keyword
https://read.qxmd.com/read/37765151/abiraterone-acetate-complexes-with-biometals-synthesis-characterization-in-solid-and-solution-and-the-nature-of-chemical-bonding
#21
JOURNAL ARTICLE
Petr Buikin, Anna Vologzhanina, Roman Novikov, Pavel Dorovatovskii, Alexander Korlyukov
Abiraterone acetate (AbirAc) is the most used steroidal therapeutic agent for treatment of prostate cancer. The mainly hydrophobic molecular surface of AbirAc results in its poor solubility and plays an important role for retention of abiraterone in the cavity of the receptor formed by peptide chains and heme fragments. In order to evaluate the hydrolytic stability of AbirAc, to modify its solubility by formation of new solid forms and to model bonding of this medication with the heme, a series of d-metal complexes with AbirAc was obtained...
August 23, 2023: Pharmaceutics
https://read.qxmd.com/read/37713984/a-fully-validated-method-for-simultaneous-determination-of-icotinib-osimertinib-gefitinib-and-o-desmethyl-gefitinib-in-human-plasma-using-uplc-ms-ms-for-therapeutic-drug-monitoring
#22
JOURNAL ARTICLE
Bo Li, Wenqian Chen, Fang Liu, Xiaoxue Wang, Wei Qin, Shu Li, Hongkai Lu, Guan Wang, Xiaoyang Liu, Pengmei Li, Xianbo Zuo, Xianglin Zhang, Lihong Liu, Meng Yang
BACKGROUND AND AIMS: A few researches have reported the exposure-efficacy/toxicity relationships of epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs). On account of the large interpatient pharmacokinetic variability, therapeutic drug monitoring (TDM) seems promising for optimizing dosage regimen and improving treatment efficacy and safety. Therefore, a rapid and convenient ultrahigh performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was developed and validated for the determination of icotinib, osimertinib, gefitinib and O-demesthyl gefitinib in human plasma for TDM...
September 3, 2023: Journal of Pharmaceutical and Biomedical Analysis
https://read.qxmd.com/read/37674107/the-panda-derived-lactiplantibacillus-plantarum-bsg201683-improves-lps-induced-intestinal-inflammation-and-epithelial-barrier-disruption-in-vitro
#23
JOURNAL ARTICLE
Yi Zhou, Ling Duan, Yan Zeng, Xu Song, Kangcheng Pan, Lili Niu, Yang Pu, Jiakun Li, Abdul Khalique, Jing Fang, Bo Jing, Dong Zeng, Bairong Shen, Xueqin Ni
Captive pandas are suffering from intestinal infection due to intestinal microbiota characterized by a high abundance of Enterobacteriaceae induced by long-term captivity. Probiotic supplements showed improvement in intestinal barrier function and inflammation. However, the effects of panda-derived probiotics on the intestinal epithelium and inflammation have not been elucidated. In the present study, lipopolysaccharide (LPS) impaired Caco-2 and RAW264.7 inflammatory models were applied to assess the protection of Lactiplantibacillus plantarum BSG201683 (L...
September 6, 2023: BMC Microbiology
https://read.qxmd.com/read/37646374/pharmacology-and-therapeutic-potential-of-benzothiazole-analogues-for-cocaine-use-disorder
#24
JOURNAL ARTICLE
Comfort A Boateng, Ashley N Nilson, Rebekah Placide, Mimi L Pham, Franziska M Jakobs, Noelia Boldizsar, Scot McIntosh, Leia S Stallings, Ivana V Korankyi, Shreya Kelshikar, Nisha Shah, Diandra Panasis, Abigail Muccilli, Maria Ladik, Brianna Maslonka, Connor McBride, Moises Ximello Sanchez, Ebrar Akca, Mohammad Alkhatib, Julianna Saez, Catherine Nguyen, Emily Kurtyan, Jacquelyn DePierro, Raymond Crowthers, Dylan Brunt, Alessandro Bonifazi, Amy Hauck Newman, Rana Rais, Barbara S Slusher, R Benjamin Free, David R Sibley, Kent D Stewart, Chun Wu, Scott E Hemby, Thomas M Keck
Pharmacological targeting of the dopamine D4 receptor (D4 R)─expressed in brain regions that control cognition, attention, and decision-making─could be useful for several neuropsychiatric disorders including substance use disorders (SUDs). This study focused on the synthesis and evaluation of a novel series of benzothiazole analogues designed to target D4 R. We identified several compounds with high D4 R binding affinity ( Ki ≤ 6.9 nM) and >91-fold selectivity over other D2 -like receptors (D2 R, D3 R) with diverse partial agonist and antagonist profiles...
August 30, 2023: Journal of Medicinal Chemistry
https://read.qxmd.com/read/37590410/cd44-acts-as-a-coreceptor-for-cell-specific-enhancement-of-signaling-and-regulatory-t-cell-induction-by-tgm1-a-parasite-tgf-%C3%AE-mimic
#25
JOURNAL ARTICLE
Maarten van Dinther, Kyle T Cunningham, Shashi Prakash Singh, Madeleine P J White, Tiffany Campion, Claire Ciancia, Peter A van Veelen, Arnoud H de Ru, Román González-Prieto, Ananya Mukundan, Chang-Hyeock Byeon, Sophia R Staggers, Cynthia S Hinck, Andrew P Hinck, Peter Ten Dijke, Rick M Maizels
Long-lived parasites evade host immunity through highly evolved molecular strategies. The murine intestinal helminth, Heligmosomoides polygyrus , down-modulates the host immune system through release of an immunosuppressive TGF-β mimic, TGM1, which is a divergent member of the CCP (Sushi) protein family. TGM1 comprises 5 domains, of which domains 1-3 (D1/2/3) bind mammalian TGF-β receptors, acting on T cells to induce Foxp3+ regulatory T cells; however, the roles of domains 4 and 5 (D4/5) remain unknown...
August 22, 2023: Proceedings of the National Academy of Sciences of the United States of America
https://read.qxmd.com/read/37588794/canine-interleukin-31-binds-directly-to-osmr%C3%AE-with-higher-binding-affinity-than-to-il-31ra
#26
JOURNAL ARTICLE
Yuxin Zheng, Jing Zhang, Tianling Guo, Jin Cao, Lixian Wang, Jie Zhang, Xuefei Pang, Feng Gao, Hua Sun, Haixia Xiao
Interleukin-31 (IL-31) is a pro-inflammatory cytokine involved in skin inflammation and tumor progression. The IL-31 signaling cascade is initiated by its binding to two receptors, IL-31 receptor alpha (IL-31RA) and oncostatin M receptor subunit beta (OSMRβ). The previous study suggested that human IL-31 (hIL-31) directly interacts with IL-31RA and OSMRβ, independently, but the binding ability of hIL-31 to IL-31RA is stronger than to OSMRβ. In different to its human ortholog, feline IL-31 (fIL-31) has a higher binding affinity for feline OSMRβ...
September 2023: 3 Biotech
https://read.qxmd.com/read/37531334/genetic-polymorphisms-in-the-serotonin-dopamine-and-opioid-pathways-influence-social-attention-in-rhesus-macaques-macaca-mulatta
#27
JOURNAL ARTICLE
Emmeline R I Howarth, Isabelle D Szott, Claire L Witham, Craig S Wilding, Emily J Bethell
Behaviour has a significant heritable component; however, unpicking the variants of interest in the neural circuits and molecular pathways that underpin these has proven difficult. Here, we present a comprehensive analysis of the relationship between known and new candidate genes from identified pathways and key behaviours for survival in 109 adult rhesus macaques (Macaca mulatta). Eight genes involved in emotion were analysed for variation at a total of nine loci. Genetic data were then correlated with cognitive and observational measures of behaviour associated with wellbeing and survival using MCMC-based Bayesian GLMM in R, to account for relatedness within the macaque population...
2023: PloS One
https://read.qxmd.com/read/37509696/decreased-platelet-aggregation-in-patients-with-decompensated-liver-cirrhosis-and-tips-implantation
#28
JOURNAL ARTICLE
Asala Nassar, Jan Patrick Huber, Daniela Stallmann, Diana Sharipova, Muataz Ali Hamad, Michael Schultheiss, Robert Thimme, Daniel Duerschmied, Rüdiger Eberhard Scharf, Dominik Bettinger, Krystin Krauel
Transjugular intrahepatic portosystemic shunt (TIPS) implantation is an effective treatment of portal hypertension in patients with decompensated liver cirrhosis. However, some patients develop TIPS thrombosis with recurrence of portal hypertension. The role of platelets in TIPS thrombosis and the necessity of antiplatelet therapy is unclear. Therefore, we aimed to study platelet function in patients with liver cirrhosis prior to and after TIPS implantation. Platelet aggregation was tested in peripheral and portal-vein blood patient samples on the day (D) of TIPS implantation (D0), D4 and D30 following the procedure (platelet count above 100 × 103 /µL, aspirin starting on D5) using whole-blood impedance aggregometry (WBIA) and light transmission aggregometry (LTA)...
July 21, 2023: Biomedicines
https://read.qxmd.com/read/37499734/in-vivo-synaptic-potency-short-term-and-long-term-plasticity-at-the-hippocampal-schaffer-collateral-ca1-synapses-role-of-different-light-dark-cycles-in-male-rats
#29
JOURNAL ARTICLE
Maryam Radahmadi, Kowsar Salehifard, Parham Reisi
The changes in the light-dark(L/D) cycle could modify cellular mechanisms in some brain regions. The present study compared the effects of various L/D cycles on invivo synaptic potency, short-term and long-term plasticity in the hippocampal CA1 area, adrenal glands weight(AGWs), corticosterone (CORT) levels, and body weight differences(BWD) in male rats. Male rats were assigned into different L/D cycle groups: L4/D20, L8/D16, L12/D12(control), L16/D8, and L20/D4. The slope, amplitude, and the area under curve(AUC) related to the field excitatory postsynaptic potentials(fEPSPs) were assessed, using the input-output(I/O) functions, paired-pulse(PP) responses at different interpulse intervals, and after the induction of long-term potentiation(LTP) in the hippocampal CA1 area...
July 25, 2023: Brain Research
https://read.qxmd.com/read/37464153/significant-functional-differences-between-dopamine-d-4-receptor-polymorphic-variants-upon-heteromerization-with-%C3%AE-1a-adrenoreceptors
#30
JOURNAL ARTICLE
Patricia Homar-Ruano, Ning-Sheng Cai, Verònica Casadó-Anguera, Vicent Casadó, Sergi Ferré, Estefanía Moreno, Enric I Canela
The functional role of the dopamine D4 receptor (D4 R) and its main polymorphic variants has become more evident with the demonstration of heteromers of D4 R that control the function of frontal cortico-striatal neurons. Those include heteromers with the α2A adrenoceptor (α2A R) and with the D2 R, localized in their cortical somato-dendritic region and striatal nerve terminals, respectively. By using biophysical and cell-signaling methods and heteromer-disrupting peptides in mammalian transfected cells and rat brain slice preparations, here we provide evidence for a new functionally relevant D4 R heteromer, the α1A R-D4 R heteromer, which is also preferentially localized in cortico-striatal glutamatergic terminals...
July 18, 2023: Molecular Neurobiology
https://read.qxmd.com/read/37450764/exploring-structural-determinants-of-bias-among-d4-subtype-selective-dopamine-receptor-agonists
#31
JOURNAL ARTICLE
Fabian Graßl, Leonard Bock, Álvaro Huete-Huerta González, Martin Schiller, Peter Gmeiner, Jörg König, Martin F Fromm, Harald Hübner, Markus R Heinrich
The high affinity dopamine D4 receptor ligand APH199 and derivatives thereof exhibit bias toward the Gi signaling pathway over β-arrestin recruitment compared to quinpirole. Based on APH199, two novel groups of D4 subtype selective ligands were designed and evaluated, in which the original benzyl phenylsemicarbazide substructure was replaced by either a biphenylmethyl urea or a biphenyl urea moiety. Functional assays revealed a range of different bias profiles among the newly synthesized compounds, namely, with regard to efficacy, potency, and GRK2 dependency, in which bias factors range from 1 to over 300 and activation from 15% to over 98% compared to quinpirole...
July 14, 2023: Journal of Medicinal Chemistry
https://read.qxmd.com/read/37379214/npas4-mediated-dopaminergic-regulation-of-safety-memory-consolidation
#32
JOURNAL ARTICLE
BumJin Ko, Jong-Yeon Yoo, Taesik Yoo, Woochul Choi, Rumeysa Dogan, Kibong Sung, Dahun Um, Su Been Lee, Hyun Jin Kim, Sangjun Lee, Seung Tae Beak, Sang Ki Park, Se-Bum Paik, Tae-Kyung Kim, Joung-Hun Kim
Amygdala circuitry encodes associations between conditioned stimuli and aversive unconditioned stimuli and also controls fear expression. However, whether and how non-threatening information for unpaired conditioned stimuli (CS- ) is discretely processed remains unknown. The fear expression toward CS- is robust immediately after fear conditioning but then becomes negligible after memory consolidation. The synaptic plasticity of the neural pathway from the lateral to the anterior basal amygdala gates the fear expression of CS- , depending upon neuronal PAS domain protein 4 (Npas4)-mediated dopamine receptor D4 (Drd4) synthesis, which is precluded by stress exposure or corticosterone injection...
June 27, 2023: Cell Reports
https://read.qxmd.com/read/37259420/towards-radiolabeled-egfr-specific-peptides-alternatives-to-ge11
#33
JOURNAL ARTICLE
Benedikt Judmann, Björn Wängler, Ralf Schirrmacher, Gert Fricker, Carmen Wängler
The human epidermal growth factor receptor (EGFR) is closely related to several cancer-promoting processes and overexpressed on a variety of tumor types, rendering it an important target structure for the imaging and therapy of several malignancies. To date, approaches to develop peptidic radioligands able to specifically address and visualize EGFR-positive tumors have been of limited success. Most of the attempts were based on the lead GE11, as this peptide was previously described to be a highly potent EGFR-specific agent...
February 11, 2023: Pharmaceuticals
https://read.qxmd.com/read/37239274/erectile-dysfunction-treatments-advances-and-new-therapeutic-strategies
#34
REVIEW
Antonio Argiolas, Francesco Mario Argiolas, Giacomo Argiolas, Maria Rosaria Melis
Erectile dysfunction (ED) is the inability to get and maintain an adequate penile erection for satisfactory sexual intercourse. Due to its negative impacts on men's life quality and increase during aging (40% of men between 40 and 70 years), ED has always attracted researchers of different disciplines, from urology, andrology and neuropharmacology to regenerative medicine, and vascular and prosthesis implant surgery. Locally and/or centrally acting drugs are used to treat ED, e.g., phosphodiesterase 5 inhibitors (first in the list) given orally, and phentolamine, prostaglandin E1 and papaverine injected intracavernously...
May 15, 2023: Brain Sciences
https://read.qxmd.com/read/37216997/effects-of-choline-supplementation-on-growth-performance-liver-histology-nonspecific-immunity-and-related-genes-expression-of-hybrid-grouper-%C3%A2-epinephelus-fuscoguttatus-%C3%A3-%C3%A2-e-lanceolatu-fed-with-high-lipid-diets
#35
JOURNAL ARTICLE
Tao Li, Xiaobo Yan, Xiaohui Dong, Simiao Pan, Beiping Tan, Shuang Zhang, Xiangxiang Suo, Weibin Huang, Menglong Zhou, Yuanzhi Yang
This study was conducted to evaluate the effect of dietary choline levels on growth performance, liver histology, nonspecific immunity and related gene expression of hybrid grouper (♀ Epinephelus fuscoguttatus × ♂ E. lanceolatus) fed with high-lipid diets. The fish (initial body weight 6.86 ± 0.01 g) were fed diets containing different choline levels (0, 5, 10, 15, and 20 g/kg, named D1, D2, D3, D4, and D5, respectively) for 8 weeks. The results showed that:(1) dietary choline levels had no significant effect on final body weight (FBW), feed conversion rate (FCR), visceral somatic index(VSI) and condition factor (CF) compared with the control group (P > 0...
July 2023: Fish & Shellfish Immunology
https://read.qxmd.com/read/37211288/differential-effects-of-dopamine-receptor-agonists-ropinirole-and-quinpirole-on-locomotor-and-anxiolytic-behaviors-in-larval-zebrafish-danio-rerio-a-role-for-the-gabaergic-and-glutamate-system
#36
JOURNAL ARTICLE
Andrew Wengrovitz, Emma Ivantsova, Natalie Crespo, Mansi Patel, Christopher L Souders, Christopher J Martyniuk
Zebrafish are frequently used as a vertebrate model to elucidate toxicological and pharmacological mechanisms of action in the central nervous system. Pharmacological studies demonstrate that dopamine, signaling via several receptor subtypes, regulates zebrafish larval behavior. Quinpirole is a selective dopamine receptor agonist for D2 and D3 subtypes while ropinirole exhibits selectivity toward D2, D3, and D4 receptors. The main objective of this study was to determine the short-term actions of quinpirole and ropinirole on the locomotor activity and anxiolytic/anti-anxiolytic behaviors of zebrafish...
May 19, 2023: Neurotoxicology and Teratology
https://read.qxmd.com/read/37206223/galactosylated-hydroxyl-polyamidoamine-dendrimer-targets-hepatocytes-and-improves-therapeutic-outcomes-in-a-severe-model-of-acetaminophen-poisoning-induced-liver-failure
#37
JOURNAL ARTICLE
Joshua E Porterfield, Rishi Sharma, Ambar Scarlet Jimenez, Nirnath Sah, Sean McCracken, Lucia Zhang, Hyoung-Tae An, Seulki Lee, Sujatha Kannan, Anjali Sharma, Rangaramanujam M Kannan
Toxicity to hepatocytes caused by various insults including drugs is a common cause of chronic liver failure requiring transplantation. Targeting therapeutics specifically to hepatocytes is often a challenge since they are relatively nonendocytosing unlike the highly phagocytic Kupffer cells in the liver. Approaches that enable targeted intracellular delivery of therapeutics to hepatocytes have significant promise in addressing liver disorders. We synthesized a galactose-conjugated hydroxyl polyamidoamine dendrimer (D4-Gal) that targets hepatocytes efficiently through the asialoglycoprotein receptors in healthy mice and in a mouse model of acetaminophen (APAP)-induced liver failure...
May 2023: Bioengineering & Translational Medicine
https://read.qxmd.com/read/37203102/can-montelukast-sodium-be-an-alternative-treatment-in-the-treatment-of-interstitial-cystitis
#38
JOURNAL ARTICLE
O C Gunizi, A Kol, H Gunizi
BACKGROUND: The leukotriene D4 receptors have been detected in human bladder detrusor myocytes, and they can play the role of interstitial cystitis etiology. AIM: Our study aims to explain the role of mast cells histologically and immunohistochemically in the pathogenesis and the effectiveness of montelukast that leukotriene D4 receptor antagonist in the treatment of interstitial cystitis. SUBJECTS AND METHODS: Twenty-four Wistar albino adult female rats were used...
April 2023: Nigerian Journal of Clinical Practice
https://read.qxmd.com/read/37165046/improved-predictability-of-pancreatic-ductal-adenocarcinoma-diagnosis-using-a-blood-immune-cell-biomarker-panel-developed-from-bulk-mrna-sequencing-and-single-cell-rna-sequencing
#39
JOURNAL ARTICLE
Sung Ill Jang, Hyung Keun Lee, Eun-Ju Chang, Somi Kim, So Young Kim, In Young Hong, Jong Kyoung Kim, Hye Sun Lee, Juyeon Yang, Jae Hee Cho, Dong Ki Lee
BACKGROUND: Pancreatic ductal adenocarcinoma (PDAC) remains a devastating cancer due to its poor survival rate, early detection, and resectability. This study aimed to determine the peripheral blood mononuclear cell (PBMC) immune biomarkers in patients with PDAC and investigate the PDAC-specific peripheral blood biomarker panel and validate its clinical performance. METHODS: In this prospective, blinded, case-control study, a biomarker panel formula was generated using a development cohort-including healthy controls, patients at high risk of PDAC, and patients with benign pancreatic disease, PDAC, or other gastrointestinal malignancies-and its diagnostic performance was verified using a validation cohort, including patients with ≥ 1 lesion suspected as PDAC on computed tomography (CT)...
May 10, 2023: Cancer Immunology, Immunotherapy: CII
https://read.qxmd.com/read/37145966/cost-effectiveness-analysis-of-car-t-cell-therapy-for-patients-with-relapsed-refractory-multiple-myeloma-in-china
#40
JOURNAL ARTICLE
Weijia Wu, Shuyi Ding, Zhang Mingming, Zhou Yuping, Xueshan Sun, Zixuan Zhao, Yi Yang, Yongxian Hu, Hengjin Dong
BACKGROUND: The landscape of treatment strategies for relapsed/refractory multiple myeloma (RRMM) has dramatically changed due to the emergence of chimeric antigen receptor T (CAR-T) cell therapy. The aim of this study was to evaluate the cost-effectiveness of two CAR-T cell treatments for RRMM patients from the perspective of the Chinese healthcare system. METHODS: Markov model was used to compare currently available salvage chemotherapy with Idecabtagene vicleucel (Ide-cel) and Ciltacabtagene autoleucel (Cilta-cel) for treatment of patients with RRMM...
May 5, 2023: Journal of Medical Economics
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