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Probes for narcotic receptor mediated phenomena. 12. cis-(+)-3-Methylfentanyl isothiocyanate, a potent site-directed acylating agent for delta opioid receptors. Synthesis, absolute configuration, and receptor enantioselectivity.

TBA
Probes for narcotic receptor mediated phenomena. 9. Synthesis of (+/-)-(3 alpha,6a alpha,11a beta)-1,3,4,5,6,11a-hexahydro-2-methyl-2H-3,6a- methanobenzofuro[2,3-c]azocin-10-ol, an oxide-bridged 5-(m-hydroxyphenyl)morphan.

TBA
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
4-amino-1-hydroxy-2-oxo-1,8-naphthyridine-containing compounds having high potency against raltegravir-resistant integrase mutants of HIV-1.

National Institutes of Health
Synthesis, configuration, and evaluation of two conformationally restrained analogues of phencyclidine.

National Institute of Diabetes, Digestive and Kidney Diseases
Non-proteinogenic amino acids in the pThr-2 position of a pentamer peptide that confer high binding affinity for the polo box domain (PBD) of polo-like kinase 1 (Plk1).

Frederick National Laboratory For Cancer Research
Discovery of thioether-bridged cyclic pentapeptides binding to Grb2-SH2 domain with high affinity.

Chinese Academy of Sciences
Protected aminooxyprolines for expedited library synthesis: application to Tsg101-directed proline-oxime containing peptides.

Nih
Structure activity of 3-aryl-1,3-diketo-containing compounds as HIV-1 integrase inhibitors.

National Cancer Institute/Nih
Antiretroviral agents as inhibitors of both human immunodeficiency virus type 1 integrase and protease.

National Cancer Institute-Bethesda
Probes for narcotic receptor mediated phenomena. 7. Synthesis and pharmacological properties of irreversible ligands specific for mu or delta opiate receptors.

TBA
Elucidation of New Binding Interactions with the Tumor Susceptibility Gene 101 (Tsg101) Protein Using Modified HIV-1 Gag-p6 Derived Peptide Ligands.

Nci-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
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
Identification of Shc Src homology 2 domain-binding peptoid-peptide hybrids.

National Cancer Institute-Frederick
Fine-tuning probes for fluorescence polarization binding assays of bivalent ligands against polo-like kinase 1 using full-length protein.

Institute of Science Tokyo
Coumarin-based inhibitors of human NAD(P)H:quinone oxidoreductase-1. Identification, structure-activity, off-target effects and in vitro human pancreatic cancer toxicity.

University of Manchester
Examination of acylated 4-aminopiperidine-4-carboxylic acid residues in the phosphotyrosyl+1 position of Grb2 SH2 domain-binding tripeptides.

National Cancer Institute-Frederick
Application of azide-alkyne cycloaddition 'click chemistry' for the synthesis of Grb2 SH2 domain-binding macrocycles.

Nih
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
Synthesis of tripeptides as potent Yersinia protein tyrosine phosphatase inhibitors.

Nih
Examination of phosphoryl-mimicking functionalities within a macrocyclic Grb2 SH2 domain-binding platform.

National Cancer Institute-Frederick
Utilization of a nitrobenzoxadiazole (NBD) fluorophore in the design of a Grb2 SH2 domain-binding peptide mimetic.

Nih
Design and synthesis of conformationally constrained Grb2 SH2 domain binding peptides employing alpha-methylphenylalanyl based phosphotyrosyl mimetics.

National Cancer Institute-Frederick
Macrocyclization in the design of non-phosphorus-containing Grb2 SH2 domain-binding ligands.

National Cancer Institute-Frederick
Design and synthesis of photoactivatable aryl diketo acid-containing HIV-1 integrase inhibitors as potential affinity probes.

Nci-Frederick
Synthesis of a 5-methylindolyl-containing macrocycle that displays ultrapotent Grb2 SH2 domain-binding affinity.

National Cancer Institute-Frederick
Acylsulfonamide-containing PTP1B inhibitors designed to mimic an enzyme-bound water of hydration.

Nih
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
Azido-containing aryl beta-diketo acid HIV-1 integrase inhibitors.

National Cancer Institute-Bethesda
Macrocyclization in the design of Grb2 SH2 domain-binding ligands exhibiting high potency in whole-cell systems.

National Cancer Institute-Frederick
Metal-dependent inhibition of HIV-1 integrase.

University of Southern California
Development of a phosphatase-stable phosphotyrosyl mimetic suitably protected for the synthesis of high-affinity Grb2 SH2 domain-binding ligands.

National Institutes of Health
Utilization of a peptide lead for the discovery of a novel PTP1B-binding motif.

National Cancer Institute-Frederick
Macrocyclization in the design of a conformationally constrained Grb2 SH2 domain inhibitor.

National Institutes of Health
Examination of novel non-phosphorus-containing phosphotyrosyl mimetics against protein-tyrosine phosphatase-1B and demonstration of differential affinities toward Grb2 SH2 domains.

National Cancer Institute-Bethesda
Inhibition of Grb2 SH2 domain binding by non-phosphate-containing ligands. 2. 4-(2-Malonyl)phenylalanine as a potent phosphotyrosyl mimetic.

National Cancer Institute-Bethesda
Chicoric acid analogues as HIV-1 integrase inhibitors.

National Cancer Institute-Bethesda
Monocarboxylic-based phosphotyrosyl mimetics in the design of GRB2 SH2 domain inhibitors.

National Cancer Institute-Bethesda
Potent inhibition of Grb2 SH2 domain binding by non-phosphate-containing ligands.

National Cancer Institute-Bethesda
Potent inhibition of protein-tyrosine phosphatase-1B using the phosphotyrosyl mimetic fluoro-O-malonyl tyrosine (FOMT).

National Cancer Institute-Bethesda
Salicylhydrazine-containing inhibitors of HIV-1 integrase: implication for a selective chelation in the integrase active site.

National Cancer Institute-Bethesda
Arylamide inhibitors of HIV-1 integrase.

National Cancer Institute-Bethesda
Hydrazide-containing inhibitors of HIV-1 integrase.

National Cancer Institute-Bethesda
Discovery of HIV-1 integrase inhibitors by pharmacophore searching.

National Cancer Institute-Bethesda
Coumarin-based inhibitors of HIV integrase.

National Cancer Institute-Bethesda
4'-O-[2-(2-fluoromalonyl)]-L-tyrosine: a phosphotyrosyl mimic for the preparation of signal transduction inhibitory peptides.

National Cancer Institute-Bethesda
Bicyclic compounds as ring-constrained inhibitors of protein-tyrosine kinase p56lck.

National Cancer Institute-Bethesda
Hydroxylated 2-(5'-salicyl)naphthalenes as protein-tyrosine kinase inhibitors.

National Institutes of Health
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
Non-amine based analogues of lavendustin A as protein-tyrosine kinase inhibitors.

National Institutes of Health
L-O-(2-malonyl)tyrosine: a new phosphotyrosyl mimetic for the preparation of Src homology 2 domain inhibitory peptides.

National Cancer Institute-Bethesda
Hydroxylated aromatic inhibitors of HIV-1 integrase.

National Cancer Institute-Bethesda
6,7-Dihydroxy-1-oxoisoindoline-4-sulfonamide-containing HIV-1 integrase inhibitors.

Frederick National Laboratory For Cancer Research
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
Synthesis and pharmacological characterization of (+/-)-5,9 alpha-dimethyl-2-[2-(4-fluorophenyl)ethyl]-2'-hydroxy-6,7-benzomorphan (fluorophen), a ligand suitable for visualization of opiate receptors in vivo.

TBA
Histidine N(τ)-cyclized macrocycles as a new genre of polo-like kinase 1 polo-box domain-binding inhibitors.

National Cancer Institute-Frederick
Phosphonate-containing inhibitors of tyrosine-specific protein kinases.

National Cancer Institute-Bethesda
Enhancing polo-like kinase 1 selectivity of polo-box domain-binding peptides.

National Cancer Institute-Frederick
Novel nonsecosteroidal vitamin D mimics exert VDR-modulating activities with less calcium mobilization than 1,25-dihydroxyvitamin D3.

Ligand Pharmaceuticals
A fragment-based approach for the discovery of isoform-specific p38alpha inhibitors.

Burnham Institute For Medical Research