketamine Metabolites on Evoked Striatal Dopamine Release, Dopamine Receptors, and Monoamine Transporters
Effects of Ketamine and Ketamine Metabolites on Evoked Striatal Dopamine Release, Dopamine Receptors, and Monoamine Transporters Open
Following administration at subanesthetic doses, (R,S)-ketamine (ketamine) induces rapid and robust relief from symptoms of depression in treatment-refractory depressed patients. Previous studies suggest that ketamine’s antidepressant prop…
View article: Design and synthesis of dual 5-HT1A and 5-HT7 receptor ligands
Design and synthesis of dual 5-HT1A and 5-HT7 receptor ligands Open
5-HT and 5-HT receptors have been at the center of discussions recently due in part to their major role in the etiology of major central nervous system diseases such as depression, sleep disorders, and schizophrenia. As part of our search …
View article: Synthesis and Characterization of Fluorine-18-Labeled <i>N</i>-(4-Chloro-3-((fluoromethyl-<i>d</i><sub>2</sub>)thio)phenyl)picolinamide for Imaging of mGluR4 in Brain
Synthesis and Characterization of Fluorine-18-Labeled <i>N</i>-(4-Chloro-3-((fluoromethyl-<i>d</i><sub>2</sub>)thio)phenyl)picolinamide for Imaging of mGluR4 in Brain Open
We have synthesized and characterized [18F]-N-(4-chloro-3-((fluoromethyl-d2)thio)phenyl)-picolinamide ([18F]15) as a potential ligand for the positron emission tomography (PET) imaging of mGluR4 in the brain. Radioligand [18F]15 displays c…
View article: Synthesis and Preliminary Studies of a Novel Negative Allosteric Modulator, 7-((2,5-Dioxopyrrolidin-1-yl)methyl)-4-(2-fluoro-4-[ 11 C]methoxyphenyl) quinoline-2-carboxamide, for Imaging of Metabotropic Glutamate Receptor 2
Synthesis and Preliminary Studies of a Novel Negative Allosteric Modulator, 7-((2,5-Dioxopyrrolidin-1-yl)methyl)-4-(2-fluoro-4-[ 11 C]methoxyphenyl) quinoline-2-carboxamide, for Imaging of Metabotropic Glutamate Receptor 2 Open
Metabotropic glutamate 2 receptors (mGlu2) are involved in the pathogenesis of several CNS disorders and neurodegenerative diseases. Pharmacological modulation of this target represents a potential disease-modifying approach for the treatm…
View article: Zebrafish behavioral profiling identifies ligands, targets, and neurons related to sedation and paradoxical excitation
Zebrafish behavioral profiling identifies ligands, targets, and neurons related to sedation and paradoxical excitation Open
Anesthetics are generally associated with sedation, but some anesthetics can also increase brain and motor activity — a phenomenon known as paradoxical excitation. Previous studies have identified GABAA receptors as the primary targets of …