ADVERTISEMENT RETURN TO ISSUEPREVCommunicationNEXTAntiparallel Leucine Zipper-Directed Protein Reassembly: Application to the Green Fluorescent ProteinIndraneel Ghosh, Andrew D. Hamilton, and Lynne ReganView Author Information Department of Chemistry Molecular Biophysics Biochemistry Yale University, New Haven, Connecticut 06520 Cite this: J. Am. Chem. Soc. 2000, 122, 23, 5658–5659Publication Date (Web):May 24, 2000Publication History Received20 December 1999Published online24 May...

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTMolecular recognition: hydrogen-bonding receptors that function in highly competitive solventsErkang Fan, Scott A. Van Arman, Kincaid, and Andrew D. HamiltonCite this: J. Am. Chem. Soc. 1993, 115, 1, 369–370Publication Date (Print):January 1993Publication History Published online1 May 2002Published inissue 1 January 1993https://pubs.acs.org/doi/10.1021/ja00054a066https://doi.org/10.1021/ja00054a066research-articleACS PublicationsRequest reuse...

Signal transducers and activators of transcription (STATs) comprise a family cytoplasmic signaling proteins that participates in normal cellular responses to cytokines growth factors. Frequently, however, constitutive activation certain STAT members, particularly Stat3, has accompanied wide variety human malignancies. To identify small molecule inhibitors we investigated the ability Stat3 SH2 domain-binding peptide, PY*LKTK (where Y* represents phosphotyrosine), disrupt activity <i>in...

Identification of protein binding partners is one the key challenges proteomics. We recently introduced a screen for detecting protein−protein interactions based on reassembly dissected fragments green fluorescent fused to interacting peptides. Here, we present set comaintained Escherichia coli plasmids facile subcloning fusions fragments. Using library antiparallel leucine zippers, have shown that can detect very weak (KD ≈ 1 mM). In vitro kinetics show reaction essentially irreversible,...

Accumulated studies have shown that activation of the Akt pathway plays a pivotal role in malignant transformation and chemoresistance by inducing cell survival, growth, migration, angiogenesis. Therefore, is believed to be critical target for cancer intervention. Here, we report discovery small molecule inhibitor, Akt/protein kinase B signaling inhibitor-2 (API-2), screening National Cancer Institute Diversity Set. API-2 suppressed activity phosphorylation level Akt. The inhibition resulted...

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTMolecular recognition of biologically interesting substrates: synthesis an artificial receptor for barbiturates employing six hydrogen bondsSuk Kyu. Chang and Andrew D. HamiltonCite this: J. Am. Chem. Soc. 1988, 110, 4, 1318–1319Publication Date (Print):February 17, 1988Publication History Published online1 May 2002Published inissue 17 February 1988https://pubs.acs.org/doi/10.1021/ja00212a065https://doi.org/10.1021/ja00212a065research-articleACS...

Intrusion detection has attracted a considerable interest from researchers and industries. The community, after many years of research, still faces the problem building reliable efficient IDS that are capable handling large quantities data, with changing patterns in real time situations. work presented this manuscript classifies intrusion systems (IDS). Moreover, taxonomy survey shallow deep networks is based on previous current works. This reviews machine learning techniques their...

Ras-induced malignant transformation requires Ras farnesylation, a lipid posttranslational modification catalyzed by farnesyltransferase (FTase). Inhibitors of this enzyme have been shown to block Ras-dependent transformation, but the mechanism which occurs remains largely unknown. We designed FTI-276, peptide mimetic COOH-terminal Cys-Val-Ile-Met K-Ras4B that inhibited potently FTase in vitro (IC50 = 500 pM) and was highly selective for over geranylgeranyltransferase I (GGTase I) 50 nM)....

Abstract Bisphosphonates are the important class of antiresorptive drugs used in treatment metabolic bone diseases. Although their molecular mechanism action has not been fully elucidated, recent studies have shown that nitrogen-containing bisphosphonates can inhibit protein prenylation macrophages vitro. In this study, we show risedronate, zoledronate, ibandronate, alendronate, and pamidronate (but non clodronate, etidronate, tiludronate) prevent incorporation [14C]mevalonate into...

ADVERTISEMENT RETURN TO ISSUEPREVCommunicationNEXTToward Proteomimetics: Terphenyl Derivatives as Structural and Functional Mimics of Extended Regions an α-HelixBrendan P. Orner, Justin T. Ernst, Andrew D. HamiltonView Author Information Department Chemistry, Yale University P.O. Box 208107, New Haven, Connecticut 06510-8107 Cite this: J. Am. Chem. Soc. 2001, 123, 22, 5382–5383Publication Date (Web):May 11, 2001Publication History Received13 July 2000Published online11 May 2001Published...

A family of novel oligomers based on the anthranilamide nucleus has been prepared and shown to form well-defined secondary structural features. 1H NMR X-ray crystallographic techniques have demonstrated that intramolecular hydrogen bonds play a key role in stabilizing both linear sheet helical conformational forms.

At concentrations as low 0.3 wt % a novel family of bis-urea dicarboxylic acids gel water (see picture). The aggregation state (vesicles, gel, or fibers) depends on the pH, ionic strength, and molecular weight gelator. In this way, gelation properties an aqueous system are controlled by design.

The prevention of cell death by the antiapoptotic protein Bcl-xL has been linked to a number cancers. Bcl-xl binds BH3 domain proapoptotic Bak, thus preventing programmed death. A competitive assay and docking studies have shown that polyamide scaffold 1, which was synthesized based on rational structure-based design, interferes with Bak BH3/Bcl-xl complexation.

The design of artificial models the processes biomineralization has resulted in union inorganic materials research and supramolecular organic chemistry. Recent work this field bioinspired synthesis composite organic/inorganic is reviewed prospects for future are discussed. Attention focused on use self-assembled superstructures to template with controlled morphologies.

The critical role of signal transducer and activator transcription 3 (Stat3) in the growth survival human tumor cells identifies it as a promising target for cancer drug discovery. We previously identified Stat3 SH2 domain-binding phosphopeptide, PY*LKTK, its tripeptide derivatives, PY*L AY*L (where Y* represents phosphotyrosine), which inhibit biochemical activity biological function. Here, we report novel peptidomimetic compounds based on (or AY*L) with substitution Y-1 residue by benzyl,...

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTInduced fit in synthetic receptors: nucleotide base recognition by a molecular hingeAndrew D. Hamilton and Donna Van EngenCite this: J. Am. Chem. Soc. 1987, 109, 16, 5035–5036Publication Date (Print):August 1, 1987Publication History Published online1 May 2002Published inissue 1 August 1987https://pubs.acs.org/doi/10.1021/ja00250a052https://doi.org/10.1021/ja00250a052research-articleACS PublicationsRequest reuse permissionsArticle...