64 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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A nonpromoting phorbol from the samoan medicinal plant Homalanthus nutans inhibits cell killing by HIV-1.
National Cancer Institute-Frederick
Application of oxime-diversification to optimize ligand interactions within a cryptic pocket of the polo-like kinase 1 polo-box domain.
National Cancer Institute-Frederick
Screening and Biological Effects of Marine Pyrroloiminoquinone Alkaloids: Potential Inhibitors of the HIF-1a/p300 Interaction.
National Cancer Institute-Frederick
Synthetic derivatives of the SUMO consensus sequence provide a basis for improved substrate recognition.
National Cancer Institute-Frederick
Nitric oxide (NO) releasing poly ADP-ribose polymerase 1 (PARP-1) inhibitors targeted to glutathione S-transferase P1-overexpressing cancer cells.
National Cancer Institute-Frederick
Synthesis and structure-activity relationship studies of novel dihydropyridones as androgen receptor modulators.
National Cancer Institute-Frederick
Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges.
National Cancer Institute-Frederick
Inhibitors of human tyrosyl-DNA phospodiesterase (hTdp1) developed by virtual screening using ligand-based pharmacophores.
National Cancer Institute-Frederick
Quassinoid inhibition of AP-1 function does not correlate with cytotoxicity or protein synthesis inhibition.
National Cancer Institute-Frederick
Conformationally constrained analogues of diacylglycerol (DAG). 27. Modulation of membrane translocation of protein kinase C (PKC) isozymes alpha and delta by diacylglycerol lactones (DAG-lactones) containing rigid-rod acyl groups.
National Cancer Institute-Frederick
Conformationally constrained analogues of diacylglycerol (DAG). 23. Hydrophobic ligand-protein interactions versus ligand-lipid interactions of DAG-lactones with protein kinase C (PK-C).
National Cancer Institute-Frederick
Synthesis and biological evaluation of 5-substituted derivatives of the potent antiherpes agent (north)-methanocarbathymine.
National Cancer Institute-Frederick
Conformationally constrained analogues of diacylglycerol. 20. The search for an elusive binding site on protein kinase C through relocation of the carbonyl pharmacophore along the sn-1 side chain of 1,2-diacylglycerol lactones.
National Cancer Institute-Frederick
A conformationally locked analogue of the anti-HIV agent stavudine. An important correlation between pseudorotation and maximum amplitude.
National Cancer Institute-Frederick
Conformationally constrained analogues of diacylglycerol. 19. Synthesis and protein kinase C binding affinity of diacylglycerol lactones bearing an N-hydroxylamide side chain.
National Cancer Institute-Frederick
An optimized protein kinase C activating diacylglycerol combining high binding affinity (Ki) with reduced lipophilicity (log P).
National Cancer Institute-Frederick
Peptide-linked 1,3-dialkyl-3-acyltriazenes: gastrin receptor directed antineoplastic alkylating agents.
National Cancer Institute-Frederick
Grassypeptolides F and G, cyanobacterial peptides from Lyngbya majuscula.
National Cancer Institute-Frederick
Cryptocaryols A-H,a-pyrone-containing 1,3-polyols from Cryptocarya sp. implicated in stabilizing the tumor suppressor Pdcd4.
National Cancer Institute-Frederick
Utilization of nitrophenylphosphates and oxime-based ligation for the development of nanomolar affinity inhibitors of the Yersinia pestis outer protein H (YopH) phosphatase.
National Cancer Institute-Frederick
Inhibitors of the oncogenic transcription factor AP-1 from Podocarpus latifolius.
National Cancer Institute-Frederick
Flavonoids from eight tropical plant species that inhibit the multidrug resistance transporter ABCG2.
National Cancer Institute-Frederick
Structure-activity analysis of vinylogous urea inhibitors of human immunodeficiency virus-encoded ribonuclease H.
National Cancer Institute-Frederick
A rapid oxime linker-based library approach to identification of bivalent inhibitors of the Yersinia pestis protein-tyrosine phosphatase, YopH.
National Cancer Institute-Frederick
Application of ring-closing metathesis macrocyclization to the development of Tsg101-binding antagonists.
National Cancer Institute-Frederick
Directed discovery of agents targeting the Met tyrosine kinase domain by virtual screening.
National Cancer Institute-Frederick
Conformationally constrained analogues of diacylglycerol (DAG). 31. Modulation of the biological properties of diacylgycerol lactones (DAG-lactones) containing rigid-rod acyl groups separated from the core lactone by spacer units of different lengths.
National Cancer Institute-Frederick
Identification of Shc Src homology 2 domain-binding peptoid-peptide hybrids.
National Cancer Institute-Frederick
Discovery of new pyridoacridine alkaloids from Lissoclinum cf. badium that inhibit the ubiquitin ligase activity of Hdm2 and stabilize p53.
National Cancer Institute-Frederick
Conformationally constrained analogues of diacylglycerol. 30. An investigation of diacylglycerol-lactones containing heteroaryl groups reveals compounds with high selectivity for Ras guanyl nucleotide-releasing proteins.
National Cancer Institute-Frederick
Conformationally constrained analogues of diacylglycerol. 29. Cells sort diacylglycerol-lactone chemical zip codes to produce diverse and selective biological activities.
National Cancer Institute-Frederick
Natural products as leads to potential drugs: an old process or the new hope for drug discovery?
National Cancer Institute-Frederick
Inhibition of metalloprotease botulinum serotype A from a pseudo-peptide binding mode to a small molecule that is active in primary neurons.
National Cancer Institute-Frederick
Conformationally constrained analogues of diacylglycerol (DAG). 28. DAG-dioxolanones reveal a new additional interaction site in the C1b domain of PKC delta.
National Cancer Institute-Frederick
Examination of acylated 4-aminopiperidine-4-carboxylic acid residues in the phosphotyrosyl+1 position of Grb2 SH2 domain-binding tripeptides.
National Cancer Institute-Frederick
Conformationally constrained analogues of diacylglycerol. 26. Exploring the chemical space surrounding the C1 domain of protein kinase C with DAG-lactones containing aryl groups at the sn-1 and sn-2 positions.
National Cancer Institute-Frederick
Conformationally constrained analogues of diacylglycerol (DAG). 25. Exploration of the sn-1 and sn-2 carbonyl functionality reveals the essential role of the sn-1 carbonyl at the lipid interface in the binding of DAG-lactones to protein kinase C.
National Cancer Institute-Frederick
Design and synthesis of 4-(alpha-hydroxymalonyl)phenylalanine as a new phosphotyrosyl mimetic and its use in growth factor receptor bound 2 src-homology 2 (Grb2 SH2) domain-binding peptides.
National Cancer Institute-Frederick
Examination of phosphoryl-mimicking functionalities within a macrocyclic Grb2 SH2 domain-binding platform.
National Cancer Institute-Frederick
Design and synthesis of conformationally constrained Grb2 SH2 domain binding peptides employing alpha-methylphenylalanyl based phosphotyrosyl mimetics.
National Cancer Institute-Frederick
Synthesis and HIV-1 integrase inhibitory activity of dimeric and tetrameric analogs of indolicidin.
National Cancer Institute-Frederick
Macrocyclization in the design of non-phosphorus-containing Grb2 SH2 domain-binding ligands.
National Cancer Institute-Frederick
Synthesis of a 5-methylindolyl-containing macrocycle that displays ultrapotent Grb2 SH2 domain-binding affinity.
National Cancer Institute-Frederick
Tripeptide inhibitors of Yersinia protein-tyrosine phosphatase.
National Cancer Institute-Frederick
Utilization of a beta-aminophosphotyrosyl mimetic in the design and synthesis of macrocyclic Grb2 SH2 domain-binding peptides.
National Cancer Institute-Frederick
Potent Grb2-SH2 domain antagonists not relying on phosphotyrosine mimics.
National Cancer Institute-Frederick
Molecular modeling calculations of HIV-1 reverse transcriptase nonnucleoside inhibitors: correlation of binding energy with biological activity for novel 2-aryl-substituted benzimidazole analogues.
National Cancer Institute-Frederick
Differential binding modes of diacylglycerol (DAG) and DAG lactones to protein kinase C (PK-C).
National Cancer Institute-Frederick
Structure-based design of thioether-bridged cyclic phosphopeptides binding to Grb2-SH2 domain.
National Cancer Institute-Frederick
Macrocyclization in the design of Grb2 SH2 domain-binding ligands exhibiting high potency in whole-cell systems.
National Cancer Institute-Frederick
Synthesis and evaluation of the sunflower derived trypsin inhibitor as a potent inhibitor of the type II transmembrane serine protease, matriptase.
National Cancer Institute-Frederick
Utilization of a peptide lead for the discovery of a novel PTP1B-binding motif.
National Cancer Institute-Frederick
Cyclopropane-derived peptidomimetics. Design, synthesis, evaluation, and structure of novel HIV-1 protease inhibitors.
National Cancer Institute-Frederick
Synthesis and biological activity of novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 2-Aryl-substituted benzimidazoles.
National Cancer Institute-Frederick
All-atom models for the non-nucleoside binding site of HIV-1 reverse transcriptase complexed with inhibitors: a 3D QSAR approach.
National Cancer Institute-Frederick
Bicyclic 1-hydroxy-2-oxo-1,2-dihydropyridine-3-carboxamide-containing HIV-1 integrase inhibitors having high antiviral potency against cells harboring raltegravir-resistant integrase mutants.
National Cancer Institute-Frederick
Synthesis, activity, and structural analysis of novel α-hydroxytropolone inhibitors of human immunodeficiency virus reverse transcriptase-associated ribonuclease H.
National Cancer Institute-Frederick
Development of tricyclic hydroxy-1H-pyrrolopyridine-trione containing HIV-1 integrase inhibitors.
National Cancer Institute-Frederick
Diketoacid-genre HIV-1 integrase inhibitors containing enantiomeric arylamide functionality.
National Cancer Institute-Frederick
Examination of halogen substituent effects on HIV-1 integrase inhibitors derived from 2,3-dihydro-6,7-dihydroxy-1H-isoindol-1-ones and 4,5-dihydroxy-1H-isoindole-1,3(2H)-diones.
National Cancer Institute-Frederick
2,3-dihydro-6,7-dihydroxy-1H-isoindol-1-one-based HIV-1 integrase inhibitors.
National Cancer Institute-Frederick
Histidine N(τ)-cyclized macrocycles as a new genre of polo-like kinase 1 polo-box domain-binding inhibitors.
National Cancer Institute-Frederick
Enhancing polo-like kinase 1 selectivity of polo-box domain-binding peptides.
National Cancer Institute-Frederick
