Explanipedia

Replacement of Phe6, Phe7, and Phe11ofd-Trp8-Somatostatin-14 withl-Pyrazinylalanine. Predicted and Observed Effects on Binding Affinities at hSST2 and hSST4. An Unexpected Effect of the Chirality of Trp8on NMR Spectra in Methanol Open

Santhosh Neelamkavil, Byron H. Arison, Elizabeth T. Birzin, Jin-Jye Feng, Kuo-Hsin Chen , et al. · 2005

An alanine scan performed in the 1970s suggested that Phe(6) and Phe(11) are required for the binding of somatostatin (SRIF-14). Molecular modeling studies and replacement of Phe(6) and Phe(11) with a cystine bridge affording ligands with …

CCDC 100975: Experimental Crystal Structure Determination Open

Stefan Knapp, Jayasree Vasudevan, Thomas J. Emge, Byron H. Arison, J.A. Potenza , et al. · 1999

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …

Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2 Open

Lihu Yang, Scott C. Berk, Susan P. Rohrer, Ralph T. Mosley, Liangqin Guo , et al. · 1998

A series of nonpeptide somatostatin agonists which bind selectively and with high affinity to somatostatin receptor subtype 2 (sst2) have been synthesized. One of these compounds, L-054,522, binds to human sst2 with an apparent dissociatio…

Synthesis of the first tricyclic homodetic peptide. Use of coordinated orthogonal deprotection to achieve directed ring closure Open

Ralph Hirschmann, Wenqing Yao, Byron H. Arison, Laurie Maechler, Avery Rosegay , et al. · 1998

The discovery of somatostatin antagonists at one or more receptor subtypes remains an important goal. We therefore undertook the synthesis of the homodetic tricyclic peptide (1) hoping to cause conformational distortion and thereby achieve…

Cumulative Author Index Open

Robert Aarhus, Derek Abbott, Aida Abdulmessih, Abe Hiromi, Amy Abell , et al. · 1997

Farnesol-derived Dicarboxylic Acids in the Urine of Animals Treated with Zaragozic Acid A or with Farnesol Open

Richard G. Bostedor, John D. Karkas, Byron H. Arison, Vinay S. Bansal, Sanskruti Vaidya , et al. · 1997

Farnesyl diphosphate, the substrate for squalene synthase, accumulates in the presence of zaragozic acid A, a squalene synthase inhibitor. A possible metabolic fate for farnesyl diphosphate is its conversion to farnesol, then to farnesoic …

Chemical and Biological Characterization of Two FK506 Analogs Produced by Targeted Gene Disruption in Streptomyces sp. MA6548. Open

Ali Shafiee, Haideh Motamedi, Francis J. Dumont, Byron H. Arison, Randall R. Miller · 1997

Two genetically engineered mutant strains of Streptomyces sp. MA6548 produced two FK506 analogs, 9-deoxo-31-O-demethylFK506 and 31-O-demethylFK506. The structures were determined by a combination of NMR and mass spectrometry. These compoun…

Characterization of methyltransferase and hydroxylase genes involved in the biosynthesis of the immunosuppressants FK506 and FK520 Open

Haideh Motamedi, Ali Shafiee, Sheng‐Jian Cai, S L Streicher, Byron H. Arison , et al. · 1996

FK506 and FK520 are 23-membered macrocyclic polyketides with potent immunosuppressive and antifungal activities. The gene encoding 31-O-demethyl-FK506 methyltransferase, fkbM, was isolated from Streptomyces sp. strains MA6858 and MA6548, t…

The first synthesis of a tricyclic homodetic peptide employing coordinated orthogonal protection Open

Ralph Hirschmann, Wenqing Yao, Byron H. Arison, Laurie Maechler, Avery Rosegay , et al. · 1996

In an effort to cause significant conformational distortion and thereby possibly generate a pure SRIF antagonist, we undertook the synthesis of 2, the first homodetic tricyclic peptide. This required five dimensional orthogonal amino prote…

Microbial transformation ofN-heptyl physostigmine, a semisynthetic alkaloid inhibitor of cholinesterase Open

Lie So, Rebecca B. White, Byron H. Arison, Brian R. Petuch, Michael S. Schwartz , et al. · 1995

The microbiological transformation of N-heptyl physostigmine (L-693,487) (1), a semisynthetic physostigmine cholinesterase inhibitor, was investigated using Verticillium lecanii MF 5713 (ATCC 74148), Acremonium sp MF 5723 (ATCC 74164) and …

Microbial conversion of avermectins by Saccharopolyspora erythraea: Hydroxylation at C-27. Open

Marvin Schulman, Patrick Doherty, Deborah L. Zink, Byron H. Arison · 1994

The avermectins, a family of secondary metabolites produced by Streptomyces avermitilis, are oleandrose disaccharide derivatives of sixteen membered macrolides with potent anthelmintic and insecticidal activity1 ~4).The general structure o…

Microbial transformations of immunosuppressive compounds. IV. Hydroxylation and hemiketal formation of ascomycin(immunomycin) by Streptomyces sp. MA6970(ATCC No.55281). Open

Tom S. Chen, Brian R. Petuch, Richard White, Gabe Dezeny, X. Li , et al. · 1994

The important immunosuppressive agents FK 5061>2) and ascomycin3~5) (1) have been the target of intensive structure-activity relationship (SAR) studies6).FK 506 recently received FDAapproval for liver organ transplantation in the United St…

Microbial conversion of avermectins by Saccharopolyspora erythrea: Hydroxylation at C28. Open

Marvin Schulman, Patrick Doherty, Deborah L. Zink, Byron H. Arison · 1993

Microbial transformation of immunosuppressive compounds. I. Desmethylation of FK 506 and immunomycin (FR 900520) by Actinoplanes sp. ATCC 53771. Open

Tom S. Chen, Byron H. Arison, Linda S. Wicker, Edward Inamine, Richard L. Monaghan · 1992

The immunosuppressants FK506 and FR 900520 were desmethylated by Actinoplanes sp. ATCC 53771 to yield various O-desmethylated products. The products were isolated and purified by solvent extraction and HPLC chromatography, and identified b…

Microbial transformation of immunosuppressive compounds. II. Specific desmethylation of 13-methoxy group of FK 506 and FR 900520 by Actinomycete sp. ATCC 53828. Open

Tom S. Chen, Byron H. Arison, Linda S. Wicker, Edward Inamine · 1992

FK 506 and FR 900520 are a new class of fermentation products, isolated from Streptomyces tsukubaensisjStreptomyces hygroscopicus species ascomyceticus MA64751~5),showing potent inhibition of T cell activation6).In the course of our recent…

Epoxyexserohilone, a Novel Metabolite from Nigrospora sphaerica. Open

Horace G. Cutler, Karst Hoogsteen, R. H. Littrell, Byron H. Arison · 1991

Fermentation of Nigrospora sphaerica on shredded wheat medium generated the novel metabolite, epoxyexserohilone, a congener of the known phytotoxin, exserohilone. Single crystal X-ray diffraction determined the structure and absolute stere…

Purification and identification of dTDP-oleandrose, the precursor of the oleandrose units of the avermectins. Open

Marvin D. Schulman, Susan Acton, Delia Valentino, Byron H. Arison · 1990

The nucleotide sugar precursor of the oleandrose units of the avermectins has been purified from a mutant of Streptomyces avermitilis, which does not synthesize any avermectins but which converts avermectin aglycones to their respective di…

Further studies on the biosynthesis of the avermectins Open

Tom S. Chen, Byron H. Arison, Vincent P. Gullo, Edward Inamine · 1989

The biosynthesis of avermectins was studied further inStreptomyces avermitilis MA5502 by feeding experiments with labeled precursors.13C-NMR analysis of the compounds biosynthesized from [2-13C]acetate, [1,2-13C2]acetate, [3-13C]propionate…

3-Methylpseudouridine as a fermentation product. Open

Jennifer Nielsen, Byron H. Arison · 1989

3-Methylpseudouridine (beta isomer) has been identified in fermentation broths of Nocardia lactamdurans. It accumulates at quite high levels following the accumulation of extracellular uracil in strains exhibiting increased levels of de no…

Cinereain. A novel metabolite with plant growth regulating properties from Botrytis cinerea. Open

Horace G. Cutler, James P. Springer, Richard F. Arrendale, Byron H. Arison, Patsy D. Cole , et al. · 1988

Botrytis cinerea, which was isolated from the surface of stored sunflower seed, produced a novel biologically active natural product when cultured on shredded wheat medium. The metabolite, trivially named cinereain, was a ruby red crystall…

Isopentenoid synthesis in isolated embryonic Drosophila cells. Farnesol catabolism and omega-oxidation. Open

Dolores González‐Pacanowska, Byron H. Arison, Christopher Havel, John Watson · 1988

Kc cells divert minimally 40% of their mevalonate carbon to n-fatty acids and unidentified compounds covalently linked to macromolecules (Havel, C., Rector, E. R., II, and Watson, J. A. (1986) J. Biol. Chem. 261, 10150-10156). Furthermore …

Biosynthesis of fluorothreonine and fluoroacetic acid by the thienamycin producer, Streptomyces cattleya. Open

M Sanada, Tetsuji Miyano, Shuichi Iwadare, Joanne M. Williamson, Byron H. Arison , et al. · 1986

An antimetabolite, THX, was isolated from fermentation broths of the thienamycin producer, Streptomyces cattleya, when the organism was grown in the presence of a fluorine-containing substrate. THX was subsequently identified as one of the…

The structure of efrotomycin. Open

Ray S. Dewey, Byron H. Arison, John Hannah, David H. Shih, GEORG ALBERS-SCHÖNBERG · 1985

The antibiotic efrotomycin (I), C59H88N2O20, was isolated from cultures of Nocardia lactamdurans as an amorphous yellow powder. Mass spectral and NMR analyses show that the compound is a glycoside of the known antibiotic aurodox (II), C44H…

The pterin component of the molybdenum cofactor. Structural characterization of two fluorescent derivatives. Open

Jason L. Johnson, Bryan E. Hainline, K.V. Rajagopalan, Byron H. Arison · 1984

Two stable fluorescent derivatives of molybdopterin have been structurally characterized. Form A is an oxidized pterin with a 6-alkyl substituent. Results of chemical, mass spectral, and NMR studies are consistent with the side chain formu…

Production of the cephalosporate C-2 by a Streptomyces lactamdurans mutant defective in cephamycin C biosynthesis. Open

A Rein, Byron H. Arison, Thomas W. Miller, Barbara D. Lago, Charles Ginther · 1984

The structure of virustomycin A. Open

Satoshi Ōmura, Nobutaka Imamura, Kiyoizumi Hinotozawa, Kazuhiko Otoguro, Gabor Lukacs , et al. · 1983

Northienamycin and 8-epi-thienamycin, new carbapenems from Streptomyces cattleya. Open

Kenneth E. Wilson, AUGUST J. KEMPF, Jerrold M. Liesch, Byron H. Arison · 1983

Two new carbapenem antibiotics, northienamycin and 8-epi-thienamycin have been isolated from culture broth of Streptomyces cattleya grown under conditions for thienamycin production. The isolation, structure elucidation and in vitro antiba…

Epithienamycins. II. Isolation and structure assignment. Open

Patrick J. Cassidy, G. Albers‐Schönberg, Robert T. Goegelman, Thomas W. Miller, Byron H. Arison , et al. · 1981

At least six distinct beta-lactam antibiotics of the epithienamycin family are produced by a strain of Streptomyces flavogriseus MB 4638. Each of the six can be isolated in substantially pure form by column chromatography using Dowex 1, Am…

Book Review Open

Sidney Udenfriend, Carol A. Shively, Richard J. Simons, Elliot S. Vesell, Jack Hinson , et al. · 1979

REVISED STRUCTURE OF CERULENIN Open

Byron H. Arison, Satoshi Ōmura · 1974

An evaluation of the 100 MHz NMR spectrum strongly suggests that the structure of cerulenin is (2S) (3R) 2, 3-epoxy-4-oxo-7, 10-dodecadienoyl amide rather than the -6, 10-dodecadienoyl amide analog. This conclusion was experimentally suppo…

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