Inhibitory Concentration 50

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  Subject Areas on Research

  • A Computational Model of Inhibition of HIV-1 by Interferon-Alpha. 
  • A New, Second Generation Trithiol Bifunctional Chelate for 72,77As: Trithiol(b)-(Ser)2-RM2. 
  • Acquisition of a side population fraction augments malignant phenotype in ovarian cancer. 
  • Activation of the mTOR Pathway by Oxaliplatin in the Treatment of Colorectal Cancer Liver Metastasis. 
  • An unbiased evaluation of CK2 inhibitors by chemoproteomics: characterization of inhibitor effects on CK2 and identification of novel inhibitor targets. 
  • Androgen receptor antagonism drives cytochrome P450 17A1 inhibitor efficacy in prostate cancer. 
  • Anthrabenzoxocinones from Streptomyces sp. as liver X receptor ligands and antibacterial agents. 
  • Anti-AIDS agents 87. New bio-isosteric dicamphanoyl-dihydropyranochromone (DCP) and dicamphanoyl-khellactone (DCK) analogues with potent anti-HIV activity. 
  • Anti-AIDS agents. 42. Synthesis and anti-HIV activity of disubstituted (3'R,4'R)-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone analogues. 
  • Anti-AIDS agents. 78. Design, synthesis, metabolic stability assessment, and antiviral evaluation of novel betulinic acid derivatives as potent anti-human immunodeficiency virus (HIV) agents. 
  • Antibodies VRC01 and 10E8 neutralize HIV-1 with high breadth and potency even with Ig-framework regions substantially reverted to germline. 
  • Antiviral Effect of Retro-2.1 against Herpes Simplex Virus Type 2 In Vitro. 
  • Antiviral effects of Retro-2cycl and Retro-2.1 against Enterovirus 71 in vitro and in vivo. 
  • Artemisinin resistance in Plasmodium falciparum malaria. 
  • Betulinic acid derivatives as human immunodeficiency virus type 2 (HIV-2) inhibitors. 
  • Broad and potent HIV-1 neutralization by a human antibody that binds the gp41-gp120 interface. 
  • 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 Plasmodium liver stage inhibition by halofuginone. 
  • Cholesterol interaction with the daunorubicin binding site of P-glycoprotein. 
  • Conformation-assisted inhibition of protein-tyrosine phosphatase-1B elicits inhibitor selectivity over T-cell protein-tyrosine phosphatase. 
  • Conformational considerations in the design of dual antagonists of platelet-activating factor (PAF) and histamine. 
  • Constitutively activated STAT3 frequently coexpresses with epidermal growth factor receptor in high-grade gliomas and targeting STAT3 sensitizes them to Iressa and alkylators. 
  • Design and synthesis of naphthoquinone derivatives as antiproliferative agents and 20S proteasome inhibitors. 
  • Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding. 
  • Design, synthesis, and biologic evaluation of novel galloyl derivatives as HIV-1 RNase H inhibitors. 
  • Detection of Chemotherapy-resistant Pancreatic Cancer Using a Glycan Biomarker, sTRA. 
  • Differential effects of arsenic trioxide on chemosensitization in human hepatic tumor and stellate cell lines. 
  • Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R). 
  • Discovery of an inhibitor of insulin-like growth factor 1 receptor activation: implications for cellular potency and selectivity over insulin receptor. 
  • Discovery of thiophene inhibitors of polo-like kinase. 
  • Diterpenoid, steroid, and triterpenoid agonists of liver X receptors from diversified terrestrial plants and marine sources. 
  • Durhamycin A, a potent inhibitor of HIV Tat transactivation. 
  • Effects of the proteasome inhibitor PS-341 on apoptosis and angiogenesis in orthotopic human pancreatic tumor xenografts. 
  • Estimating the probability of polyreactive antibodies 4E10 and 2F5 disabling a gp41 trimer after T cell-HIV adhesion. 
  • Functional expression of an arachnid sodium channel reveals residues responsible for tetrodotoxin resistance in invertebrate sodium channels. 
  • Genomic and molecular profiling predicts response to temozolomide in melanoma. 
  • Guttiferone I, a new prenylated benzophenone from Garcinia humilis as a liver X receptor ligand. 
  • HIV-1 Neutralizing Antibody Signatures and Application to Epitope-Targeted Vaccine Design. 
  • Heterobiaryl human immunodeficiency virus entry inhibitors. 
  • High-throughput affinity ranking of antibodies using surface plasmon resonance microarrays. 
  • IGF1R as a Key Target in High Risk, Metastatic Medulloblastoma. 
  • Identification of a novel malonyl-CoA IC(50) for CPT-I: implications for predicting in vivo fatty acid oxidation rates. 
  • Identification of an ADAMTS-4 cleavage motif using phage display leads to the development of fluorogenic peptide substrates and reveals matrilin-3 as a novel substrate. 
  • Identification of the GPR55 antagonist binding site using a novel set of high-potency GPR55 selective ligands. 
  • Improving neutralization potency and breadth by combining broadly reactive HIV-1 antibodies targeting major neutralization epitopes. 
  • In vitro evaluation of dimethane sulfonate analogues with potential alkylating activity and selective renal cell carcinoma cytotoxicity. 
  • Induction of HIV Neutralizing Antibody Lineages in Mice with Diverse Precursor Repertoires. 
  • Inhibitory effect of b-AP15 on the 20S proteasome. 
  • Initial testing (stage 1) of BAL101553, a novel tubulin binding agent, 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 of the CENP-E inhibitor GSK923295A by the pediatric preclinical testing program. 
  • Isolation and structure of antagonists of chemokine receptor (CCR5). 
  • Isolation, structure and biological activities of platensimycin B4 from Streptomyces platensis. 
  • Isolation, structure, absolute stereochemistry, and HIV-1 integrase inhibitory activity of integrasone, a novel fungal polyketide. 
  • Isolation, structure, and HIV-1 integrase inhibitory activity of Cytosporic acid, a fungal metabolite produced by a Cytospora sp. 
  • Liver-stage malaria parasites vulnerable to diverse chemical scaffolds. 
  • Masitinib is a broad coronavirus 3CL inhibitor that blocks replication of SARS-CoV-2. 
  • Mechanism-Specific Pharmacodynamics of a Novel Complex-I Inhibitor Quantified by Imaging Reversal of Consumptive Hypoxia with [18F]FAZA PET In Vivo. 
  • N-(6-chloro-pyridin-3-yl)-3,4-difluoro-benzamide (ICA-27243): a novel, selective KCNQ2/Q3 potassium channel activator. 
  • Neutralization properties of simian immunodeficiency viruses infecting chimpanzees and gorillas. 
  • Neutralizing Activity of Broadly Neutralizing Anti-HIV-1 Antibodies against Clade B Clinical Isolates Produced in Peripheral Blood Mononuclear Cells. 
  • New Member of the V1V2-Directed CAP256-VRC26 Lineage That Shows Increased Breadth and Exceptional Potency. 
  • Non-peptidic, non-prenylic inhibitors of the prenyl protein-specific protease Rce1. 
  • Novel Synthetic Polyamines Have Potent Antimalarial Activities in vitro and in vivo by Decreasing Intracellular Spermidine and Spermine Concentrations. 
  • Novel light-driven functional AgNPs induce cancer death at extra low concentrations. 
  • O (4)-benzylfolic acid inactivates O (6)-alkylguanine-DNA alkyltransferase in brain tumor cell lines. 
  • Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series. 
  • Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors. 
  • Pharmacodynamic and genomic markers associated with response to the XPO1/CRM1 inhibitor selinexor (KPT-330): A report from the pediatric preclinical testing program. 
  • Phosphorus-based SAHA analogues as histone deacetylase inhibitors. 
  • Preclinical toxicity evaluation of a novel immunotoxin, D2C7-(scdsFv)-PE38KDEL, administered via intracerebral convection-enhanced delivery in rats. 
  • Preparation of antibodies and development of an enzyme immunoassay for determination of atrazine in environmental samples. 
  • Pyridazinones as selective cyclooxygenase-2 inhibitors. 
  • Pyrvinium selectively targets blast phase-chronic myeloid leukemia through inhibition of mitochondrial respiration. 
  • Quinocarmycin analog DX-52-1 inhibits cell migration and targets radixin, disrupting interactions of radixin with actin and CD44. 
  • Relative resistance of HIV-1 founder viruses to control by interferon-alpha. 
  • Role of YAP1 as a Marker of Sensitivity to Dual AKT and P70S6K Inhibition in Ovarian and Uterine Malignancies. 
  • Six-helix bundle assembly and characterization of heptad repeat regions from the F protein of Newcastle disease virus. 
  • Steroidal and triterpenoidal fungal metabolites as ligands of liver X receptors. 
  • Substrate specificities of g protein-coupled receptor kinase-2 and -3 at cardiac myocyte receptors provide basis for distinct roles in regulation of myocardial function. 
  • Synthesis and Biological Evaluation of Manassantin Analogues for Hypoxia-Inducible Factor 1α Inhibition. 
  • Synthesis and characterization of a thermally-responsive tumor necrosis factor antagonist. 
  • Synthesis of new 2'-deoxy-2'-fluoro-4'-azido nucleoside analogues as potent anti-HIV agents. 
  • Takinib, a Selective TAK1 Inhibitor, Broadens the Therapeutic Efficacy of TNF-α Inhibition for Cancer and Autoimmune Disease. 
  • Tenascin-C is an innate broad-spectrum, HIV-1-neutralizing protein in breast milk. 
  • The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor. 
  • The structural basis for the selectivity of benzotriazole inhibitors of PTP1B. 
  • Tumor cell sensitivity to vemurafenib can be predicted from protein expression in a BRAF-V600E basket trial setting. 
  • Virologic failure in therapy-naive subjects on aplaviroc plus lopinavir-ritonavir: detection of aplaviroc resistance requires clonal analysis of envelope. 
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  Keywords of People

  • Erickson, Harold Paul, James B. Duke Distinguished Professor Emeritus, Cell Biology