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C-kit ligand

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https://www.readbyqxmd.com/read/28075350/hydroxypyridinone-chelators-from-iron-scavenging-to-radiopharmaceuticals-for-pet-imaging-with-gallium-68
#1
REVIEW
Ruslan Cusnir, Cinzia Imberti, Robert C Hider, Philip J Blower, Michelle T Ma
Derivatives of 3,4-hydroxypyridinones have been extensively studied for in vivo Fe(3+) sequestration. Deferiprone, a 1,2-dimethyl-3,4-hydroxypyridinone, is now routinely used for clinical treatment of iron overload disease. Hexadentate tris(3,4-hydroxypyridinone) ligands (THP) complex Fe(3+) at very low iron concentrations, and their high affinities for oxophilic trivalent metal ions have led to their development for new applications as bifunctional chelators for the positron emitting radiometal, (68)Ga(3+), which is clinically used for molecular imaging in positron emission tomography (PET)...
January 8, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28040471/developmental-effects-of-imatinib-mesylate-on-follicle-assembly-and-early-activation-of-primordial-follicle-pool-in-postnatal-rat-ovary
#2
Babak Asadi-Azarbaijani, Regiane R Santos, Kirsi Jahnukainen, Saskia Braber, Majorie B M van Buursen, Jorma Toppari, Ola D Saugstad, Mirja Nurmio, Irma C Oskam
Imatinib mesylate is an anti-cancer agent that competitively inhibits several receptor tyrosine kinases (RTKs). RTKs play important roles in the regulation of primordial follicle formation, the recruitment of primordial follicles into the pool of growing follicles and maturation of the follicles. In the present study, we investigated the effects of the tyrosine kinase inhibitor imatinib on primordial follicle assembly and early folliculogenesis in postnatal rats. Female Sprague-Dawley rats were treated with either imatinib (150mg/kg) or placebo (water) on postnatal days 2-4...
December 28, 2016: Reproductive Biology
https://www.readbyqxmd.com/read/28004478/cs2164-a-novel-multi-target-inhibitor-against-tumor-angiogenesis-mitosis-chronic-inflammation-with-anti-tumor-potency
#3
You Zhou, Song Shan, Zhi-Bin Li, Li-Jun Xin, De-Si Pan, Qian-Jiao Yang, Ying-Ping Liu, Xu-Peng Yue, Xiao-Rong Liu, Ji-Zhou Gao, Jin-Wen Zhang, Zhi-Qiang Ning, Xian-Ping Lu
Although inhibitors targeting tumor angiogenic pathway have provided improvement for clinical treatment in patients with various solid tumors, the still very limited anti-cancer efficacy and acquired drug resistance demand new agents that may offer better clinical benefits. In the efforts of finding a small molecule potentially targeting several key pathways for tumor development, we designed, discovered and evaluated a novel multi-kinase inhibitor, CS2164. CS2164 inhibited the angiogenesis-related kinases (VEGFR2, VEGFR1, VEGFR3, PDGFRα, and c-Kit), mitosis-related kinase Aurora B, and chronic inflammatory-related kinase CSF-1R in a high potency manner with the IC50 at a single digital nanomolar range...
December 22, 2016: Cancer Science
https://www.readbyqxmd.com/read/27899264/cyclic-ferrocenylnaphthalene-diimide-derivative-as-a-new-class-of-g-quadruplex-dna-binding-ligand
#4
Md Monirul Islam, Shinobu Sato, Shingo Shinozaki, Shigeori Takenaka
To identify an effective ligand that binds to a G-quadruplex structure but not a double-stranded DNA (dsDNA), a set of biophysical and biochemical experiments were carried out using newly synthesized cyclic ferrocenylnaphthalene diimide (cFNDI, 1) or the non-cyclic derivative (2) with various structures of G-quadruplex DNAs and dsDNA. Compound 1 bound strongly to G-quadruplexes DNAs (10(6)M(-1) order) with diminished binding to dsDNA (10(4)M(-1) order) in 100mM AcOH-AcOK buffer (pH 5.5) containing 100mM KCl...
January 15, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27872880/data-on-quantification-of-signaling-pathways-activated-by-kit-and-pdgfra-mutants
#5
Christelle Bahlawane, Martine Schmitz, Elisabeth Letellier, Karthik Arumugam, Nathalie Nicot, Petr V Nazarov, Serge Haan
The present data are related to the article entitled "Insights into ligand stimulation effects on gastro-intestinal stromal tumors signaling" (C. Bahlawane, M. Schmitz, E. Letellier, K. Arumugam, N. Nicot, P.V. Nazarov, S. Haan, 2016) [1]. Constitutive and ligand-derived signaling pathways mediated by KIT and PDGFRA mutated proteins found in gastrointestinal stromal tumors (GIST) were compared. Expression of mutant proteins was induced by doxycycline in an isogenic background (Hek293 cells). Kit was identified by FACS at the cell surface and found to be quickly degraded or internalized upon SCF stimulation for both Kit Wild type and Kit mutant counterparts...
December 2016: Data in Brief
https://www.readbyqxmd.com/read/27855694/cd274-promotes-cell-cycle-entry-of-leukemia-initiating-cells-through-jnk-cyclin-d2-signaling
#6
Xia Fang, Chiqi Chen, Fangzhen Xia, Zhuo Yu, Yaping Zhang, Feifei Zhang, Hao Gu, Jiangbo Wan, Xiaocui Zhang, Wei Weng, Cheng Cheng Zhang, Guo-Qiang Chen, Aibing Liang, Li Xie, Junke Zheng
BACKGROUND: CD274 (programmed death ligand 1, also known as B7H1) is expressed in both solid tumors and hematologic malignancies and is of critical importance for the escape of tumor cells from immune surveillance by inhibiting T cell function via its receptor, programmed death 1 (PD-1). Increasing evidence indicates that functional monoclonal antibodies of CD274 may potently enhance the antitumor effect in many cancers. However, the role of CD274 in leukemia-initiating cells (LICs) remains largely unknown...
November 17, 2016: Journal of Hematology & Oncology
https://www.readbyqxmd.com/read/27822137/axitinib-has-antiangiogenic-and-antitumorigenic-activity-in-myxoid-liposarcoma
#7
Lauren T Kerr, Jacqueline F Donoghue, Alexander L Wilding, Terrance G Johns
Myxoid liposarcoma is a rare form of soft-tissue sarcoma. Although most patients initially respond well to treatment, approximately 21% relapse, highlighting the need for alternative treatments. To identify novel treatment regimens and gain a better understanding of myxoid liposarcoma tumor biology, we screened various candidate and approved targeted therapeutics and chemotherapeutics against myxoid liposarcoma cell lines. Therapeutics that target angiogenesis showed antitumor activity. The small molecule inhibitor axitinib, which targets angiogenesis by inhibiting the VEGFR and PDGFR families and c-Kit, inhibited cell cycle progression and induced apoptosis in vitro, as well as having significant antitumor activity against MLS 1765 myxoid liposarcoma xenografts in mice...
2016: Sarcoma
https://www.readbyqxmd.com/read/27818316/tnf-r1-and-fadd-mediate-uvb-induced-activation-of-k-channels-in-corneal-epithelial-cells
#8
Peter M Boersma, Loren D Haarsma, Mark P Schotanus, John L Ubels
The goal of this study was to elucidate the role of Fas, TNF-R1, FADD and cytochrome c in UVB-induced K(+) channel activation, an early step in UVB-induced apoptosis, in human corneal limbal epithelial (HCLE) cells. HCLE cells were treated with Fas, TNF-R1 or FADD siRNA and exposed to 80 or 150 mJ/cm(2) UVB. K(+) channel activation and loss of intracellular K(+) were measured using whole-cell patch-clamp recording and ion chromatography, respectively. Cytochrome c was measured with an ELISA kit. Cells in which Fas was knocked down exhibited identical UVB-induced K(+) channel activation and loss of intracellular K(+) to control cells...
November 3, 2016: Experimental Eye Research
https://www.readbyqxmd.com/read/27802519/antiapoptotic-effect-of-acetylcholine-in-fas-induced-apoptosis-in-human-keratocytes
#9
Marta Sloniecka, Ludvig J Backman, Patrik Danielson
Purpose: To investigate the possible antiapoptotic effect of acetylcholine (ACh) in Fas-mediated apoptosis of primary human keratocytes in vitro, and to explore the underlying mechanism. Methods: Primary human keratocytes were isolated from healthy corneas. Fas ligand (FasL) was used to induce apoptosis in keratocytes. Cell death was assessed by ELISA. Activity of caspase-3, -7, -8, and -9 was measured with luminescent caspase activity assays. Expression of nuclear factor-κB (NF-κB) gene was assessed with RT-quantitative (q)PCR...
November 1, 2016: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/27788708/-role-of-neutrophils-in-treatment-of-rats-with-d-galactosamine-induced-acute-liver-failure-with-bone-marrow-mesenchymal-stem-cells
#10
X Zhao, X L Shi, Z H Zhang, H C Ma, X W Yuan, Y T Ding
Objective: To investigate the therapeutic effect of bone marrow mesenchymal stromal cell (BMSC) transplantation on D-galactosamine-induced acute liver failure in Sprague-Dawley (SD) rats, as well as the mechanism of neutrophils in this process. Methods: A total of 39 male SD rats were divided into control group (8 rats, intraperitoneal injection of isotonic saline), model group (10 rats, intraperitoneal injection of D-galactosamine), solvent group (9 rats, tail vein injection of isotonic saline at 2 hours after intraperitoneal injection of D-galactosamine), and treatment group (12 rats, tail vein injection of MSCs at 2 hours after intraperitoneal injection of D-galactosamine)...
August 20, 2016: Zhonghua Gan Zang Bing za Zhi, Zhonghua Ganzangbing Zazhi, Chinese Journal of Hepatology
https://www.readbyqxmd.com/read/27717372/development-of-a-programmed-cell-death-ligand-1-immunohistochemical-assay-validated-for-analysis-of-non-small-cell-lung-cancer-and-head-and-neck-squamous-cell-carcinoma
#11
Marlon C Rebelatto, Anita Midha, Amita Mistry, Constantine Sabalos, Nicole Schechter, Xia Li, Xiaoping Jin, Keith E Steele, Paul B Robbins, John A Blake-Haskins, Jill Walker
BACKGROUND: A high-quality programmed cell-death ligand 1 (PD-L1) diagnostic assay may help predict which patients are more likely to respond to anti-programmed cell death-1 (PD-1)/PD-L1 antibody-based cancer therapy. Here we describe a PD-L1 immunohistochemical (IHC) staining protocol developed by Ventana Medical Systems Inc. and key analytical parameters of its use in formalin-fixed, paraffin-embedded (FFPE) samples of non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC)...
October 8, 2016: Diagnostic Pathology
https://www.readbyqxmd.com/read/27704558/bone-shaft-revascularization-after-marrow-ablation-is-dramatically-accelerated-in-bsp-mice-along-with-faster-haematopoietic-recolonization
#12
Wafa Bouleftour, Renata Neves Granito, Arnaud Vanden-Bossche, Odile Sabido, Bernard Roche, Mireille Thomas, Marie Thérèse Linossier, Jane E Aubin, Marie-Hélène Lafage-Proust, Laurence Vico, Luc Malaval
The bone organ integrates the activity of bone tissue, bone marrow and blood vessels and the factors ensuring this coordination remain ill defined. Bone sialoprotein (BSP) is with osteopontin (OPN) a member of the Small Integrin Binding Ligand N-Linked Glycoprotein (SIBLING) family, involved in bone formation, hematopoiesis and angiogenesis. In rodents, bone marrow ablation induces a rapid formation of medullary bone which peaks by ∼8 days (d8) and is blunted in BSP-/- mice. We investigated the coordinate hematopoietic and vascular recolonization of the bone shaft after marrow ablation of 2 month old BSP + /+ and BSP-/- mice...
October 5, 2016: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/27698080/tyrosine-kinase-receptor-expression-in-canine-liposarcoma
#13
G Avallone, V Pellegrino, P Roccabianca, E Lepri, L Crippa, G Beha, L De Tolla, G Sarli
The expression of tyrosine kinase receptors is attracting major interest in human and veterinary oncological pathology because of their role as targets for adjuvant therapies. Little is known about tyrosine kinase receptor (TKR) expression in canine liposarcoma (LP), a soft tissue sarcoma. The aim of this study was to evaluate the immunohistochemical expression of the TKRs fibroblast growth factor receptor 1 (FGFR1) and platelet-derived growth factor receptor-β (PDGFRβ); their ligands, fibroblast growth factor 2 (FGF2) and platelet-derived growth factor B (PDGFB); and c-kit in canine LP...
October 3, 2016: Veterinary Pathology
https://www.readbyqxmd.com/read/27566408/microrna-expression-profiles-in-testicular-biopsies-of-patients-with-impaired-spermatogenesis
#14
P Noveski, K Popovska-Jankovic, K Kubelka-Sabit, V Filipovski, S Lazarevski, T Plaseski, D Plaseska-Karanfilska
Spermatogenesis is a complex process that involves thousands of genes whose expression during different stages is strictly regulated. Small non-coding microRNAs play an important role in the posttranscriptional regulation of mRNA processing during spermatogenesis. Using Agilent SurePrint v16 microRNA 8 × 60 K microarray kit, we investigated the microRNA expression profiles of 24 formalin-fixed paraffin-embedded testicular biopsies from patients with hypospermatogenesis (n = 10), hypospermatogenesis and azoospermia factor c region on the Y chromosome (AZFc) deletion (n = 3), Sertoli cell-only syndrome (n = 3) and maturation arrest (n = 2), in comparison with subjects with normal spermatogenesis (n = 6)...
August 27, 2016: Andrology
https://www.readbyqxmd.com/read/27563224/cocculus-hirsutus-molecular-docking-to-identify-suitable-targets-for-hepatocellular-carcinoma-by-in-silico-technique
#15
B Samuel Thavamani, Molly Mathew, S P Dhanabal
BACKGROUND: Protein-ligand interaction plays a major role in identification of the possible mechanism by which a ligand can bind with the target and exerts the pharmacological action. OBJECTIVE: The aim is to identify the best candidate of Cocculus hirsutus which binds with the hepatocellular carcinoma (HCC) targets by docking studies. MATERIALS AND METHODS: The reported phytoconstituents such as coclaurine, hirsutine, cohirsine, cohirsinine, lirioresinol, cohirsitinine, haiderine, jamtinine, isotrilobine, shaheenine, jamtine, and cocsoline present in the plant, C...
May 2016: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/27511040/-effect-of-zinc-ion-on-the-expression-of-osteoblastic-proteins-in-mc3t3-e1-cells-in-inflammatory-environment
#16
J Z Tan, E M Nie, C Y Zhang, R Jiang
OBJECTIVE: To investigate the effect of zinc ion on the expression of osteoblastic proteins. METHODS: Mice osteoblasts MC3T3-E1 cells were subcultured. Inflammatory environment model was established by tumor necrosis factor α(TNF-α)at a concentration of 10 mg/L. According to different concentration of Zn(2+), the cells were divided into TNF-α group, control group, group A(TNF-α+10(-4) mol/L Zn(2+)), group B(TNF-α+10(-5) mol/L Zn(2+)), group C(TNF-α+10(-6) mol/L Zn(2+))...
August 2016: Zhonghua Kou Qiang Yi Xue za Zhi, Zhonghua Kouqiang Yixue Zazhi, Chinese Journal of Stomatology
https://www.readbyqxmd.com/read/27492081/effect-of-kit-ligand-on-natriuretic-peptide-precursor-c-and-oocyte-maturation-in-cattle
#17
Paula F Lima, Cinthia M Ormond, Ester S Caixeta, Rodrigo G Barros, Christopher A Price, José Buratini
In vitro maturation (IVM) of oocytes in cattle is inefficient, and there is great interest in the development of approaches to improve maturation and fertilization rates. Intraovarian signalling molecules are being explored as potential additives to IVM media. One such factor is kit ligand (KITL), which stimulates the growth of oocytes. We determined if KITL enhances oocyte maturation in cattle. The two main isoforms of KITL (KITL1 and KITL2) were expressed in bovine cumulus-oocyte complexes (COC), and levels of mRNA increased during FSH-stimulated IVM...
November 2016: Reproduction: the Official Journal of the Society for the Study of Fertility
https://www.readbyqxmd.com/read/27478893/total-glucosides-of-paeony-promote-intestinal-motility-in-slow-transit-constipation-rats-through-amelioration-of-interstitial-cells-of-cajal
#18
Feiye Zhu, Shan Xu, Yongsheng Zhang, Fangming Chen, Jinjun Ji, Guanqun Xie
OBJECTIVES: Using an atropine-diphenoxylate-induced slow transit constipation (STC) model, this study explored the effects of the total glucosides of paeony (TGP) in the treatment of STC and the possible mechanisms. STUDY DESIGN: A prospective experimental animal study. METHODS: The constipation model was set up in rats with an oral gavage of atropine-diphenoxylate and then treated with the TGP. The volume and moisture content of the faeces were observed and the intestinal kinetic power was evaluated...
2016: PloS One
https://www.readbyqxmd.com/read/27446554/cxcl8-il-1%C3%AE-and-scd200-are-pro-inflammatory-cytokines-and-their-levels-increase-in-the-circulation-of-breast-carcinoma-patients
#19
Betul Celik, Arzu Didem Yalcin, Gizem Esra Genc, Tangul Bulut, Sibel Kuloglu Genc, Saadet Gumuslu
The influence of biomarkers on carcinogenesis has been investigated extensively. Whether they promote carcinogenesis or work against cancer development remains to be elucidated. To the best of our knowledge, the novel molecule cluster of differentiation 200 (CD200) has not been studied on human breast cancer subjects. The present study aimed to evaluate interleukin-1β (IL-1β), C-X-C motif chemokine ligand 8 (CXCL8), cancer antigen 15.3 (CA 15.3) and the soluble CD200 (sCD200) levels in the serum samples of breast carcinoma patients in order to predict their role in breast carcinoma...
August 2016: Biomedical Reports
https://www.readbyqxmd.com/read/27340921/impact-of-the-scf-signaling-pathway-on-leukemia-stem-cell-mediated-atl-initiation-and-progression-in-an-hbz-transgenic-mouse-model
#20
Wakako Kuribayashi, Kazuya Takizawa, Kenji Sugata, Madoka Kuramitsu, Haruka Momose, Eita Sasaki, Yuki Hiradate, Keiko Furuhata, Yoshihisa Asada, Atsushi Iwama, Masao Matsuoka, Takuo Mizukami, Isao Hamaguchi
Adult T-cell leukemia (ATL) is a malignant disease caused by human T-lymphotropic virus type 1. In aggressive ATL, the response to chemotherapy is extremely poor. We hypothesized that this poor response is due to the existence of chemotherapy-resistant cells, such as leukemic stem cells. Previously, we successfully identified an ATL stem cell (ATLSC) candidate as the c-kit+/CD38-/CD71- cells in an ATL mouse model using Tax transgenic mice. Here, with a new ATL mouse model using HBZ-transgenic mice, we further discovered that the functional ATLSC candidate, which commonly expresses c-kit, is drug-resistant and has the ability to initiate tumors and reconstitute lymphomatous cells...
August 9, 2016: Oncotarget
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