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drug-penetration

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Journal Articles
Cancer Res (2022) 82 (12_Supplement): 6302.
Published: 15 June 2022
... inhibition. There has been strong rationale for the use of PARP inhibitors in neuro-oncology. However, the first-generation PARP inhibitors have limited CNS distribution as these drugs were not designed for brain penetration. Recently AstraZeneca has reported the discovery of AZD5305, a next generation PARP1...
Journal Articles
Cancer Res (2022) 82 (12_Supplement): 5329.
Published: 15 June 2022
.... Treatment is hindered by the blood-brain barrier (BBB) that restricts entry of the vast majority of cancer therapeutics to the brain. We have designed a peptide-drug conjugate, (Pt(IV)-M13), comprised of M13, a perfluoroaryl-stapled cell-penetrating peptide, covalently linked to Pt(IV) via an amide bond...
Journal Articles
Cancer Res (2020) 80 (16_Supplement): 3041.
Published: 15 August 2020
... increases significantly. In combination with live cell imaging capabilities a powerful tool for dynamic studies of drug-cell interactions arises. In the current study we determined the penetration of anti-EGFR antibodies cetuximab and panitumumab in NSCLC spheroids in different culture conditions (w/wo...
Journal Articles
Cancer Res (2020) 80 (16_Supplement): 5493.
Published: 15 August 2020
... nanoparticles conjugated with cancer cell specific antibodies (trastuzumab) to improve drug delivery to the tumor, while sparing healthy tissues. These antibody nano-conjugates (ANCs) consist in docetaxel-encapsulated liposomes engrafted with trastuzumab on the surface. Intra-tumor penetration properties...
Journal Articles
Cancer Res (2022) 82 (22): 4191–4205.
Published: 15 November 2022
... , Liang XH . Antisense technology: an overview and prospectus . Nat Rev Drug Discov 2021 ; 20 : 427 – 53 . 44. Chen X , Ying Z , Lin X , Lin H , Wu J , Li M , . Acylglycerol kinase augments JAK2/STAT3 signaling in esophageal squamous cells . J...
Includes: Supplementary data
Journal Articles
Cancer Res (2022) 82 (22): 4114–4123.
Published: 15 November 2022
.... Jang H. Massive efforts have focused on searches, identification, and analyses of activating mutations, particularly those involved in cancer initiation and drug resistance, and multiple reviews have described them ( 1–10 ). Some are broad range; some involve specific cancers. Some focus...
Images
Pharmacologic blockade of SQLE attenuates CRPC growth <em>in vitro</em>...
Published: 02 September 2022
Figure 6. Pharmacologic blockade of SQLE attenuates CRPC growth in vitro and in vivo. A and B, Cell growth curve ( A ) and colony formation ( B ) of PC3 cells were assessed after treatment with increasing doses of FR194738 for the indicated times. C, Representative images of vehicle- or FR194738- treated PC3 xenografts 6 weeks after drug administration (n  =  6 mice per group). D, Tumor weight of vehicle- or FR194738-treated mice at 6 weeks after the starting dose of drug administration. E, Waterfall plot of the response of PC3 xenografts at 6 weeks after the starting dose of drug administration. F, Representative images of immunohistochemistry for Ki67 and cleaved caspase-3 staining in xenografts. Scale bars, 200 μm. Quantification of positive signals is provided on the right of the representative images. G, Relative cholesterol levels of PC3 xenografts after 6 weeks of treatment with vehicle or FR194738. H, Study design of the Ptenpc−/−; Trp53pc−/− murine model used. I, Representative image of vehicle- or FR194738-treated Ptenpc−/−; Trp53pc−/− mouse prostate tumors at 6 weeks after the starting dose of drug administration (n  =  6 mice per group). J, Tumor weight of vehicle- or FR194738-treated PtenPC−/−; Trp53PC−/− mice at 6 weeks after the starting dose of drug administration. K, Histologic analysis (hematoxylin and eosin staining) of a representative metastatic lymph node from Ptenpc−/−; Trp53pc−/− mice. Scale bars, 200 μm. L, Quantifications of the penetrance of metastasis in vehicle- or FR194738-treated Ptenpc−/−; Trp53PC−/− mice at 6 weeks after the starting dose of drug administration. M, Representative images of IHC for Ki67 and cleaved caspase-3 staining in the tumor tissue of vehicle- or FR194738-treated PtenPC−/−; Trp53PC−/− mice at 6 weeks after the starting dose of drug administration. Scale bars, 200 μm. Quantification of positive signals is provided on the right of the representative images. N, Relative cholesterol levels in the tumor tissue of vehicle- or FR194738-treated Ptenpc−/−; Trp53pc−/− mice at 6 weeks after the starting dose of drug administration. O, Kaplan-Meier survival plots of vehicle- or FR194738-treated Ptenpc−/−; Trp53pc−/− mice (Vehicle = 8; FR194738 = 7). P, Schematic diagram delineating the mechanism by which SQLE exerts its oncogenic function in PTEN/p53-deficient CRPC. One-way ANOVA ( A ).Two-tailed Student t test ( B , D , E , F , G , J , M , and N ). Log-rank test ( O ). Error bars, ± SD. **, P < 0.01; ***, P < 0.001. Figure 6. Pharmacologic blockade of SQLE attenuates CRPC growth in vitro and in vivo. A, Cell growth curve and (B) colony formation of PC3 cells were assessed after treatment with increasing doses of FR194738 for the indicated times. C, Representative images of vehicle- or FR194738- treated PC3 xenografts 6 weeks after drug administration (n  =  6 mice per group). D, Tumor weight of vehicle- or FR194738-treated mice at 6 weeks after the starting dose of drug administration. E, Waterfall plot of the response of PC3 xenografts at 6 weeks after the starting dose of drug administration. F, Representative images of immunohistochemistry for Ki67 and cleaved caspase 3 staining in xenografts. Scale bars, 200 μmol/L. Quantification of positive signals is provided on the right of the representative images. G, Relative cholesterol levels of PC3 xenografts after 6 weeks of treatment with vehicle or FR194738. H, Study design of the Ptenpc–/–; Trp53pc–/– murine model used. I, Representative image of vehicle- or FR194738-treated Ptenpc–/–; Trp53pc–/– mouse prostate tumors at 6 weeks after the starting dose of drug administration (n  =  6 mice per group). J, Tumor weight of vehicle- or FR194738- treated PtenPC–/–; Trp53PC–/– mice at 6 weeks after the starting dose of drug administration. K, Histologic analysis (H&E staining) of a representative metastatic lymph node from Ptenpc–/–; Trp53pc–/– mice. Scale bars, 200 μmol/L. L, Quantifications of the penetrance of metastasis in vehicle- or FR194738- treated Ptenpc–/–; Trp53PC–/– mice at 6 weeks after the starting dose of drug administration. M, Representative images of IHC for Ki67 and cleaved caspase 3 staining in the tumor tissue of vehicle- or FR194738- treated PtenPC–/–; Trp53PC–/– mice at 6 weeks after the starting dose of drug administration. Scale bars, 200 μmol/L. Quantification of positive signals is provided on the right of the representative images. N, Relative Cholesterol levels in the tumor tissue of vehicle- or FR194738- treated Ptenpc–/–; Trp53pc–/– mice at 6 weeks after the starting dose of drug administration. O, Kaplan-Meier survival plots of vehicle- or FR194738- treated Ptenpc–/–; Trp53pc–/– mice (Vehicle = 8; FR194738 = 7). P, Schematic diagram delineating the mechanism by which SQLE exerts its oncogenic function in PTEN/p53-deficient CRPC. One-way ANOVA (A).Two-tailed Student t test (B, D, E, F, G, J, M, N). Log-rank test (O). Error bars represent ± SD (**, P < 0.01; ***, P < 0.001). More
Journal Articles
Cancer Res (2022) 82 (12_Supplement): 385.
Published: 15 June 2022
... for their abundant desmoplastic stroma that acts as a barrier for drug penetration and reduces treatment efficacy. iRGD is a tumor-penetrating peptide that initially targets αv integrins expressed on tumor vasculature with its RGD motif and then is proteolytically processed to expose a CendR motif (R/KXXR/K...
Journal Articles
Cancer Res (2022) 82 (22): 4261–4273.
Published: 15 November 2022
..., although responses to vertical inhibition of BRAFV600E signaling often elicit striking responses, many patients develop lethal drug-resistant disease, emphasizing the need for improved therapeutic approaches for these diseases. We have previously described genetically engineered mice...
Includes: Supplementary data
Journal Articles
Cancer Res CAN-22-1433.
Published: 09 November 2022
... neuroendocrine (NE) carcinomas, but not in most normal adult tissues, making it an attractive NE carcinoma surface protein target. Prior efforts to target DLL3 in NE carcinomas have been disappointing. The first-in-class antibody-drug conjugate (ADC), Rovalpituzumab tesirine (Rova-T), targeted DLL3 to deliver...
Includes: Multimedia, Supplementary data
Journal Articles
Cancer Res (2022) 82 (20): 3650–3658.
Published: 17 October 2022
... be beneficial in this setting. For tumors where drug penetration is a concern, studies combining standard therapies with TTFields should be considered given its effects on the blood brain barrier and cell membrane permeability. It is well known that intratumoral immune responses may spread to nontreated tumors...
Includes: Supplementary data
Journal Articles
Cancer Res CAN-22-0391.
Published: 08 November 2022
... authors declare no potential conflicts of interest. 2 Significance CRISPR-Cas9 screening and protein activity mapping reveal combinations that increase potency of CDK4/6 inhibitors and overcome drug-induced compensations in pancreatic cancer. 3 Abstract Mutational loss of CDKN2A (encoding p16INK4A) tumor...
Includes: Supplementary data
Journal Articles
Cancer Res (2022) 82 (12_Supplement): 10.
Published: 15 June 2022
... and suitable tool for drug penetration studies. Conclusion: Together, our results suggest that single cell-derived clonal spheroid from different wells would represent the genetic and functional heterogeneity of the cell population. Such a spheroid model can reveal heterogeneity inside a tumor formed...
Journal Articles
Cancer Res (2022) 82 (21): 4016–4030.
Published: 02 November 2022
... on FAO for tumor growth, metastasis, and drug resistance ( 5 ). CYP4A and 4F ω-hydroxylases comprise a critical metabolic node that initiates the formation of mono- and dicarboxylic acids, which are then catabolized through the β-oxidation pathway ( 6 ). CYP4 ω-hydroxylases show preferences...
Includes: Supplementary data
Journal Articles
Cancer Res CAN-22-0787.
Published: 12 October 2022
...; Fred A. Dijcks; Wim H.A. Dokter; Javier Cortés; Cristina Saura; Joaquín Arribas Antibody-drug conjugates (ADC) are anti-neoplastic agents recently introduced into the anti-tumor arsenal. T-DM1, a trastuzumab-based ADC that relies on lysosomal processing to release the payload, is approved for HER2...
Includes: Supplementary data
Journal Articles
Cancer Res (2022) 82 (20): 3830–3844.
Published: 17 October 2022
... utility in reducing breast cancer progression and drug resistance. PELP1 ( 10 ), serves as an ER coregulator and plays a critical role in breast cancer progression ( 11, 12 ). PELP1 expression is upregulated in breast cancer ( 13 ), its status is a prognostic indicator of poor breast cancer survival...
Includes: Supplementary data
Journal Articles
Cancer Res CAN-22-0736.
Published: 12 October 2022
... cancer, checkpoint 106 inhibitors show the greatest benefits in triple-negative subtype, whereas other subtypes, especially the luminal, 107 hormone receptor-positive one, are innately insensitive to these immunotherapy drugs (13). Thus, it is clinically 108 urgent to better understand the basis...
Includes: Supplementary data
Journal Articles
Journal Articles
Cancer Res (2022) 82 (18): 3359–3374.
Published: 16 September 2022
... oncolytic virus (OV) therapy has been proposed as a potential approach to treat GBM, it frequently fails because GBM cells are usually nonpermissive to OV. Here, we describe a dual-step drug screen for identifying chemical enhancers of OV in GBM. From a high-throughput screen of 1416 FDA-approved drugs...
Includes: Supplementary data
Journal Articles
Cancer Res (2022) 82 (19): 3499–3515.
Published: 04 October 2022
... manufacturer's instructions, using a 1:2.5 or 1:2 ratio of DNA: Lipofectamine. Cells were treated with the appropriate drugs 24 hours posttransfection. To assess mitotic checkpoint function, transfected cells, fibroblasts, and MEFs were synchronized with 0.61 mg/mL thymidine (Sigma) for 22 to 24 hours, released...
Includes: Supplementary data