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1

Santamaria, P., T. Utsugi, B. J. Park, N. Averill, S. Kawazu, and J. W. Yoon. "Beta-cell-cytotoxic CD8+ T cells from nonobese diabetic mice use highly homologous T cell receptor alpha-chain CDR3 sequences." Journal of Immunology 154, no. 5 (1995): 2494–503. http://dx.doi.org/10.4049/jimmunol.154.5.2494.

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Abstract Insulin-dependent diabetes mellitus (IDDM) in nonobese diabetic (NOD) mice results from a cell-mediated autoimmune process against pancreatic beta-cells. We have shown that beta-cell-cytotoxic CD8+ T cell clones can transfer IDDM to irradiated NOD mice if co-injected with nondiabetogenic CD4+ spleen T cells. To determine whether CTLs recruited to pancreatic islets recognize a restricted set of local Ags, we sequenced TCR-alpha and TCR-beta cDNA generated by anchor PCR from CD8+ CTL lines and clones derived from islets of 10 different NOD mice. These CTL lines were oligoclonal, but did
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2

Quentmeier, Hilmar, Claudia Pommerenke, and Hans G. Drexler. "Epigenetic Modifier Mutations in the LL-100 Panel." Blood 132, Supplement 1 (2018): 5271. http://dx.doi.org/10.1182/blood-2018-99-110060.

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Abstract The NCI-60 human cell line panel, developed for use in drug development comprises sixty human cancer cell lines derived from nine different tissues. Only six cell lines of the NCI-60 were derived from blood cancers. Therefore, most forms and subtypes of leukemia and lymphoma are not represented in the NCI-60 panel. To respond to this apparent gap, we suggest the novel LL-100 panel, 100 leukemia and lymphoma cell lines representing the major leukemia/lymphoma entities, for basic research and drug development. Whole exome sequencing and RNA sequencing were performed to identify mutation
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3

Moudgil, Tarsem, Bernard Fox, and Hong-Ming Hu. "85 Detection of human angiotensin-converting enzyme 2 receptor (hACE2R) on human cancer cell lines." Journal for ImmunoTherapy of Cancer 9, Suppl 2 (2021): A93. http://dx.doi.org/10.1136/jitc-2021-sitc2021.085.

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BackgroundSARS-CoV-2 infections have delayed administration of treatments for some patients with cancer, increasing the number of avoidable deaths. However, we hypothesized that infection of cancer cells with SARS-CoV-2 might increase the immunogenicity of those cancer cells. Here we sought to determine whether non-small cell lung cancer (NSCLC) and head and neck squamous cell cancer (HNSCC) cell lines could be a potential target of SARS-CoV-2, which binds and infects host cells via interactions between the viral spike glycoprotein and the human angiotensin-converting enzyme 2 receptor (hACE2)
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4

Nagai, T., H. Harigae, H. Ishihara, et al. "Transcription factor GATA-2 is expressed in erythroid, early myeloid, and CD34+ human leukemia-derived cell lines." Blood 84, no. 4 (1994): 1074–84. http://dx.doi.org/10.1182/blood.v84.4.1074.1074.

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Abstract To understand the functional roles that the GATA factors may play during hematopoietic cell differentiation, we examined the expression of GATA factor mRNAs and protein products in various human cell lines. Blot hybridization analyses demonstrated that GATA-1 and GATA-2 mRNAs are expressed abundantly in a set of cell lines established from human myelogenous leukemia cells, but the expression pattern of each factor is distinct. GATA-2 mRNA is expressed in all cell lines tested that express erythroid markers, and, in addition, the mRNA is also expressed in three CD34+ cell lines and two
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5

Nagai, T., H. Harigae, H. Ishihara, et al. "Transcription factor GATA-2 is expressed in erythroid, early myeloid, and CD34+ human leukemia-derived cell lines." Blood 84, no. 4 (1994): 1074–84. http://dx.doi.org/10.1182/blood.v84.4.1074.bloodjournal8441074.

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To understand the functional roles that the GATA factors may play during hematopoietic cell differentiation, we examined the expression of GATA factor mRNAs and protein products in various human cell lines. Blot hybridization analyses demonstrated that GATA-1 and GATA-2 mRNAs are expressed abundantly in a set of cell lines established from human myelogenous leukemia cells, but the expression pattern of each factor is distinct. GATA-2 mRNA is expressed in all cell lines tested that express erythroid markers, and, in addition, the mRNA is also expressed in three CD34+ cell lines and two early my
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6

Resar, Linda, Donna Marie Williams, Lingling Xian, et al. "High Mobility Group A1 Chromatin Remodeling Proteins Amplify Inflammatory Networks to Drive Leukemic Transformation in Chronic Myeloproliferative Neoplasia in Humans and JAK2V617F Transgenic Mouse Models." Blood 132, Supplement 1 (2018): 102. http://dx.doi.org/10.1182/blood-2018-99-119549.

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Abstract Introduction: Myeloproliferative neoplasms (MPN) are clonal hematopoietic stem cell (HSC) disorders characterized by overproduction of mature blood cells and increased risk of transformation to myelofibrosis (MF) and acute myeloid leukemia (AML), although molecular mechanisms driving disease progression remain elusive. While most patients who acquire a JAK2V617F mutation in CD34+ cells present with chronic, indolent Polycythemia Vera (PV), ~25% will progress to MF or AML. High Mobility Group A1/2 (HMGA1/2) genes encode oncogenic chromatin remodeling proteins which are overexpressed in
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7

Lindhout, E., A. Lakeman, M. L. Mevissen, and C. de Groot. "Functionally active Epstein-Barr virus-transformed follicular dendritic cell-like cell lines." Journal of Experimental Medicine 179, no. 4 (1994): 1173–84. http://dx.doi.org/10.1084/jem.179.4.1173.

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Follicular dendritic cells (FDC) are unique nonlymphoid cells found only in germinal centers. FDC can be distinguished from other accessory cells based on a characteristic set of cell surface markers. It is known that FDC are able to rescue germinal center B cells from apoptosis. To investigate the role of FDC in the process of selection and maturation of B cells during germinal center reactions, we tried to establish factor-independent immortalized FDC-like cell lines. Because freshly isolated FDC express the Epstein-Barr Virus (EBV) receptor CD21, we attempted EBV transformation on isolated
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8

Troeger, Anja, Pascal-David Johann, Mumine Senturk, Michael D. Milsom, and David A. Williams. "Intact Rac Signaling Is Important for Leukemia Cell Survival." Blood 116, no. 21 (2010): 2885. http://dx.doi.org/10.1182/blood.v116.21.2885.2885.

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Abstract Abstract 2885 Rho GTPases, Ras-related small G proteins, regulate multiple cell processes in hematopoietic cells. There is growing evidence that acute myeloid leukemia (AML) blasts and particularly MLL-rearranged AML blasts, rely on Rac activity (Mulloy JC et al, Blood, 2010). However, little is known about the role of these GTPases in acute lymphoblastic leukemia (ALL) and particularly precursor B cell ALL. To investigate the role of Rac and potential compensation by other GTPases in ALL, we first assessed the protein expression and activation of Rac in a number of B-ALL cell lines (
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9

Verheul, C., T. V. Kers, A. Van Der Ploeg, et al. "P11.47 Generation, characterisation and drug screening of patient-derivedIDH1-mutated glioma cell lines." Neuro-Oncology 21, Supplement_3 (2019): iii54. http://dx.doi.org/10.1093/neuonc/noz126.193.

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Abstract BACKGROUND Despite considerable scientific efforts, endogenous in vitro isocitrate dehydrogenase (IDH)-mutated glioma models remain scarce. Availability of these models is key to understanding underlying molecular mechanisms and vital for the development of new therapeutic interventions. We established and characterized a set of seven cell lines derived from IDH1-mutated gliomas and utilized them to investigate IDH-mutant glioma drug-response in vitro. MATERIAL AND METHODS Fresh tumor material was collected directly from the operating room, mechanically and enzymatically dissociated a
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10

Gozgit, Joseph M., Geraldine A. Bebernitz, Pankaj Patil, et al. "Effects of a Novel, Selective Jak2 Inhibitor, AZ60, on STAT5 Signaling and Cellular Growth in Jak2 V617F Cell Lines." Blood 110, no. 11 (2007): 3549. http://dx.doi.org/10.1182/blood.v110.11.3549.3549.

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Abstract A role for Jak2 in the etiology of the myeloproliferative diseases (MPDs) was discovered with the identification of a single activating point mutation, V617F, in the pseudokinase domain of JAK2. We have developed a Jak2 inhibitor, AZ60, which inhibits in vitro JAK2 enzyme activity with a Ki of 0.45 nM. AZ60 demonstrates inhibition of STAT5 phosphorylation and proliferation in a Tel-Jak2 engineered cell line with IC50 values of 18 and 23 nM, respectively. To understand the selectivity versus other Jak kinase family members we engineered three additional cell lines containing Tel fusion
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11

Sidorchuk, Yu V., A. A. Fomenkov, V. V. Kuznetsov, et al. "Variation in GFP Gene Expression in Arabidopsis thaliana Monoclonal Cell Lines." Biotekhnologiya 35, no. 1 (2019): 58–67. http://dx.doi.org/10.21519/0234-2758-2019-35-1-58-67.

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A set of transgenic Arabidopsis thaliana monoclonal cell lines has been created by selecting individual cells (cell aggregates) with random GFP gene integration events after the Agrobacterium-mediated transformation. The yield of the recombinant GFP ranged from 0.07 to 2.37% of the total soluble protein. Three lines with the highest, about 2% of the total soluble protein, accumulation of the target GFP protein were isolated. Areas of T-DNA insertions into the plant genome for 12 monoclonal cell lines were determined. The variation in this characteristic among 21 examined cell lines can serve a
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12

Garitano-Trojaola, Andoni, Eva Teufel, Matteo Claudio Da Via', et al. "The Role of NRAS G12D Mutations in the Response to Conventional Chemotherapy and 5-Azacitidine in Secondary AML." Blood 132, Supplement 1 (2018): 5148. http://dx.doi.org/10.1182/blood-2018-99-118484.

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Abstract Secondary Acute Myeloid Leukemia (sAML) accounts for 10-30% of all AML. It arises from a preexisting clonal disorder of hematopoiesis, such as myelodysplastic syndromes (MDS) or chronic myeloproliferative neoplasia (cMPN) in most cases (60-70%) or from exposure to a leukemogenic agent e.g. chemotherapy. sAML is generally considered to be of unfavorable prognosis, as treatment sensitivity is reduced, compared to de novo AML (dnAML) and overall survival is shortened. The incidence of AML associated NRAS are similar between sAML and dnAML (10 to 15%, Jelena D. Milosevic et al.). Prognost
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13

Hom, J. T., J. M. Stuart, and J. M. Chiller. "Murine T cells reactive to type II collagen. I. Isolation of lines and clones and characterization of their antigen-induced proliferative responses." Journal of Immunology 136, no. 3 (1986): 769–75. http://dx.doi.org/10.4049/jimmunol.136.3.769.

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Abstract Mice of the DBA/1 strain develop arthritis after immunization with native chick type II collagen. Although both a humoral and a cell-mediated response specific to type II collagen are associated with the disease, the underlying immunologic basis remains to be established. As an initial step to analyzing the involvement of cellular immunity in collagen-induced arthritis, we isolated and characterized T cell lines and clones specific to type II collagen. Two sets of T cell lines were obtained by limiting dilution. One set was found to react exclusively with denatured type II collagen, w
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14

Quentmeier, Hilmar, Roderick A. F. MacLeod, Julia Reinhardt, Margarete Zaborski, and Hans G. Drexler. "JAK2 V617F Tyrosine Kinase Mutation in Leukemia Cell Lines." Blood 106, no. 11 (2005): 4505. http://dx.doi.org/10.1182/blood.v106.11.4505.4505.

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Abstract It has recently been shown that the majority of patients with polycythemia vera, and substantial numbers of patients with idiopathic myelofibrosis and essential thrombocythemia, carry a single nucleotide mutation in the JAK2 gene. The JAK2 V617F mutation was also found in patients with other myeloproliferative disorders, though at lower percentages. The JAK2 point mutation may contribute to the development of these diseases, and the elucidation of the cellular function of mutated JAK2 might facilitate the development of a suitable drug. In numerous cases, the effects of a mutationally
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15

Al-saraireh, Yousef M., Ahmed M. M. Youssef, Fatemah O. F. O. Alshammari, et al. "Phytochemical characterization and anti-cancer properties of extract of Ephedra foeminea (Ephedraceae) aerial parts." Tropical Journal of Pharmaceutical Research 20, no. 8 (2022): 1675–81. http://dx.doi.org/10.4314/tjpr.v20i8.18.

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Purpose: To evaluate the phytochemical profile of methanol extract of Ephedra foeminea and assess its anti-carcer effect on a large set of normal and cancerous cell lines.
 Methods: Extraction of air-dried powder of aerial parts of E. foeminea was carried out with methanol. The bioactive compounds in the extract were determined using gas chromatography/mass spectrometry (GC-MS). The anti-cancer effect of the extract was determined by 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) assay against various types of normal and cancer cell lines. Serial concentrations of plan
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16

Bebb, Gwyn, Huong Muzik, Sophia Nguyen, Don Morris, and Douglas A. Stewart. "In Vitro and In Vivo Anti Lymphoma Effect of GX15-070 in Mantle Cell Lymphoma." Blood 108, no. 11 (2006): 4756. http://dx.doi.org/10.1182/blood.v108.11.4756.4756.

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Abstract Introduction Mantle cell lymphoma (MCL), an incurable B cell lymphoma, consistently over expresses bcl-2 despite not carrying the t(14;18). The attenuation of apoptosis by bcl-2 is thought to contribute to the malignant process and increase resistance to some cytotoxic agents. We recently demonstrated that GX15-070, a small molecular inhibitor of the BH3 binding groove of bcl-2, has activity against MCL cell lines in vitro. We set out to assess the effect of GX15-070 alone and in combination with Vincristine on the viability of MCL cells in vitro and in vivo. Methods 3 previously char
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17

Fichtner, A., H. Bohnenberger, O. Elakad, et al. "Proteomic profiling of cisplatin-resistant and cisplatin-sensitive germ cell tumour cell lines using quantitative mass spectrometry." World Journal of Urology 40, no. 2 (2022): 373–83. http://dx.doi.org/10.1007/s00345-022-03936-1.

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Abstract Purpose Advanced testicular germ cell tumours (GCT) generally have a good prognosis owing to their unique sensitivity towards cisplatin-based chemotherapies. However, cisplatin-resistant GCT have a poor outcome. Further studies are mandatory to better understand resistance mechanisms and develop therapeutic strategies for refractory GCTs. Methods Protein levels in cisplatin-resistant GCT cell lines of NTERA-2, NCCIT and 2102EP were analyzed by quantitative proteomic mass spectrometry (MS) in combination with stable isotope labelling by amino acids in cell culture (SILAC). Differential
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18

Abadleh, Mohammed M., Mustafa M. El-Abadelah, Salim S. Sabri, Hanan H. Mohammed, Malek A. Zihlif, and Wolfgang Voelter. "Synthesis and Antitumor Activity of Some N2-(Thien-3-yl)amidrazones." Zeitschrift für Naturforschung B 69, no. 7 (2014): 811–16. http://dx.doi.org/10.5560/znb.2014-4062.

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6aA set of new N2-(thien-3-yl)amidrazones (-h) incorporating N-piperazines and related congeners has been synthesized by reacting the hydrazonoyl chloride 4(derived from 3-aminothiophene- 2-carboxylate) with the appropriate sec-cyclic amine. The antitumor activity of these compounds was evaluated on breast cancer (MCF-7) and leukemic (K562) cell lines by a cell viability assay utilizing the tetrazolium dye (MTT). The amidrazone 6d encompassing the N-piperazine moiety, was the most active against MCF-7 and K562 with IC50 of 7.28 and 9:91 μM, respectively.
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19

Ogato, Denis Mabeya, Eliakim Mbaka Mauti, Godfrey Omare Mauti, Barasa Ambrose, and David Keno Kowanga. "Anticancer activity of Eugenia jambolana seeds against Hep2 cell lines." Journal of Phytopharmacology 4, no. 6 (2016): 295–98. http://dx.doi.org/10.31254/phyto.2015.4604.

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Cancer is a life-threatening disease and leads to high rates of mortality worldwide, after cardiovascular disease, is the second leading cause of death. Investigations for finding new plant based anticancer compounds are imperative and interesting. There are many studies on anticancer herb/plant extracts in cell line models. Eugenia jambolana has been reported to contain phytochemicals like coumarin, flavanoids, glycosides, phenols, tannins and steroids. The various part of Eugenia jambolana have therapeutic applications. Plant active components were extracted using the decoction extraction me
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20

Reinke, Stefan O., Marion Bayer, Markus Berger, Stephan Hinderlich, and Véronique Blanchard. "The analysis of N-glycans of cell membrane proteins from human hematopoietic cell lines reveals distinctions in their pattern." Biological Chemistry 393, no. 8 (2012): 731–47. http://dx.doi.org/10.1515/hsz-2012-0195.

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Abstract Human cell lines are often different in their features and present variations in the glycosylation patterns of cell membrane proteins. Protein glycosylation is the most common posttranslational modification and plays a particular role in functionality and bioactivity. The key approach of this study is the comparative analysis of five hematopoietic cell lines for their N-glycosylation pattern. The N-glycans of membrane proteins were elucidated by matrix-assisted laser desorption ionization time-of-flight mass spectrometry (MALDI-TOF-MS) and MALDI-TOF/TOF-MS analyses. Furthermore, the e
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Willis, Clinton, Johanna Nyffeler, and Joshua Harrill. "Phenotypic Profiling of Reference Chemicals across Biologically Diverse Cell Types Using the Cell Painting Assay." SLAS DISCOVERY: Advancing the Science of Drug Discovery 25, no. 7 (2020): 755–69. http://dx.doi.org/10.1177/2472555220928004.

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Cell Painting is a high-throughput phenotypic profiling assay that uses fluorescent cytochemistry to visualize a variety of organelles and high-content imaging to derive a large number of morphological features at the single-cell level. Most Cell Painting studies have used the U-2 OS cell line for chemical or functional genomics screening. The Cell Painting assay can be used with many other human-derived cell types, given that the assay is based on the use of fluoroprobes that label organelles that are present in most (if not all) human cells. Questions remain, however, regarding the optimizat
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Kozako, Tomohiro, Teruhisa Shoji, Akiyoshi Aikawa, et al. "SIRT1, a Longevity Gene Encoded Protein, Regulates Apoptosis of Adult T-Cell Leukemia Cells and Its Inhibition by Sirtinol Induces Apoptosis." Blood 114, no. 22 (2009): 3684. http://dx.doi.org/10.1182/blood.v114.22.3684.3684.

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Abstract Abstract 3684 Poster Board III-620 Adult T-cell leukemia-lymphoma (ATL) is an aggressive peripheral T-cell neoplasm with a poor prognosis developing after long-term infection with human T-cell leukemia virus-1 (HTLV-1). HTLV-1 Tax is closely related to leukemic cell proliferation through nuclear factor-kappa B (NF-ƒÈB) activation. Recent studies have demonstrated that histone deacetylase class I/II inhibitors induce growth arrest and apoptosis of HTLV-1-infected T-cells via blockade of NF-ƒÈB signaling. SIRT1, an NAD(+)-dependent class III histone deacetylase, is widely recognized f
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23

Sherman, Emily J., Carmen Mirabelli, Vi T. Tang, et al. "Identification of cell type specific ACE2 modifiers by CRISPR screening." PLOS Pathogens 18, no. 3 (2022): e1010377. http://dx.doi.org/10.1371/journal.ppat.1010377.

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SARS-CoV-2 infection is initiated by binding of the viral spike protein to its receptor, ACE2, on the surface of host cells. ACE2 expression is heterogeneous both in vivo and in immortalized cell lines, but the molecular pathways that govern ACE2 expression remain unclear. We now report high-throughput CRISPR screens for functional modifiers of ACE2 surface abundance. In liver-derived HuH7 cells, we identified 35 genes whose disruption was associated with a change in the surface abundance of ACE2. Enriched among these ACE2 regulators were established transcription factors, epigenetic regulator
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24

Hattori, M., T. Sudo, M. Iizuka, et al. "Generation of continuous large granular lymphocyte lines by interleukin 2 from the spleen cells of mice infected with Moloney leukemia virus. Involvement of interleukin 3." Journal of Experimental Medicine 166, no. 4 (1987): 833–49. http://dx.doi.org/10.1084/jem.166.4.833.

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Continuous cell lines could be reproducibly established by culturing spleen cells from adult mice injected with MLV-producer cells or directly infected with Mo-MLV with rIL-2, whereas the culture of normal splenic cells with rIL-2 induced only transient and limited proliferation resulting in no such lines. All of the lines showed morphological characteristics as LGL with Thy-1+,Lyt-1-,L3T4-,Lyt-2-,AsGM1+,FcR gamma+ phenotype without exception, and most of them exhibited typical NK-patterned cytotoxicity. Analysis of reverse transcriptase activity of the culture supernatants as well as Southern
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25

Markovtsov, Vadim, Diane Yu, Marina Gelman, et al. "Targeting Myeloproliferative Diseases with JAK2 Inhibitors." Blood 110, no. 11 (2007): 3550. http://dx.doi.org/10.1182/blood.v110.11.3550.3550.

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Abstract Limited options provided by the current standard of care for the patients suffering from myeloproliferative diseases (MPDs) prompted an extensive search for the underlying molecular mechanisms of these disorders. Recent discovery of a single activating mutation (V617F) in JAK2 kinase gene associated with the development of the polycythemia vera (PV), essential thrombocythemia (ET) and chronic idiopathic myelofibrosis (CIMF) opened up a possibility to develop highly targeted therapies against these debilitating ailments. To that end, we engineered cytokine-independent Ba/F3 cell line e
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Li, Liping, Wenyan Lu, Alison R. Moliterno, et al. "High Mobility Group A1 Chromatin Regulators: Key Epigenetic Switches and Therapeutic Targets Required for Leukemic Transformation in JAK2 Mutant MPN." Blood 134, Supplement_1 (2019): 1680. http://dx.doi.org/10.1182/blood-2019-130262.

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Introduction: Myeloproliferative neoplasms (MPN) are clonal hematopoietic stem cell (HSC) disorders characterized by hyperactive JAK/STAT signaling and increased risk of transformation to myelofibrosis (MF) and acute myeloid leukemia (AML). However, mechanisms driving progression remain elusive and therapies are ineffective after leukemia develops. The High Mobility Group A1/2 (HMGA1/2) genes encode oncogenic chromatin remodeling proteins which are overexpressed in aggressive solid tumors where they portend adverse outcomes. HMGA1/2 genes are also up-regulated in hematologic malignancies and M
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Patel, Mrugesh, and Kaushal Patel. "Naphthalene substituted benzo[c]coumarins: Synthesis, characterization and evaluation of antibacterial activity and cytotoxicity." Heterocyclic Communications 25, no. 1 (2019): 146–51. http://dx.doi.org/10.1515/hc-2019-0024.

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AbstractNovel congeners of naphthalene substituted benzo[c]coumarins (2a-f) were synthesized by reaction of various 3-coumarinoyl methyl pyridinium bromide salts (1a-d) with a selected set of acetyl naphthalene in the presence of sodium acetate in refluxing glacial acetic acid. Structures of the synthesized compounds were confirmed by elemental analysis and by various spectroscopic techniques such as 1H-NMR, 13C-NMR, DEPT, and MS spectral data. Synthesised compounds were screened for antibacterial activity and cytotoxicity against different human cancer cell lines including cervix cancer (HeLa
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Aponte-López, Angélica, Jennifer Enciso, Samira Muñoz-Cruz, and Ezequiel M. Fuentes-Pananá. "An In Vitro Model of Mast Cell Recruitment and Activation by Breast Cancer Cells Supports Anti-Tumoral Responses." International Journal of Molecular Sciences 21, no. 15 (2020): 5293. http://dx.doi.org/10.3390/ijms21155293.

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Breast cancer (BrC) affects millions of women yearly. Mast cells (MCs) are common components of breast tumors with documented agonistic and antagonistic roles in tumor progression. Understanding the participation of MCs in BrC may lead to new therapies to control tumor growth. In this study, we looked into mechanistic models of MC responses triggered by BrC cells (BrCC), assessing both early degranulation and late transcriptional activities. We used aggressive and non-aggressive BrCC to model the progressive staging of the disease over HMC1 and LAD-2 human MC lines. We found that both MC lines
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Szafrański, Krzysztof, Jarosław Sławiński, Łukasz Tomorowicz, and Anna Kawiak. "Synthesis, Anticancer Evaluation and Structure-Activity Analysis of Novel (E)- 5-(2-Arylvinyl)-1,3,4-oxadiazol-2-yl)benzenesulfonamides." International Journal of Molecular Sciences 21, no. 6 (2020): 2235. http://dx.doi.org/10.3390/ijms21062235.

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To learn more about the structure–activity relationships of (E)-3-(5-styryl-1,3,4-oxadiazol-2-yl)benzenesulfonamide derivatives, which in our previous research displayed promising in vitro anticancer activity, we have synthesized a group of novel (E)-5-[(5-(2-arylvinyl)-1,3,4-oxadiazol-2-yl)]-4-chloro-2-R1-benzenesulfonamides 7–36 as well as (E)-4-[5-styryl1,3,4-oxadiazol-2-yl]benzenesulfonamides 47–50 and (E)-2-(2,4-dichlorophenyl)-5-(2-arylvinyl)-1,3,4-oxadiazols 51–55. All target derivatives were evaluated for their anticancer activity on HeLa, HCT-116, and MCF-7 human tumor cell lines. The
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30

Camacho, Cláudia, Helena Tomás, and João Rodrigues. "Use of Half-Generation PAMAM Dendrimers (G0.5–G3.5) with Carboxylate End-Groups to Improve the DACHPtCl2 and 5-FU Efficacy as Anticancer Drugs." Molecules 26, no. 10 (2021): 2924. http://dx.doi.org/10.3390/molecules26102924.

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The DACHPtCl2 compound (trans-(R,R)-1,2-diaminocyclohexanedichloroplatinum(II)) is a potent anticancer drug with a broad spectrum of activity and is less toxic than oxaliplatin (trans-l-diaminocyclohexane oxalate platinum II), with which it shares the active metal fragment DACHPt. Nevertheless, due to poor water solubility, its use as a chemotherapeutic drug is limited. Here, DACHPtCl2 was conjugated, in a bidentate form, with half-generation PAMAM dendrimers (G0.5–G3.5) with carboxylate end-groups, and the resulting conjugates were evaluated against various types of cancer cell lines. In this
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Rødland, Gro Elise, Katrine Melhus, Roman Generalov, et al. "The Dual Cell Cycle Kinase Inhibitor JNJ-7706621 Reverses Resistance to CD37 Targeted Radioimmunotherapy in Activated B Cell like Diffuse Large B Cell Lymphoma Cell Lines." Blood 134, Supplement_1 (2019): 2574. http://dx.doi.org/10.1182/blood-2019-123287.

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The CD37 targeting radioimmunoconjugate 177Lu-lilotomab satetraxetan (Betalutin®) is currently being evaluated as monotherapy in a clinical phase 2b trial for patients with follicular lymphoma (FL) and in a phase 1 trial for patients with diffuse large B-cell lymphoma (DLBCL), as well as in a phase 1b trial in combination with rituximab for patients with relapsed/refractory FL. Herein we have investigated the effect of 177Lu-lilotomab satetraxetan in seven activated B-cell like (ABC) DLBCL cell lines. Although the radioimmunoconjugate showed anti-tumor activity, primary resistance was observed
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Pietarinen, Paavo, Muntasir Mamun Majumder, Disha Malani, et al. "High-Throughput Drug Sensitivity and Resistance Testing (DSRT) Platform Reveals Novel Candidate Drugs For Advanced Phase BCR-ABL1-Positive Leukemia." Blood 122, no. 21 (2013): 2719. http://dx.doi.org/10.1182/blood.v122.21.2719.2719.

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Abstract Background Advanced BCR-ABL1-positive leukemias (chronic myeloid leukemia in blast crisis and Ph+ALL) remain a therapy challenge despite advances in tyrosine kinase inhibitor (TKI) therapy. Emergence of primary and secondary resistance due to gatekeeper and compound mutations within the BCR-ABL1 kinase domain is common even with the novel 2nd and 3rd generation TKIs (dasatinib, nilotinib, ponatinib). We set out to identify novel candidate drugs for advanced BCR-ABL1-positive leukemias by using an unbiased high-throughput drug testing platform and utilizing both primary patient cells a
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33

Davis, Carter Thomas, Arati V. Rao, Eross Guadalupe, Dale J. Christensen, and J. Brice Weinberg. "Fingolimod Is Cytotoxic in Acute Myeloid Leukemia Independent of Additional Chemotherapeutic Agents." Blood 128, no. 22 (2016): 5126. http://dx.doi.org/10.1182/blood.v128.22.5126.5126.

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Abstract INTRODUCTION: Conventional treatment of acute myeloid leukemia (AML) remains largely unchanged for over thirty years. With poor overall survival and disease cure rates, novel therapies are needed. The SET oncoprotein has been implicated in AML as essential for proliferation through inhibition of the tumor suppressor protein phosphatase 2A (PP2A). Interaction between SET and PP2A leads to inactivation of PP2A, leaving cell survival and proliferation signals unchecked. PP2A has been postulated to be an important target in AML. Fingolimod (FTY720), an FDA approved drug for relapsing-remi
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Cardile, Venera, Rosa Chillemi, Laura Lombardo, Sebastiano Sciuto, Carmela Spatafora, and Corrado Tringali. "Antiproliferative Activity of Methylated Analogues of E- and Z-Resveratrol." Zeitschrift für Naturforschung C 62, no. 3-4 (2007): 189–95. http://dx.doi.org/10.1515/znc-2007-3-406.

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Abstract The stilbenoids E-resveratrol (E-3,5,4′-trihydroxystilbene, 1), E-3,5,4′-trimethoxystilbene (2), E-3,4,4′-trimethoxystilbene (3) and E-3,4′-dimethoxy-5-hydroxystilbene (4) were converted by photoisomerization to their corresponding Z-isomers 5D8. Compounds 1D8 were subjected to antiproliferative activity bioassays towards a set of four different human cancer cell lines, namely DU-145 (androgen not responsive human prostate tumor), LNCaP (androgen responsive human prostate tumor), M-14 (human melanoma) and KB (human mouth epidermoid carcinoma). The methylated analogues of 1 are more ac
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Quentmeier, Hilmar, Sonja Eberth, Roderick AF MacLeod, et al. "CRLF2 and JAK2 Mutations: Occurrence and Function In Pre-B ALL Cell Lines." Blood 116, no. 21 (2010): 5109. http://dx.doi.org/10.1182/blood.v116.21.5109.5109.

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Abstract Abstract 5109 Thymic stromal lymphopoietin (TSLP), a cytokine produced by epithelial cells promotes early B-cell development and activates dendritic cells. It has recently been reported that a subset of B-cell precursor acute lymphoblastic leukemia (pre-B ALL) overexpresses the TSLP receptor CRLF2. CRLF2 overexpression is linked to translocations between sex chromosomes – localizing CRLF2 – and the immunoglobulin heavy chain locus on chromosome 14, or to an interstitial deletion on the gonosomes. Both events, translocation and deletion juxtapose CRLF2 to a different promoter (IgH or P
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Luo, Jia, He Xiao, Qian Chen, Yanlan Li, Chuan Chen, and Mingying Geng. "Abstract 5720: Niraparib enhances radiosensitivity of glioblastoma cells with proficient BRCA1/2 through proliferation-related nucleolar protein DDX21." Cancer Research 82, no. 12_Supplement (2022): 5720. http://dx.doi.org/10.1158/1538-7445.am2022-5720.

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Abstract Background Intrinsic resistance to irradiation is one of important factors leading to recurrence of glioblastoma (GBM) patients underwent standard treatment. The radiosensitization by various poly-(ADP-ribose)-polymerase (PARP) inhibitors have been intensively investigated in many solid tumor models especially harboring deficient BRCA1/2. However, the impact of a PARP1/2 inhibitor niraparib on radiosensitivity of glioblastoma cell lines with proficient BRCA1/2 and underling mechanisms has yet not been fully elucidated. Methods GDSC dataset with IC50 of PARP inhibitors and transcriptom
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Finlay, Jack, Clement Hallou, Pooran Dewari, et al. "Characterising a SOX2+ OLIG2+ glioma stem cell using Crispr-engineered fluorescent reporters in primary patient-derived GBM and DIPG cells." Neuro-Oncology 21, Supplement_4 (2019): iv9. http://dx.doi.org/10.1093/neuonc/noz167.039.

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Abstract Malignant glioma can be understood as a cancer stem cell disease. There is strong evidence that expression of a core set of neural stem cell master regulators is necessary and sufficient for tumour initiation in both adult and childhood disease subtypes, and across a range of underlying mutation signatures and expression profiles. We hypothesise that a double positive SOX2+ OLIG2+ progenitor is the cancer stem cell in H3K27M diffuse intrinsic pontine glioma (DIPG) and adult glioblastoma (GBM) alike. We present expression data in 4 patient-derived cell lines (2 adult GBM, 2 DIPG) in vi
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Lee, Jinyoung, Sou Hyun Kim, Seung Tae Kim, et al. "Discovery of 2-Anilinopyrimidine-based Selective Inhibitors against Non-small Cell Lung Cancer Cell Line H1975." Yakhak Hoeji 66, no. 6 (2022): 345–49. http://dx.doi.org/10.17480/psk.2022.66.6.345.

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Small molecular EGFR-tyrosine kinase inhibitors (EGFR-TKIs) have been proved as a successful and powerful strategy for the treatment of non-small-cell lung cancer (NSCLC). Recent studies have reported that the T790M mutation in EGFR is the most prevalent factor in acquired resistance for NSCLC patients. In an effort to identify small molecules for the inhibition of T790M mutant EGFR, a screening of our in-house chemical library was conducted by an MTT assay. A set of 2-anilinopyrimidine derivatives was rationally selected and then evaluated for their antiproliferative activities against three
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Tugcu, Gulcin, Hande Sipahi, and Ahmet Aydin. "Application of a Validated QSTR Model for Repurposing COX-2 Inhibitor Coumarin Derivatives as Potential Antitumor Agents." Current Topics in Medicinal Chemistry 19, no. 13 (2019): 1121–28. http://dx.doi.org/10.2174/1568026619666190618143552.

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Background: The discovery of novel potent molecules for both cancer prevention and treatment has been continuing over the past decade. In recent years, identification of new, potent, and safe anticancer agents through drug repurposing has been regarded as an expeditious alternative to traditional drug development. The cyclooxygenase-2 is known to be over-expressed in several types of human cancer. For this reason cyclooxygenase-2 inhibition may be useful tool for cancer chemotherapy. Objective: The first aim of the study was to develop a validated linear model to predict antitumor activity. Su
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Kawashima, Nozomu, Yusuke Okuno, Yuko Sekiya, et al. "Generation of Cell Lines Harboring SETBP1 Mutations By the Crispr/Cas9 System." Blood 124, no. 21 (2014): 4622. http://dx.doi.org/10.1182/blood.v124.21.4622.4622.

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Abstract Introduction Recent advances in cancer genetics have led to the identification of somatic mutations in SET-binding protein 1 (SETBP1) in myeloid malignancies categorized as myeloproliferative neoplasm (MPN) and myelodysplastic syndromes (MDS). Heterozygous point mutations in SETBP1 are essentially found at a genomic level in myeloid malignancies, and the frequency of the mutated allele in cDNA suggests somatic heterozygosity without substantial imbalance in allelic expression. Thus, mutant SETBP1 presumably has a dominant altered biological activity. Most mutations in SETBP1 are locat
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41

Kester, Monique H. A., George G. J. M. Kuiper, Rogier Versteeg, and Theo J. Visser. "Regulation of Type III Iodothyronine Deiodinase Expression in Human Cell Lines." Endocrinology 147, no. 12 (2006): 5845–54. http://dx.doi.org/10.1210/en.2006-0590.

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Type I iodothyronine deiodinase (D1) and type II iodothyronine deiodinase (D2) catalyze the activation of the prohormone T4 to the active hormone T3; type III iodothyronine deiodinase (D3) catalyzes the inactivation of T4 and T3. D3 is highly expressed in brain, placenta, pregnant uterus, and fetal tissues and plays an important role in regulating thyroid hormone bioavailability during fetal development. We examined the activity of the different deiodinases in human cell lines and investigated the regulation of D3 activity and mRNA expression in these cell lines, as well as its possible coexpr
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42

van den Akker, Guus G. H., Lars M. T. Eijssen, Stephen M. Richardson, et al. "A Membranome-Centered Approach Defines Novel Biomarkers for Cellular Subtypes in the Intervertebral Disc." CARTILAGE 11, no. 2 (2018): 203–20. http://dx.doi.org/10.1177/1947603518764260.

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Objective Lack of specific marker-sets prohibits definition and functional distinction of cellular subtypes in the intervertebral disc (IVD), such as those from the annulus fibrosus (AF) and the nucleus pulposus (NP). Design We recently generated immortalized cell lines from human NP and AF tissues; these comprise a set of functionally distinct clonal subtypes. Whole transcriptome analyses were performed of 12 phenotypically distinct clonal cell lines (4× NP-Responder, 4× NP-nonResponder, 2× AF-Sheet forming, and 2× AF-nonSheet forming). Data sets were filtered for membrane-associated marker g
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43

Gupta, Vikas A., Scott Newman, Nizar J. Bahlis, et al. "B-Cell Markers Predict Response to Venetoclax in Multiple Myeloma." Blood 128, no. 22 (2016): 2108. http://dx.doi.org/10.1182/blood.v128.22.2108.2108.

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Abstract BCL2 family members such as MCL1, BCLXL, and BCL2 are critical for cancer cell survival and therefore represent promising therapeutic targets. Both B cells and CLL cells depend primarily on BCL-2 and are thus sensitive to the BCL2 specific inhibitor venetoclax, while plasma cells and multiple myeloma typically depend on Mcl-1 and would therefore be resistant to venetoclax. However, a subset of myeloma is venetoclax sensitive based on recent in vitro and clinical trial data. In preliminary results from a phase I trial of venetoclax in multiple myeloma, 40% of patients positive for t(11
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44

Johnson, David, Carolyn Conant, Gary Withey, Andrea Löhr, Andro Hsu, and Everett Meyer. "Massively parallel phenotyping and clonotyping of single T cells (P3380)." Journal of Immunology 190, no. 1_Supplement (2013): 135.16. http://dx.doi.org/10.4049/jimmunol.190.supp.135.16.

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Abstract Flow cytometry captures T cell functionality but not individual T cell receptor clonal sequences. DNA sequencing characterizes the T cell clonotype repertoire, but lacks functional information. We report a method, T cell receptor-Effector Linkage Sequencing (TELS), which uses single-cell microfluidics and next-generation sequencing (NGS) to determine clonotype and phenotype for millions of T cells simultaneously. Single T cells are encapsulated in picoliter droplets. Overlap extension reverse transcriptase PCR amplifies T cell receptor beta (TCRb) and immune effector transcripts separ
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45

Rahbar, Kambiz, Mark S. Kidd, Ignat A. Drozdov, et al. "A blood-based multi-mRNA liquid biopsy with >90% accuracy for diagnosis and assessment of prostate cancers." Journal of Clinical Oncology 38, no. 15_suppl (2020): 5574. http://dx.doi.org/10.1200/jco.2020.38.15_suppl.5574.

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5574 Background: There are a paucity of blood-based biomarkers with clinical utility for prostate cancer (PCa). We developed a circulating mRNA (27-gene) prostate cancer signature to diagnose and manage PCa. Methods: Gene identification: Publicly available PCa transcriptome sets ( n= 1,159 samples) were evaluated and compared with normal blood-based transcriptomes using gene co-expression network enrichment, differential expression and functional enrichment analyses to identify candidate markers. Gene expression evaluation: Seven PCA cell lines and two normal prostate epithelial lines were use
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46

Stiefelhagen, Marius, Marlon R. Veldwijk, Anna Jauch, et al. "Generation and Application of a CML-Specific Recombinant Adeno-Associated Virus (rAAV) Vector." Blood 106, no. 11 (2005): 4417. http://dx.doi.org/10.1182/blood.v106.11.4417.4417.

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Abstract Introduction: Chronic myelogenous leukemia can be controlled but in most patients not be cured by tyrosine kinase inhibition. Direct targeting using gene therapy vectors combined with vaccination strategies may allow to eradicate residual leukemic progenitors. Adeno-associated virus (AAV) vectors are stable DNA vectors which were proven to be effective in the clinical gene therapy for e.g. coagulation disorders. The various AAV serotypes lack specificity for BCR-ABL+ leukemia cells. Recently developed AAV-library techniques allow a retargeting of vectors. We generated a set of rAAV ve
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47

Lahortiga, Idoya, Carlos Graux, Nicole Mentens, et al. "Array-CGH Analysis of T-ALL Patients and Cell Lines." Blood 108, no. 11 (2006): 4469. http://dx.doi.org/10.1182/blood.v108.11.4469.4469.

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Abstract Background Molecular analysis of T-cell acute lymphoblastic leukemia (T-ALL) has provided evidence that a stepwise alteration of at least four specific pathways is required during transformation of thymocytes to leukemic T-cells. Genetic alterations in hematopoietic precursor cells lead to loss of cell cycle control, impaired differentiation, proliferation and survival advantages, and unlimited self-renewal capacity. These defects include inactivation of CDKN2A (P16) present in 96 % of the patients, deregulated expression of transcription factors, and mutation of NOTCH1 in 56% of pati
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48

Yamada, Yohei, Naotoshi Yamaguchi, Masakazu Ozaki, Yukihiro Shinozaki, Mikako Saito, and Hideaki Matsuoka. "An Instant Cell Recognition System Using a Microfabricated Coordinate Standard Chip Useful for Combinable Cell Observation with Multiple Microscopic Apparatuses." Microscopy and Microanalysis 14, no. 3 (2008): 236–42. http://dx.doi.org/10.1017/s1431927608080252.

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AbstractDisposable coordinate standard (CS) chips were fabricated by the ejection of melted polystyrene into a metal mold. The CS chip surface was divided into four parts different in height and width. The edge lines of these parts could be recognized as straight lines 2 μm in width in the microscope view and used as the X and Y axes for the culture dish. The CS chip was attached on the bottom of a culture dish outside. Then the dish was set on the microscope stage and moved by means of a motorized automatic stage. The X-Y coordinates of many single-cells in a culture dish were registered, res
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Abdul Razzaq, Eman, Khuloud Bajbouj, Amal Bouzid, Noura Alkhayyal, Rifat Hamoudi, and Riyad Bendardaf. "Transcriptomic Changes Associated with ERBB2 Overexpression in Colorectal Cancer Implicate a Potential Role of the Wnt Signaling Pathway in Tumorigenesis." Cancers 15, no. 1 (2022): 130. http://dx.doi.org/10.3390/cancers15010130.

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Colorectal cancer (CRC) remains the third most common cause of cancer mortality worldwide. Precision medicine using OMICs guided by transcriptomic profiling has improved disease diagnosis and prognosis by identifying many CRC targets. One such target that has been actively pursued is an erbb2 receptor tyrosine kinase 2 (ERBB2) (Human Epidermal Growth Factor Receptor 2 (HER2)), which is overexpressed in around 3–5% of patients with CRC worldwide. Despite targeted therapies against HER2 showing significant improvement in disease outcomes in multiple clinical trials, to date, no HER2-based treatm
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50

Gautier, Emilie-Fleur, Muriel Picard, Camille Laurent, et al. "The cell cycle regulator CDC25A is a target for JAK2V617F oncogene." Blood 119, no. 5 (2012): 1190–99. http://dx.doi.org/10.1182/blood-2011-01-327742.

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Abstract The JAK2V617F mutation is present in the majority of patients with polycythemia vera and one-half of those with essential thrombocythemia and primary myelofibrosis. JAK2V617F is a gain-of-function mutation resulting in constitutive JAK2 signaling involved in the pathogenesis of these diseases. JAK2V617F has been shown to promote S-phase entry. Here, we demonstrate that the CDC25A phosphatase, a key regulator of the G1/S cell-cycle transition, is constitutively overexpressed in JAK2V617F-positive cell lines, JAK2-mutated patient CD36+ progenitors, and in vitro–differentiated proerythro
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