Search Results - "SPURLINO, J"
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The 2.3-A resolution structure of the maltose- or maltodextrin-binding protein, a primary receptor of bacterial active transport and chemotaxis
Published in The Journal of biological chemistry (15-03-1991)“…The three-dimensional structure of the maltose- or maltodextrin-binding protein (Mr = 40,622) with bound maltose has been obtained by crystallographic analysis…”
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2
Crystallographic evidence of a large ligand-induced hinge-twist motion between the two domains of the maltodextrin binding protein involved in active transport and chemotaxis
Published in Biochemistry (Easton) (01-11-1992)“…The periplasmic maltodextrin binding protein of Escherichia coli serves as an initial receptor for the active transport of and chemotaxis toward…”
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3
Extensive features of tight oligosaccharide binding revealed in high-resolution structures of the maltodextrin transport/chemosensory receptor
Published in Structure (London) (15-08-1997)“…Background: Active-transport processes perform a vital function in the life of a cell, maintaining cell homeostasis and allowing access of nutrients…”
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4
1.56 A structure of mature truncated human fibroblast collagenase
Published in Proteins, structure, function, and bioinformatics (01-06-1994)“…The X-ray crystal structure of a 19 kDa active fragment of human fibroblast collagenase has been determined by the multiple isomorphous replacement method and…”
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5
Structural Analysis of Thrombin Complexed with Potent Inhibitors Incorporating a Phenyl Group as a Peptide Mimetic and Aminopyridines as Guanidine Substitutes
Published in Journal of medicinal chemistry (04-06-1998)“…The structure of the noncovalent complex of human α-thrombin with a nonpeptide inhibitor containing a central phenyl scaffold,…”
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6
Structure of human neutrophil collagenase reveals large S1′ specificity pocket
Published in Nature structural biology (01-02-1994)“…The crystal structure of the catalytic domain of human neutrophil collagenase complexed with a peptide transition state analogue has been determined to a…”
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7
Inhibition of Matrix Metalloproteinases by Hydroxamates Containing Heteroatom-Based Modifications of the P1' Group
Published in Journal of medicinal chemistry (01-07-1995)“…In this study, structure-based drug design of matrix metalloproteinase inhibitors [human fibroblast collagenase (HFC), human fibroblast stromelysin (HFS), and…”
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8
Atomic interactions in protein-carbohydrate complexes. Tryptophan residues in the periplasmic maltodextrin receptor for active transport and chemotaxis
Published in Journal of molecular biology (05-07-1992)“…We have refined the 1.9 A resolution crystal structures of two maltodextrin receptor mutants in which tryptophan residues 230 and 232 have been changed to…”
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9
Genetic approach to the role of tryptophan residues in the activities and fluorescence of a bacterial periplasmic maltose-binding protein
Published in Journal of molecular biology (05-07-1990)“…The periplasmic maltose-binding protein (MBP or MalE protein) of Escherichia coli is an essential element in the transport of maltose and maltodextrins and in…”
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10
Proposed mechanisms for binding of apo[a] kringle type 9 to apo B-100 in human lipoprotein[a]
Published in Biophysical journal (01-03-1993)“…The protein component of human lipoprotein[a] consists primarily of two apolipoproteins, apo[a] and apo B-100, linked through a cystine disulfide(s). In the…”
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11
Progress in the identification of interaction sites on the periplasmic maltose binding protein from E coli
Published in Biochimie (01-06-1990)“…The periplasmic maltose binding protein (MBP) is required for the high affinity transport of maltose and maltodextrins and for chemotaxis towards these sugars…”
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12
Acetylcholine Receptor-α-Bungarotoxin Interactions: Determination of the Region-to-Region Contacts by Peptide-Peptide Interactions and Molecular Modeling of the Receptor Cavity
Published in Proceedings of the National Academy of Sciences - PNAS (01-08-1990)“…In previous studies from this laboratory, the binding regions of α-neurotoxins on human and Torpedo acetylcholine (AcCho) receptors (AcChoRs) and the binding…”
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13
Synthesis of thiophene-2-carboxamidines containing 2-aminothiazoles and their biological evaluation as urokinase inhibitors
Published in Bioorganic & medicinal chemistry letters (09-04-2001)“…The serine protease urokinase (uPa) has been implicated in the progression of both breast and prostate cancer. Utilizing structure based design, the synthesis…”
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14
Synthesis of thiophene-2-carboxamidines containing 2-amino-thiazoles and their biological evaluation as urokinase inhibitors
Published in Bioorganic & medicinal chemistry letters (09-04-2001)“…The serine protease urokinase (uPa) has been implicated in the progression of both breast and prostate cancer. Utilizing structure based design, the synthesis…”
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15
Oxyguanidines. Part 2: Discovery of a novel orally active thrombin inhibitor through structure-based drug design and parallel synthesis
Published in Bioorganic & medicinal chemistry letters (16-07-2004)“…Through structure-based drug design and parallel synthesis, we have discovered a novel series of nonpeptidic phenyl-based thrombin inhibitors using…”
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Serendipity meets precision: the integration of structure-based drug design and combinatorial chemistry for efficient drug discovery
Published in Structure (15-03-1997)“…Structure-based drug design uses three-dimensional visualization of drug candidates bound to a target receptor to direct structural modifications that increase…”
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Book Review Journal Article -
17
Discovery and Cocrystal Structure of Benzodiazepinedione HDM2 Antagonists That Activate p53 in Cells
Published in Journal of medicinal chemistry (24-02-2005)“…HDM2 binds to an α-helical transactivation domain of p53, inhibiting its tumor suppressive functions. A miniaturized thermal denaturation assay was used to…”
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18
Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors
Published in Bioorganic & medicinal chemistry letters (17-04-2003)“…Although thrombin has been extensively researched with many examples of potent and selective inhibitors, the key characteristics of oral bioavailability and…”
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19
Amidinohydrazones as guanidine bioisosteres : Application to a new class of potent, selective and orally bioavailable, non-amide-based small-molecule thrombin inhibitors
Published in Bioorganic & medicinal chemistry letters (03-01-2000)“…We describe a new class of potent, non-amide-based small molecule thrombin inhibitors in which an amidinohydrazone is used as a guanidine bioisostere on a…”
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20
In vitro evaluation and crystallographic analysis of a new class of selective, non-amide-based thrombin inhibitors
Published in Bioorganic & medicinal chemistry letters (07-07-1998)“…We describe the in vitro evaluation and crystallographic analysis of a new class of potent and selective, non-aminoacid-based, small-molecule thrombin…”
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