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Shaw NM Blanis D Bodek A Budd H Coombes R Eno S Fry CA Harada H Ho YH Kim YK Kumita T Mori T Olsen SL Sill A Thorndike EH Ueno K Zheng HW Imlay R Kirk P Lim J McNeil RR Metcalf W Myung SS Cheng CP Gu P Li J Li YK Mao ZP Xu YT Zhu YC Abashian A Gotow K Hu K Low EH Mattson ME Naito F Piilonen L Sterner KL Lusin S Rosenfeld C Wang AT Wilson S Frautschi M Kagan H Kass R Trahern CG Breedon RE Kim GN Ko W Lander RL Maeshima K Malchow RL Smith JR Sparks K Williams MC Abe K Fujii Y Higashi Y Kim SK 《Physical review letters》1989,63(13):1342-1345
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Dr. Nadja A. Simeth Thomas Kinateder Dr. Chitra Rajendran Julian Nazet Prof. Dr. Rainer Merkl Prof. Dr. Reinhard Sterner Prof. Dr. Burkhard König Dr. Andrea C. Kneuttinger 《Chemistry (Weinheim an der Bergstrasse, Germany)》2021,27(7):2439-2451
Light regulation of drug molecules has gained growing interest in biochemical and pharmacological research in recent years. In addition, a serious need for novel molecular targets of antibiotics has emerged presently. Herein, the development of a photocontrollable, azobenzene-based antibiotic precursor towards tryptophan synthase (TS), an essential metabolic multienzyme complex in bacteria, is presented. The compound exhibited moderately strong inhibition of TS in its E configuration and five times lower inhibition strength in its Z configuration. A combination of biochemical, crystallographic, and computational analyses was used to characterize the inhibition mode of this compound. Remarkably, binding of the inhibitor to a hitherto-unconsidered cavity results in an unproductive conformation of TS leading to noncompetitive inhibition of tryptophan production. In conclusion, we created a promising lead compound for combatting bacterial diseases, which targets an essential metabolic enzyme, and whose inhibition strength can be controlled with light. 相似文献
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Ivan Limachi Mariela Gonzalez-Ramirez Sophie Manner Juan C. Ticona Efrain Salamanca Alberto Gimenez Olov Sterner 《Molecules (Basel, Switzerland)》2021,26(4)
The fractionation of an ethanol extract of the bark of Trichilia adolfi yielded four novel limonoids (trichilinones A-D, 1–4), with five fused rings and related to the hortiolide-type limonoids. Starting with an ε-lactone, which is α,β-unsaturated in trichilinones A and D (1 and 4), attached to a tetrahydrofuran ring that is connected to an unusual bicyclo [5.1.0] hexane system, joined with a cyclopentanone with a 3-furanyl substituent [(2-oxo)-furan-(5H)-3-yl in trichilinone D (4)], the four compounds isolated display a new 7/5/3/5/5 limonoid ring system. Their structures were established based on extensive analysis of NMR spectroscopic data. As the crude extract possessed anti-leishmanial properties, the compounds were assayed for cytotoxic and anti-parasitic activities in vitro in murine macrophages cells (Raw 264.7) and leishmania promastigotes (L. amazoniensis and L. braziliensis), respectively. The compounds showed moderate cytotoxicity (approximately 70 μg/mL), but are not responsible for the leishmanicidal effect of the extract. 相似文献
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Results are presented on the efficient spectral manipulation of uniform and chirped Bragg reflectors inscribed in microstructured optical fibers utilizing short lengths of ferrofluids infiltrated in their capillaries. The infiltrated ferrofluidic defects can generate either parasitic reflection notch features in uniform Bragg reflectors of up to 80% visibility and ~0.1 nm spectral shift or tunability of the bandwidth and strength reflection up to 100% when introduced into chirped gratings. Spectra are presented for different spatial positions and optical characteristics of the ferrofluidic section. 相似文献
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Hong Li Sahas Rathi Elizabeth S. Sterner Hui Zhao Shaw Ling Hsu Patrick Theato Yongming Zhang E. Bryan Coughlin 《Journal of polymer science. Part A, Polymer chemistry》2013,51(20):4309-4316
The synthesis and characterization of a photocleavable block copolymer containing an ortho‐nitrobenzyl (ONB) linker between poly(methyl methacrylate) and poly(d ‐lactide) blocks is presented here. The block copolymers were synthesized via atom transfer radical polymerization (ATRP) of MMA followed by ring‐opening polymerization (ROP) of d ‐Lactide and ROP of d ‐lactide followed by ATRP of MMA from a difunctional photoresponsive ONB initiator, respectively. The challenges and limitations during synthesis of the photocleavable block copolymers using the difunctional photoresponsive ONB initiator are discussed. The photocleavage of the copolymers occurs under mild conditions by simple irradiation with 302 nm wavelength UV light (Relative intensity at 7.6 cm: 1500 μW/cm2) for several hours. © 2013 Wiley Periodicals, Inc. J. Polym. Sci., Part A: Polym. Chem. 2013, 51, 4309–4316 相似文献
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Kim YK Auchincloss P Blanis D Bodek A Budd H Eno S Fry CA Harada H Ho YH Kumita T Mori T Olsen SL Shaw NM Sill A Thorndike EH Ueno K Zheng HW Imlay R Kirk P Lim J McNeil RR Metcalf W Myung SS Cheng CP Gu P Li J Li YK Mao ZP Xu YT Zhu YC Abashian A Gotow K Hu KP Low EH Mattson ME Piilonen L Sterner KL Lusin S Rosenfeld C Wang AT Wilson S Frautschi M Kagan H Kass R Trahern CG Breedon RE Kim GN Ko W Lander RL Maeshima K Malchow RL Smith JR Stuart D Williams MC Abe K Fujii Y Higashi Y Kim SK 《Physical review letters》1989,63(17):1772-1775
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Eno S Auchincloss P Blanis D Bodek A Budd H Fry CA Harada H Ho YH Kim YK Kumita T Mori T Olsen SL Shaw NM Sill A Thorndike EH Ueno K Zheng HW Imlay R Kirk P Lim J McNeil RR Metcalf W Myung SS Cheng CP Gu P Li J Li YK Mao ZP Xu YT Zhu YC Abashian A Gotow K Hu KP Low EH Mattson ME Piilonen L Sterner KL Lusin S Rosenfeld C Wang AT Wilson S Frautschi M Kagan H Kass R Trahern CG Breedon RE Kim GN Ko W Lander RL Maeshima K Malchow RL Smith JR Stuart D Williams MC Abe K Fujii Y Higashi Y Kim SK 《Physical review letters》1989,63(18):1910-1913
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Söhretoğlu D Sakar MK Sabuncuoğlu SA Ozgüneş H Duman H Sterner O 《Natural product research》2012,26(13):1261-1264
Chromatographic studies on the EtOAc soluble portion of the MeOH extract of Geranium lasiopus led to the isolation of eight flavonoids (kaempferol (1), quercetin (2), quercetin 3-O-β-glucopyranoside (3), quercetin 3-O-β-galactopyranoside (4), kaempferol 3-O-α-rhamnopyranosyl-(1?→?6)-β-glucopyranoside (5), quercetin 3-O-α-rhamnopyranosyl-(1?→?6)-β-glucopyranoside (6), kaempferol 3-O-α-rhamnopyranosyl-(1?→?2)-β-glucopyranoside (7) and quercetin 3-O-α-rhamnopyranosyl-(1?→?2)-β-glucopyranoside (8)), two simple phenolic compounds (gallic acid (9) and its methyl ester (10)) and a hydrolysable tannin (pusilagin (11)). The structures of the compounds were elucidated by 1- and 2-dimensional NMR techniques ((1)H, (13)C, COSY, HMBC, HMQC) and ESI-TOF-MS spectrometry. Inhibitory effects on H(2)O(2)-induced lipid peroxidation in human red blood cells of the different extracts of G. lasiopus, as well as isolated compounds, were investigated. All tested compounds showed comparable or higher activity than that of ascorbic acid and trolox. 相似文献