keyword
https://read.qxmd.com/read/37871763/xanthotoxol-relieves-itch-in-mice-via-suppressing-spinal-grp-grpr-signaling
#21
JOURNAL ARTICLE
Xinyi Gao, Yayue Yang, Jianyu Zhu, Yuxin Zhang, Chenghao Wang, Zhifei Wang, Wenli Mi, Lixia Du
Although pruritus, commonly known as itch, is a common and debilitating symptom associated with various skin conditions, there is a lack of effective therapies available. Xanthotoxol (XAN), a biologically active linear furocoumarin, shows potential in the treatment of various neurological disorders. In this study, we discovered that administering XAN either through intraperitoneal or intrathecal injections effectively reduced scratching behavior induced by compound 48/80 or chloroquine (CQ). Importantly, XAN also substantially alleviates chronic itch in dry skin and allergic contact dermatitis (ACD) mice...
October 21, 2023: European Journal of Pharmacology
https://read.qxmd.com/read/37719014/grpr-versus-psma-expression-profiles-during-prostate-cancer-progression-demonstrate-the-added-value-of-grpr-targeting-theranostic-approaches
#22
JOURNAL ARTICLE
Marjolein Verhoeven, Eline A M Ruigrok, Geert J L H van Leenders, Lilian van den Brink, Hayri E Balcioglu, Wytske M van Weerden, Simone U Dalm
INTRODUCTION: Central to targeted radionuclide imaging and therapy of prostate cancer (PCa) are prostate-specific membrane antigen (PSMA)-targeting radiopharmaceuticals. Gastrin-releasing peptide receptor (GRPR) targeting has been proposed as a potential additional approach for PCa theranostics. The aim of this study was to investigate to what extent and at what stage of the disease GRPR-targeting applications can complement PSMA-targeting theranostics in the management of PCa. METHODS: Binding of the GRPR- and PSMA-targeting radiopharmaceuticals [177 Lu]Lu-NeoB and [177 Lu]Lu-PSMA-617, respectively, was evaluated and compared on tissue sections of 20 benign prostatic hyperplasia (BPH), 16 primary PCa and 17 progressive castration-resistant PCa (CRPC) fresh frozen tissue specimens...
2023: Frontiers in Oncology
https://read.qxmd.com/read/37702025/role-of-the-grp-grpr-system-in-regulating-brain-functions
#23
REVIEW
Tiantian Zhao, Aiwen Chen, Danqing Dai, Zhen Li, Xiao-Fei Gao, Lize Xiong
Re-examining the relationship between neuropeptide systems and neural circuits will help us to understand more intensively the critical role of neuropeptides in brain function as the neural circuits responsible for specific brain functions are gradually revealed. Gastrin-releasing peptide receptors (GRPRs) are Gαq-coupling neuropeptide receptors and widely distributed in the brain, including hippocampus, amygdala, hypothalamus, nucleus tractus solitarius (NTS), suprachiasmatic nucleus (SCN), paraventricular nucleus of the hypothalamus (PVN), preoptic area of the hypothalamus (POA), preBötzinger complex (preBötC), etc...
September 13, 2023: ACS Chemical Neuroscience
https://read.qxmd.com/read/37679976/zhenxin-anshen-formula-ameliorates-atopic-der-matitis-like-skin-dysfunction-in-mice-and-regulation-of-transient-receptor-potential-vanilloid-1-and-transient-receptor-potential-ankyrin-1-in-neural-pathways
#24
JOURNAL ARTICLE
Zhao Yiding, Yan Xiaoning, Jiang Shanshan, Liu Yong, Dong Chun, Chi Huiyan, Mao Chaoyi
OBJECTIVE: To investigate the efficacy of Zhenxin Anshen formula (, ZXAS) on atopic dermatitis (AD) by transient receptor potential vanilloid 1 (TRPV1) and transient receptor potential ankyrin 1 (TRPA1) signalling pathway in mice and . METHODS: AD-like lesions were induced by 1-chloro-2,4-dinitrobenzene (DNCB) to the shaved dorsal skin of BALB/c mice. BALB/c mice were divided into five groups: normal control, model control, cetirizine, low-, medium-, and high-dose of ZXAS...
October 2023: Journal of Traditional Chinese Medicine
https://read.qxmd.com/read/37640941/the-balance-between-the-therapeutic-efficacy-and-safety-of-177-lu-lu-neob-in-a-preclinical-prostate-cancer-model
#25
JOURNAL ARTICLE
Marjolein Verhoeven, Joost Haeck, Erik de Blois, Francesca Orlandi, Donato Barbato, Mattia Tedesco, Mark Konijnenberg, Simone U Dalm
PURPOSE: Radiolabeled NeoB is a promising gastrin-releasing peptide receptor (GRPR)-targeting radiopharmaceutical for theranostics of GRPR-expressing malignancies, e.g., prostate cancer (PCa). The aim of this study was to evaluate the effect of different doses of [177 Lu]Lu-NeoB on the balance between therapeutic efficacy and safety in a preclinical PCa model. PROCEDURES: To determine the efficacy of [177 Lu]Lu-NeoB, PC-3 xenografted mice received 3 sham injections (control group) or 3 injections of 30 MBq/300 pmol, 40 MBq/400 pmol, or 60 MBq/600 pmol [177 Lu]Lu-NeoB (groups 1, 2, and 3, respectively) 1 week apart...
August 28, 2023: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
https://read.qxmd.com/read/37604300/grpr-down-regulation-inhibits-spermatogenesis-through-ca-2-mediated-by-plc%C3%AE-ip3r-signaling-pathway-in-long-term-formaldehyde-exposed-rats
#26
JOURNAL ARTICLE
Yan-Qi Yang, Rui-Fang Sun, Pan Ge, Wen-Xing Li, Xiang Zhang, Jian Zhang, Lu Ye, Nan Zhang, Si-Yu Wang, Mo-Qi Lv, Dang-Xia Zhou
Formaldehyde (FA), which is known as an air pollutant, has been proven to induce male infertility. However, the underlying mechanism of FA-induced male infertility remains elusive. In this study, 24 male SD rats were exposed to different levels of FA (0, 0.5, 2.46, and 5 mg/m3 ) for eight consecutive weeks. Through HE staining and sperm smear, we observed that FA exposure resulted in spermatogenic injury and the sperm quality decreased in rats. The qRT-PCR and Western blot analysis further revealed that GRPR was down-regulated in testicular tissues of FA-exposed rats as well as primary spermatogenic cells...
August 19, 2023: Food and Chemical Toxicology
https://read.qxmd.com/read/37584725/side-by-side-comparison-of-the-two-widely-studied-grpr-radiotracers-radiolabeled-neob-and-rm2-in-a-preclinical-setting
#27
JOURNAL ARTICLE
T S T Damiana, P Paraïso, C de Ridder, D Stuurman, Y Seimbille, S U Dalm
INTRODUCTION: NeoB and RM2 are the most investigated gastrin-releasing peptide receptor (GRPR)-targeting radiotracers in preclinical and clinical studies. Therefore, an extensive side-by-side comparison of the two radiotracers is valuable to demonstrate whether one has advantages over the other. Accordingly, this study aims to compare the in vitro and in vivo characteristics of radiolabeled NeoB and RM2 to guide future clinical studies. METHOD: The stability of the radiolabeled GRPR analogs was determined in phosphate buffered saline (PBS), and commercially available mouse and human serum...
August 16, 2023: European Journal of Nuclear Medicine and Molecular Imaging
https://read.qxmd.com/read/37555901/modified-promise-criteria-for-standardized-interpretation-of-gastrin-releasing-peptide-receptor-grpr-targeted-pet
#28
JOURNAL ARTICLE
Heying Duan, Guido A Davidzon, Farshad Moradi, Tie Liang, Hong Song, Andrei Iagaru
PURPOSE: There are image interpretation criteria to standardize reporting prostate-specific membrane antigen (PSMA)-targeted positron emission tomography (PET). As up to 10% of prostate cancer (PC) do not express PSMA, other targets such as gastrin-releasing peptide receptor (GRPR) are evaluated. Research on GRPR-targeted imaging has been slowly increasing in usage at staging and biochemical recurrence (BCR) of PC. We therefore propose a modification of the Prostate Cancer Molecular Imaging Standardized Evaluation (PROMISE) criteria (mPROMISE) for GRPR-targeted PET...
August 9, 2023: European Journal of Nuclear Medicine and Molecular Imaging
https://read.qxmd.com/read/37522391/descending-dopaminergic-pathway-facilitates-itch-signal-processing-via-activating-spinal-grpr-neurons
#29
JOURNAL ARTICLE
Zhi-Jun Zhang, Han-Yu Shao, Chuan Liu, Hao-Lin Song, Xiao-Bo Wu, De-Li Cao, Meixuan Zhu, Yuan-Yuan Fu, Juan Wang, Yong-Jing Gao
A11 dopaminergic neurons regulate somatosensory transduction by projecting from the diencephalon to the spinal cord, but the function of this descending projection in itch remained elusive. Here, we report that dopaminergic projection neurons from the A11 nucleus to the spinal dorsal horn (dopaminergicA11-SDH ) are activated by pruritogens. Inhibition of these neurons alleviates itch-induced scratching behaviors. Furthermore, chemogenetic inhibition of spinal dopamine receptor D1-expressing (DRD1+ ) neurons decreases acute or chronic itch-induced scratching...
July 31, 2023: EMBO Reports
https://read.qxmd.com/read/37516088/antipruritic-effects-of-geraniol-on-acute-and-chronic-itch-via-modulating-spinal-gaba-grpr-signaling
#30
JOURNAL ARTICLE
Ya-Yue Yang, Li-Xia Du, Jian-Yu Zhu, Ting Yi, Ya-Chen Yang, Zheng Qiao, Qi-Liang Maoying, Yu-Xia Chu, Yan-Qing Wang, Wen-Li Mi
BACKGROUND AND PURPOSE: Itch (pruritus) is a common unpleasant feeling, often accompanied by the urge of scratching the skin. It is the main symptom of many systemic and skin diseases, which can seriously affect the patient's quality of life. Geraniol (GE; trans-3,7-dimethyl-2,6-octadien-1-ol) is a natural monoterpene with diverse effects, including anti-inflammatory, antioxidant, neuroprotective, anti-nociceptive, and anticancer properties. The study aims to examine the effects of GE on acute and chronic itch, and explore the underlying mechanisms...
July 22, 2023: Phytomedicine
https://read.qxmd.com/read/37509170/preclinical-characterization-of-a-stabilized-gastrin-releasing-peptide-receptor-antagonist-for-targeted-cancer-theranostics
#31
JOURNAL ARTICLE
Ayman Abouzayed, Panagiotis Kanellopoulos, Alisa Gorislav, Vladimir Tolmachev, Theodosia Maina, Berthold A Nock, Anna Orlova
Radiolabeled gastrin-releasing peptide receptor (GRPR) antagonists have shown great promise for the theranostics of prostate cancer; however, their suboptimal metabolic stability leaves room for improvements. It was recently shown that the replacement of Gly11 with Sar11 in the peptidic [D-Phe6 ,Leu13 -NHEt, des -Met14 ]BBN(6-14) chain stabilized the [99m Tc]Tc-DB15 radiotracer against neprilysin (NEP). We herein present DOTAGA-PEG2 -(Sar11 )RM26 (AU-RM26-M1), after Gly11 to Sar11 -replacement. The impact of this replacement on the metabolic stability and overall biological performance of [111 In]In-AU-RM26-M1 was studied using a head-to-head comparison with the unmodified reference [111 In]In-DOTAGA-PEG2 -RM26...
July 14, 2023: Biomolecules
https://read.qxmd.com/read/37476052/preclinical-assessment-of-irdye800cw-labeled-gastrin-releasing-peptide-receptor-targeting-peptide-for-near-infrared-ii-imaging-of-brain-malignancies
#32
JOURNAL ARTICLE
Yuan Zhang, Li Wang, Chengkai Zhang, Jingjing Zhang, Linhao Yuan, Shucheng Jin, Wenjianlong Zhou, Xiudong Guan, Peng Kang, Chuanbao Zhang, Jie Tian, Xiaoyuan Chen, Deling Li, Wang Jia
We aimed to develop a new biocompatible gastrin-releasing peptide receptor (GRPR) targeted optical probe, IRDye800-RM26, for fluorescence image-guided surgery (FGS) of brain malignancies in near-infrared window II (NIR-II) imaging. We developed a novel GRPR targeting probe using a nine-amino-acid bombesin antagonist analog RM26 combined with IRDye800CW, and explored the fluorescent probe according to optical properties. Fluorescence imaging characterization in NIR-I/II region was performed in vitro and in vivo...
July 2023: Bioengineering & Translational Medicine
https://read.qxmd.com/read/37474269/preclinical-comparison-of-the-64-cu-and-68-ga-labeled-grpr-targeted-compounds-rm2-and-amtg-as-well-as-first-in-humans-68-ga-ga-amtg-pet-ct
#33
JOURNAL ARTICLE
Lena Koller, Markus Joksch, Sarah Schwarzenböck, Jens Kurth, Martin Heuschkel, Nadine Holzleitner, Roswitha Beck, Gunhild von Amsberg, Hans-Jürgen Wester, Bernd Joachim Krause, Thomas Günther
Despite the recent success of prostate-specific membrane antigen (PSMA)-targeted compounds for theranostic use in prostate cancer (PCa), alternative options for the detection and treatment of PSMA-negative lesions are needed. We have recently developed a novel gastrin-releasing peptide receptor (GRPR) ligand with improved metabolic stability, which might improve diagnostic and therapeutic efficacy and could be valuable for PSMA-negative PCa patients. Our aim was to examine its suitability for theranostic use...
July 20, 2023: Journal of Nuclear Medicine
https://read.qxmd.com/read/37468417/preclinical-development-in-radiopharmaceutical-therapy-for-prostate-cancer
#34
REVIEW
Suresh Alati, Rajan Singh, Martin G Pomper, Steven P Rowe, Sangeeta Ray Banerjee
Prostate cancer is a leading cause of cancer death in men worldwide. Among the various treatment options, radiopharmaceutical therapy has shown notable success in metastatic, castration-resistant disease. Radiopharmaceutical therapy is a systemic approach that delivers cytotoxic radiation doses precisely to the malignant tumors and/or tumor microenvironment. Therapeutic radiopharmaceuticals are composed of a therapeutic radionuclide and a high-affinity, tumor-targeting carrier molecule. Therapeutic radionuclides used in preclinical prostate cancer studies are primarily α-, β- -, or Auger-electron-emitting radiometals or radiohalogens...
September 2023: Seminars in Nuclear Medicine
https://read.qxmd.com/read/37465877/novel-grpr-targeting-peptide-for-pancreatic-cancer-molecular-imaging-in-orthotopic-and-liver-metastasis-mouse-models
#35
JOURNAL ARTICLE
Yuanbiao Tu, Zhihao Han, Rongbin Pan, Kuncheng Zhou, Ji Tao, Peifei Liu, Ray P S Han, Shuaichang Gong, Yueqing Gu
Despite advancements in pancreatic cancer treatment, it remains one of the most lethal malignancies with extremely poor diagnosis and prognosis. Herein, we demonstrated the efficiency of a novel peptide GB-6 labeled with a near-infrared (NIR) fluorescent dye 3H-indolium, 2-[2-[2-[(2-carboxyethyl)thio]-3-[2-[1,3-dihydro-3,3-dimethyl-5-sulfo-1-(3-sulfopropyl)-2H-indol-2-ylidene]ethylidene]-1-cyclohexen-1-yl]ethenyl]-3,3-dimethyl-5-sulfo-1-(3-sulfopropyl)-, inner salt (MPA) and radionuclide technetium-99m (99m Tc) as targeting probes using the gastrin-releasing peptide receptor (GRPR) that is overexpressed in pancreatic cancer as the target...
July 19, 2023: Analytical Chemistry
https://read.qxmd.com/read/37415332/genetic-and-pharmacological-inhibition-of-grpr-protects-against-acute-kidney-injury-via-attenuating-renal-inflammation-and-necroptosis
#36
JOURNAL ARTICLE
Chao Li, Qiu-Ying Ma, Xue-Qi Liu, Hai-di Li, Ming-Jun Yu, Shuai-Shuai Xie, Wen-Xian Ma, Ying Chen, Jia-Nan Wang, Ruo-Bing He, He-Ge Bian, Yuan He, Li Gao, Sheng-Song Deng, Hong-Mei Zang, Qian Gong, Jia-Gen Wen, Ming-Ming Liu, Chen Yang, Hai-Yong Chen, Jun Li, Hui-Yao Lan, Juan Jin, Ri-Sheng Yao, Xiao-Ming Meng
Gastrin-releasing peptide (GRP) binds to its receptor GRPR to regulate multiple biological processes, but the function of GRP/GRPR axis in acute kidney injury (AKI) remains unknown. In the present study, GRPR is highly expressed by tubular epithelial cells (TECs) in patients or mice with AKI. While histone deacetylase 8 may lead to the transcriptional activation of GRPR. Functionally, we uncovered that GRPR was pathogenic in AKI as genetic deletion of GRPR was able to protect mice from cisplatin and ischemic induced AKI...
July 5, 2023: Molecular Therapy
https://read.qxmd.com/read/37409771/grp-grpr-enhances-alcohol-associated-liver-injury-via-the-irf1-mediated-caspase-1-inflammasome-and-nox2-dependent-ros-pathway
#37
JOURNAL ARTICLE
Haidi Li, Xin Chen, Jiejie Xu, Lin Zhu, Chao Li, Xiaolong Sun, Xiaofeng Li, Jianbo Guo, Juanjuan Li, Sheng Wang, Yong He, Hua Wang, Cheng Huang, Xiaoming Meng, Jun Li
BACKGROUND AIMS: The common characteristics for alcohol-associated liver injury (ALI) include abnormal liver function, infiltration of inflammatory cells, and generation of oxidative stress. The gastrin-releasing peptide receptor (GRPR) is activated by its neuropeptide ligand, gastrin-releasing peptide (GRP). GRP/GRPR appears to induce the production of cytokines in immune cells and promotes neutrophil migration. However, the effects of GRP/GRPR in ALI are unknown. APPROACH RESULTS: We found high GRPR expression in the liver of patients with alcoholic steatohepatitis and increased pro-GRP levels in peripheral blood mononuclear cells of these patients compared to that of the control...
July 5, 2023: Hepatology: Official Journal of the American Association for the Study of Liver Diseases
https://read.qxmd.com/read/37285007/the-effects-of-novel-macrocyclic-chelates-on-the-targeting-properties-of-the-68-ga-labeled-gastrin-releasing-peptide-receptor-antagonist-rm2
#38
JOURNAL ARTICLE
Yinwen Wang, Hongmei Yuan, Sufan Tang, Yang Liu, Ping Cai, Nan Liu, Yue Chen, Zhijun Zhou
BACKGROUND: The gastrin-releasing peptide receptor (GRPr) is a molecular target for the visualization of prostate cancer. Bombesin (BN) analogs are short peptides with a high affinity for GRPr. RM2 is a bombesin-based antagonist. It has been demonstrated that RM2 have superior in vivo biodistribution and targeting properties than high-affinity receptor agonists. This study developed new RM2-like antagonists by introducing the novel bifunctional chelators AAZTA5 and DATA5m to RM2. RESULTS: The effects of different macrocyclic chelating groups on drug targeting properties and the possibility of preparing 68 Ga-radiopharmaceuticals in a kit-based protocol were investigated using 68 Ga-labeled entities...
June 7, 2023: EJNMMI Research
https://read.qxmd.com/read/37197474/modular-one-pot-strategy-for-the-synthesis-of-heterobivalent-tracers
#39
JOURNAL ARTICLE
Thibaud Bailly, Sacha Bodin, Victor Goncalves, Franck Denat, Clément Morgat, Aurélie Prignon, Ibai E Valverde
Bivalent ligands, i.e., molecules having two ligands covalently connected by a linker, have been gathering attention since the first description of their pharmacological potential in the early 80s. However, their synthesis, particularly of labeled heterobivalent ligands, can still be cumbersome and time-consuming. We herein report a straightforward procedure for the modular synthesis of labeled heterobivalent ligands (HBLs) using dual reactive 3,6-dichloro-1,2,4,5-tetrazine as a starting material and suitable partners for sequential SN Ar and inverse electron-demand Diels-Alder (IEDDA) reactions...
May 11, 2023: ACS Medicinal Chemistry Letters
https://read.qxmd.com/read/37175001/the-grpr-antagonist-99m-tc-tc-masss-peg-2-rm26-towards-phase-i-clinical-trial-kit-preparation-characterization-and-toxicity
#40
JOURNAL ARTICLE
Ayman Abouzayed, Jesper Borin, Fanny Lundmark, Anastasiya Rybina, Sophia Hober, Roman Zelchan, Vladimir Tolmachev, Vladimir Chernov, Anna Orlova
Gastrin-releasing peptide receptors (GRPRs) are overexpressed in the majority of primary prostate tumors and in prostatic lymph node and bone metastases. Several GRPR antagonists were developed for SPECT and PET imaging of prostate cancer. We previously reported a preclinical evaluation of the GRPR antagonist [99m Tc]Tc-maSSS-PEG2 -RM26 (based on [D-Phe6 , Sta13 , Leu14 -NH2 ]BBN(6-14)) which bound to GRPR with high affinity and had a favorable biodistribution profile in tumor-bearing animal models. In this study, we aimed to prepare and test kits for prospective use in an early-phase clinical study...
May 2, 2023: Diagnostics
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