Drug Screening Assays, Antitumor

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  Subject Areas on Research

  • A Metabolomics Pilot Study on Desmoid Tumors and Novel Drug Candidates. 
  • A Precision Medicine Drug Discovery Pipeline Identifies Combined CDK2 and 9 Inhibition as a Novel Therapeutic Strategy in Colorectal Cancer. 
  • A Rational Approach to Target the Epidermal Growth Factor Receptor in Glioblastoma. 
  • A manganese porphyrin superoxide dismutase mimetic enhances tumor radioresponsiveness. 
  • A novel low-molecular weight inhibitor of focal adhesion kinase, TAE226, inhibits glioma growth. 
  • A small molecule inhibitor of isoprenylcysteine carboxymethyltransferase induces autophagic cell death in PC3 prostate cancer cells. 
  • Activity of 9-dimethylaminomethyl-10-hydroxycamptothecin against pediatric and adult central nervous system tumor xenografts. 
  • Activity of psoralen-functionalized nanoscintillators against cancer cells upon X-ray excitation. 
  • Adjuvant chemotherapy for colorectal hepatic metastases: role of route of administration and timing. 
  • Akt/protein kinase B is constitutively active in non-small cell lung cancer cells and promotes cellular survival and resistance to chemotherapy and radiation. 
  • Amino derivatives of indole as potent inhibitors of isoprenylcysteine carboxyl methyltransferase. 
  • Amphetamine decorated cationic lipid nanoparticles cross the blood-brain barrier: therapeutic promise for combating glioblastoma. 
  • An efficient multiple-exposure analysis of the toxicity of crisnatol, a DNA intercalator in phase II clinical trials. 
  • An integrated approach to the prediction of chemotherapeutic response in patients with breast cancer. 
  • Anti proliferative activity of ELACY (CP-4055) in combination with cloretazine (VNP40101M), idarubicin, gemcitabine, irinotecan and topotecan in human leukemia and lymphoma cells. 
  • Anti-HIV Agents 45 and Antitumor Agents 205. Two New Sesquiterpenes, Leitneridanins A and B, and the Cytotoxic and Anti-HIV Principles from Leitneria floridana 
  • Antibiotic and antimalarial quinones from fungus-growing ant-associated Pseudonocardia sp. 
  • Antibody-directed coupling of endoglin and MMP-14 is a key mechanism for endoglin shedding and deregulation of TGF-β signaling. 
  • Antineoplastic activity of boron-containing thymidine nucleosides in Tmolt3 leukemic cells. 
  • Antineoplastic drug screening. 
  • Antitumor Agents, 138. Potenoids and Isoflavones as Cytotoxic Constituents of Amorpha fructicosa 
  • Antitumor Agents. 152. In Vitro Inhibitory Activity of Etoposide Derivative NPF Against Human Tumor Cell Lines and a Study of its Conformation by X-Ray Crystallography, Molecular Modeling, and NMR Spectroscopy 
  • Antitumor Agents. 154. Cytotoxic and Antimitotic Flavonols from Polanisia dodecandra 
  • Antitumor agents, 135. Structure and stereochemistry of polacandrin, a new cytotoxic triterpene from Polanisia dodecandra. 
  • Antitumor agents. Part 215: antitubulin effects of cytotoxic B-ring modified allocolchicinoids. 
  • Aptamer-mediated delivery of chemotherapy to pancreatic cancer cells. 
  • Cancer immunotherapy innovator James Allison receives the 2015 Lasker~DeBakey Clinical Medical Research Award. 
  • Carbamate derivatives of colchicine show potent activity towards primary acute lymphoblastic leukemia and primary breast cancer cells-in vitro and ex vivo study. 
  • Characterization of a new model of human prostatic cancer: the multicellular tumor spheroid. 
  • Chemotaxis-driven assembly of endothelial barrier in a tumor-on-a-chip platform. 
  • Circulating tumor cell-derived organoids: Current challenges and promises in medical research and precision medicine. 
  • Combining gemcitabine with radiation in pancreatic cancer: understanding important variables influencing the therapeutic index. 
  • Cytotoxic, antifouling bromotyramines: a synthetic study on simple marine natural products and Their analogues. 
  • Cytotoxicity of alpha-particle-emitting m-[211At]astatobenzylguanidine on human neuroblastoma cells. 
  • Dasatinib (BMS-35482) interacts synergistically with docetaxel, gemcitabine, topotecan, and doxorubicin in ovarian cancer cells with high SRC pathway activation and protein expression. 
  • Design and synthesis of naphthoquinone derivatives as antiproliferative agents and 20S proteasome inhibitors. 
  • Development of a cell-based, high-throughput screening assay for ATM kinase inhibitors. 
  • Development of a precision medicine pipeline to identify personalized treatments for colorectal cancer. 
  • Discovery and characterization of small molecules that target the GTPase Ral. 
  • Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ERαWT and ERαMUT Breast Cancer. 
  • Discovery of [(3-bromo-7-cyano-2-naphthyl)(difluoro)methyl]phosphonic acid, a potent and orally active small molecule PTP1B inhibitor. 
  • Discovery of a Potent GLUT Inhibitor from a Library of Rapafucins by Using 3D Microarrays. 
  • Dissecting the roles of DR4, DR5 and c-FLIP in the regulation of geranylgeranyltransferase I inhibition-mediated augmentation of TRAIL-induced apoptosis. 
  • Distinguishing effects on tumor multiplicity and growth rate in chemoprevention experiments. 
  • Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents. 
  • Dual-targeted hybrid nanoparticles of synergistic drugs for treating lung metastases of triple negative breast cancer in mice. 
  • Effect of flaxseed supplementation on prostatic carcinoma in transgenic mice. 
  • Efficacy of compartmental administration of immunotoxin LMB-1 (B3-LysPE38) in a rat model of carcinomatous meningitis. 
  • Elevated DNA polymerase alpha, DNA polymerase beta, and DNA topoisomerase II in a melphalan-resistant rhabdomyosarcoma xenograft that is cross-resistant to nitrosoureas and topotecan. 
  • Enforced expression of wild-type p53 curtails the transcription of the O(6)-methylguanine-DNA methyltransferase gene in human tumor cells and enhances their sensitivity to alkylating agents. 
  • Epidermal growth factor receptor-targeted therapy for pancreatic cancer. 
  • Everolimus in colorectal cancer. 
  • Ex vivo expanded human Vgamma9Vdelta2+ gammadelta-T cells mediate innate antitumor activity against human prostate cancer cells in vitro. 
  • Flavopiridol induces apoptosis in chronic lymphocytic leukemia cells via activation of caspase-3 without evidence of bcl-2 modulation or dependence on functional p53. 
  • Gene expression signatures as a guide to treatment strategies for in-transit metastatic melanoma. 
  • Genomic and molecular profiling predicts response to temozolomide in melanoma. 
  • Gossypol and an HMT G9a inhibitor act in synergy to induce cell death in pancreatic cancer cells. 
  • Growth inhibitory effects of aromatic fatty acids on ovarian tumor cell lines. 
  • IGF1R as a Key Target in High Risk, Metastatic Medulloblastoma. 
  • Identification of highly potent and selective Cdc25 protein phosphatases inhibitors from miniaturization click-chemistry-based combinatorial libraries. 
  • Identification of repurposed small molecule drugs for chordoma therapy. 
  • Imidazo[5,1-f][1,2,4]triazin-2-amines as novel inhibitors of polo-like kinase 1. 
  • Importance of the stress kinase p38alpha in mediating the direct cytotoxic effects of the thalidomide analogue, CPS49, in cancer cells and endothelial cells. 
  • In vitro sensitivity testing of minimally passaged and uncultured gliomas with TRAIL and/or chemotherapy drugs. 
  • Inhibiting androgen receptor nuclear entry in castration-resistant prostate cancer. 
  • Inhibition of prostate cancer cell growth by second-site androgen receptor antagonists. 
  • Inhibition of the growth of human melanoma metastases in nude mice by melanoma-specific murine monoclonal antibody. 
  • Inhibition of vascular endothelial growth factor in the treatment of colorectal cancer. 
  • Initial testing (Stage 1) of the antibody-maytansinoid conjugate, IMGN901 (Lorvotuzumab mertansine), by the pediatric preclinical testing program. 
  • Initial testing (stage 1) of AZD6244 (ARRY-142886) by the Pediatric Preclinical Testing Program. 
  • Initial testing (stage 1) of SGI-1776, a PIM1 kinase inhibitor, by the pediatric preclinical testing program. 
  • Initial testing (stage 1) of ganetespib, an Hsp90 inhibitor, by the Pediatric Preclinical Testing Program. 
  • Initial testing (stage 1) of lapatinib by the pediatric preclinical testing program. 
  • Initial testing (stage 1) of sunitinib by the pediatric preclinical testing program. 
  • Initial testing (stage 1) of temozolomide by the pediatric preclinical testing program. 
  • Initial testing (stage 1) of the Polo-like kinase inhibitor volasertib (BI 6727), by the Pediatric Preclinical Testing Program. 
  • Initial testing (stage 1) of the phosphatidylinositol 3' kinase inhibitor, SAR245408 (XL147) by the pediatric preclinical testing program. 
  • Initial testing of a monoclonal antibody (IMC-A12) against IGF-1R by the Pediatric Preclinical Testing Program. 
  • Initial testing of cisplatin by the pediatric preclinical testing program. 
  • Initial testing of the hypoxia-activated prodrug PR-104 by the pediatric preclinical testing program. 
  • Integrative gene expression profiling reveals G6PD-mediated resistance to RNA-directed nucleoside analogues in B-cell neoplasms. 
  • Integrin-Targeting Knottin Peptide-Drug Conjugates Are Potent Inhibitors of Tumor Cell Proliferation. 
  • Intraarterial administration of melphalan for treatment of intracranial human glioma xenografts in athymic rats. 
  • Intrathecal melphalan therapy of human neoplastic meningitis in athymic nude rats. 
  • Kleinhospitine E and Cycloartane Triterpenoids from Kleinhovia hospita. 
  • Lack of evidence for a polymorphism at codon 160 of human O6-alkylguanine-DNA alkyltransferase gene in normal tissue and cancer. 
  • Meta-iodobenzylguanidine derivatives containing a second guanidine moiety. 
  • Nanoparticle Encapsulation of Synergistic Immune Agonists Enables Systemic Codelivery to Tumor Sites and IFNβ-Driven Antitumor Immunity. 
  • Nanoparticle delivery of chemosensitizers improve chemotherapy efficacy without incurring additional toxicity. 
  • New use of an old drug: inhibition of breast cancer stem cells by benztropine mesylate. 
  • Novel amphiphilic cationic porphyrin and its Ag(II) complex as potential anticancer agents. 
  • O (4)-benzylfolic acid inactivates O (6)-alkylguanine-DNA alkyltransferase in brain tumor cell lines. 
  • Organoid Profiling Identifies Common Responders to Chemotherapy in Pancreatic Cancer. 
  • Pharmacogenomic strategies provide a rational approach to the treatment of cisplatin-resistant patients with advanced cancer. 
  • Plant antitumor agents. 31. The calycopterones, a new class of biflavonoids with novel cytotoxicity in a diverse panel of human tumor cell lines. 
  • Pre-clinical evaluation of SN-38 and novel camptothecin analogs against human chronic B-cell lymphocytic leukemia lymphocytes. 
  • RRR-alpha-vitamin E succinate potentiates the antitumor effect of calcitriol in prostate cancer without overt side effects. 
  • Radiotoxicity of systemically administered 211At-labeled human/mouse chimeric monoclonal antibody: a long-term survival study with histologic analysis. 
  • Rational Design of Selective Allosteric Inhibitors of PHGDH and Serine Synthesis with Anti-tumor Activity. 
  • Safety of concomitant use of granulocyte colony-stimulating factor or granulocyte-macrophage colony-stimulating factor with cytotoxic chemotherapy agents. 
  • Semiparametric Bayes multiple testing: Applications to tumor data. 
  • Stage 1 testing and pharmacodynamic evaluation of the HSP90 inhibitor alvespimycin (17-DMAG, KOS-1022) by the pediatric preclinical testing program. 
  • Statin expression in the untreated and SarCNU-exposed human glioma cell line, SK-MG-1. 
  • Suppression of Rev3, the catalytic subunit of Pol{zeta}, sensitizes drug-resistant lung tumors to chemotherapy. 
  • Sustained in vivo regression of Dunning H rat prostate cancers treated with combinations of androgen ablation and Trk tyrosine kinase inhibitors, CEP-751 (KT-6587) or CEP-701 (KT-5555). 
  • Synergistic cytotoxicity using 2'-deoxy-5-azacytidine and cisplatin or 4-hydroperoxycyclophosphamide with human tumor cells. 
  • Synergistic cytotoxicity with 2'-deoxy-5-azacytidine and topotecan in vitro and in vivo. 
  • Synergistic effects of multiple natural products in pancreatic cancer cells. 
  • Synthesis and Anticancer Activity of Tertiary Amides of Salinomycin and Their C20-oxo Analogues. 
  • Synthesis and Cytotoxicity of Acetyl-4H,9H-naphtho[2,3-b]thiophene-4,9-diones 
  • Synthesis and biological evaluation of novel spin labeled 18β-glycyrrhetinic acid derivatives. 
  • Synthetic lethal interaction of combined BCL-XL and MEK inhibition promotes tumor regressions in KRAS mutant cancer models. 
  • TGF-β-induced stromal CYR61 promotes resistance to gemcitabine in pancreatic ductal adenocarcinoma through downregulation of the nucleoside transporters hENT1 and hCNT3. 
  • Targeting wide-range oncogenic transformation via PU24FCl, a specific inhibitor of tumor Hsp90. 
  • The Crystal Structure and Cytotoxicity of Goniodiol Monoacetate from Goniothalamus Amyon 
  • The arginase inhibitor Nω-hydroxy-nor-arginine (nor-NOHA) induces apoptosis in leukemic cells specifically under hypoxic conditions but CRISPR/Cas9 excludes arginase 2 (ARG2) as the functional target. 
  • The p16 status of tumor cell lines identifies small molecule inhibitors specific for cyclin-dependent kinase 4. 
  • The role of NAD(P)H:quinone oxidoreductase in mitomycin C- and porfiromycin-resistant HCT 116 human colon-cancer cells. 
  • The synthetic phosphagen cyclocreatine phosphate inhibits the growth of a broad spectrum of solid tumors. 
  • Therapeutic analysis of melphalan-resistant human rhabdomyosarcoma xenograft TE-671 MR. 
  • Therapeutic efficacy of the topoisomerase I inhibitor 7-ethyl-10-(4-[1-piperidino]-1-piperidino)-carbonyloxy-camptothecin against pediatric and adult central nervous system tumor xenografts. 
  • Transforming growth factor alpha expression drives constitutive epidermal growth factor receptor pathway activation and sensitivity to gefitinib (Iressa) in human pancreatic cancer cell lines. 
  • Treatment of central nervous system xenografts with camptothecins. 
  • Treatment of neoplastic meningitis with intrathecal temozolomide. 
  • Tumor Subtype Determines Therapeutic Response to Chimeric Polypeptide Nanoparticle-based Chemotherapy in Pten-deleted Mouse Models of Sarcoma. 
  • Tumor prevention by 9-cis-retinoic acid in the N-nitroso-N-methylurea model of mammary carcinogenesis is potentiated by the pineal hormone melatonin. 
  • Understanding the mechanisms of action of antiangiogenic agents in metastatic colorectal cancer: a clinician's perspective. 
  • X-ray crystal structure of acrovestone, a cytotoxic principle from Acronychia pedunculata. 
  • cis-parthenolid-9-one from Anvillea garcinii. 
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  Keywords of People

  • McDonnell, Donald Patrick, Glaxo-Wellcome Distinguished Professor of Molecular Cancer Biology, in the School of Medicine, Cell Biology
  • Sampson, John Howard, Robert H., M.D. and Gloria Wilkins Professor of Neurosurgery, in the School of Medicine, Biomedical Engineering