Search Results - "Burlingame, Mark A."
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Turning a protein kinase on or off from a single allosteric site via disulfide trapping
Published in Proceedings of the National Academy of Sciences - PNAS (12-04-2011)“…There is significant interest in identifying and characterizing allosteric sites in enzymes such as protein kinases both for understanding allosteric…”
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2
Capture of micrococcin biosynthetic intermediates reveals C-terminal processing as an obligatory step for in vivo maturation
Published in Proceedings of the National Academy of Sciences - PNAS (01-11-2016)“…Thiopeptides, including micrococcins, are a growing family of bioactive natural products that are ribosomally synthesized and heavily modified. Here we use a…”
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3
Reconstitution and Minimization of a Micrococcin Biosynthetic Pathway in Bacillus subtilis
Published in Journal of bacteriology (15-09-2016)“…Thiopeptides represent one of several families of highly modified peptide antibiotics that hold great promise for natural product engineering. These…”
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4
Identification and Optimization of Thienopyridine Carboxamides as Inhibitors of HIV Regulatory Complexes
Published in Antimicrobial agents and chemotherapy (01-07-2017)“…Viral regulatory complexes perform critical functions during virus replication and are important targets for therapeutic intervention. In HIV, the Tat and Rev…”
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5
Simple One-Pot Synthesis of Disulfide Fragments for Use in Disulfide-Exchange Screening
Published in ACS combinatorial science (09-05-2011)“…Disulfide exchange screening is a method for evaluating the binding of small molecule fragments to proteins that have at least one accessible cysteine. While…”
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6
Toward Understanding How the Lactone Moiety of Discodermolide Affects Activity
Published in Journal of the American Chemical Society (11-05-2005)“…A series of simplified discodermolide analogues have been designed and synthesized in an attempt to understand the role of the lactone ring. These synthetic…”
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7
Structure−Activity Relationships of 9-Substituted-9-Dihydroerythromycin-Based Motilin Agonists: Optimizing for Potency and Safety
Published in Journal of medicinal chemistry (12-11-2009)“…A series of 9-dihydro-9-acetamido-N-desmethyl-N-isopropyl erythromycin A analogues and related derivatives was generated as motilin agonists. The compounds…”
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8
Design, Synthesis, and Evaluation of Carbamate-Substituted Analogues of (+)-Discodermolide
Published in Organic letters (20-01-2005)“…The design, syntheses, and biological evaluation of 22 totally synthetic analogues of the potent microtubule-stabilizing agent (+)-discodermolide (1) have been…”
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Design, Synthesis, and Evaluation of Analogues of (+)-14-Normethyldiscodermolide
Published in Organic letters (20-01-2005)“…The design, syntheses, and biological evaluation of nine totally synthetic analogues of the microtubule-stabilizing agent (+)-14-normethyldiscodermolide (2)…”
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10
A series of 23,24-dihydrodiscodermolide analogues with simplified lactone regions
Published in Bioorganic & medicinal chemistry letters (01-04-2006)“…A collection of seven new 23,24-dihydrodiscodermolide analogues have been synthesized with modifications to the lactone ring, some of which show…”
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11
Design, synthesis and cytotoxicity of 7-deoxy aryl discodermolide analogues
Published in Bioorganic & medicinal chemistry letters (03-05-2004)“…A series of 7-deoxy discodermolide analogues in which the lactone fragment 'C' was replaced by aryl substituents were designed, synthesized, and evaluated for…”
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Synthesis of discodermolide intermediates from engineered polyketides
Published in Tetrahedron letters (13-02-2006)“…Key intermediates used in Smith’s total synthesis of discodermolide were synthesized from an engineered polyketide made via precusor feeding to genetically…”
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13
N-Acyl-2-benzoxazolinones in titanium-mediated aldol reactions
Published in Tetrahedron letters (29-03-2004)“…Graphic N-Acyl-2-benzoxazolinones readily form trichlorotitanium enolates that react rapidly with aldehydes to provide crystalline syn-aldol adducts in high…”
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