CAS: 1405-97-6; Gramicidin

该化合物是一种聚苯丙胺抗生素,来源于巴氏菌菌菌,因其对抗克菌细菌的强效细菌杀菌活动而得到广泛承认;它通过形成离子渠道,导致细胞完整性丧失和最终细胞死亡,干扰细菌细胞膜;克赖米西丁在专题应用中特别有效,通常与新咪素和聚咪辛B等其他抗生素结合,以强化抗微生物覆盖率;其迅速行动和抗药性低,使其在包括药膏和眼科治疗在内的医学配方中具有价值;然而,其系统性毒性限制对局部治疗的使用;格赖米西丁在防治表面细菌感染方面,特别是在皮肤和眼科环境中,仍是一个关键组成部分.

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    专利信息


    专利号:US-4515920-A
    优先权日:1984-04-30
    标题 :Synthesis of peptides and proteins
    发明人:ERICKSON BRUCE W
    权利人:UNIV ROCKEFELLER
    摘要:Solid phase synthesis of peptides and proteins have been improved by the use of a trifunctional segment, one functional group of which is bound to a solid support, the other two functional groups being available as substrates upon which identical proteins are synthesized.

    专利号:US-9206222-B2
    优先权日:2009-06-29
    标题:Solid phase peptide synthesis of peptide alcohols
    发明人:CAUSSIL-AMBLARD MURIEL; MARTINEZ JEAN; TAILHADES JULIEN
    权利人:CAUSSIL-AMBLARD MURIEL; MARTINEZ JEAN; TAILHADES JULIEN; CENTRE NAT RECH SCIENT
    摘要:The present invention relates to the synthesis of depsipeptides on solid phase support. Said depsipeptides are then implicated in a solution phase O—N acyl shift enabling to obtain the corresponding peptide alcohols.

    专利号:US-11845970-B2
    优先权日:2016-01-15
    标 题:Endo-S2 mutants as glycosynthases, method of making and use for glycoengineering of glycoproteins
    发明人:WANG LAI-XI; YANG QIANG; LI TIEZHENG; TONG XIN
    权利人:UNIV MARYLAND
    摘要:The present invention provides for recombinant Endo-S2 mutants (named Endo-S2 glycosynthases) that exhibit reduced hydrolysis activity and increased transglycosylation activity for the synthesis of glycoproteins wherein a desired sugar chain is added to a fucosylated or nonfucosylated GlcNAc-IgG acceptor. As such, the present invention allows for the synthesis and remodeling of therapeutic antibodies thereby providing for certain biological activities, such as, prolonged half-life time in vivo, less immunogenicity, enhanced in vivo activity, increased targeting ability, and/or ability to deliver a therapeutic agent.

    专利号:US-12377186-B2
    优先权日:2018-01-19
    标 题:Antimicrobial biopolymer compositions, methods of synthesis, and applications of use
    发明人:KIM MINKYU; CAMP CHRISTOPHER P
    权利人:UNIV ARIZONA
    摘要:Biopolymer compositions comprising antimicrobial peptides (AMPs) for treating infections such as bacterial infections, viral infections, fungal infections, and parasitic infections. The compositions herein may also be used for treating infections associated with antibiotic-resistant bacteria, antifungal-resistant fungi, antiviral-resistant viruses, or for treating biological warfare agents (BWAs) such as Bacillus anthracis and Yersenia pestis. The present invention also provides methods of synthesis of said biopolymer compositions, wherein AMP biopolymers can be synthesized as an artificially engineered protein by genetically fusing an AMP; a protein that behaves similarly to polymer tethers; and a protein as a modifiable material platform that can transform to self-assembled nanoparticles, self-standing films, or adhesives to easily attach tethered AMPs onto any biomaterial surface for various clinical applications.

    专利号:US-2009124012-A1
    优先权日:2007-08-08
    标题:Toxin/antitoxin systems and methods for regulating cellular growth, metabolic engineering and production of recombinant proteins
    发明人:NIKOLSKY YURI; BAEV MARK
    权利人:MAZEF BIOSCIENCES LLC
    摘要:The present invention provides compositions and method for regulating cellular growth and metabolism, intra- and extracellular enzymatic activities, and synthesis of endogenous and/or heterologous proteins, comprising the steps of cloning genes encoding an mRNA interferase (toxin) and its cognate antitoxin; expressing these proteins in a host cell from two separate constitutive or inducible promoters on one or more plasmid vectors or on a chromosome; and regulating the cellular growth and metabolism by controlling the ratio of toxin and antitoxin present in the host cell. Optionally, the method provides further steps of modifying an endogenous or heterologous gene of interest to substitute all mRNA recognition sequences with sequences that are not cleavable by the mRNA interferase being expressed without any change in the amino acid sequence of the protein encoded by the gene; and co-expressing the gene of interest in the same host cell.

    专利号:US-2022395555-A1
    优先权日:2020-06-11
    标题:Derivatives of antibiotics
    发明人:FARBER BORIS; FARBER SOF'YA; MARTYNOV ARTUR VIKTOROVICH
    权利人:FARBER BORIS; FARBER SOFYA; MARTYNOV ARTUR VIKTOROVICH
    摘要:Field of application: The invention relates to chemistry, pharmacy and cosmetology, allows to synthesize of supramolecular structure on base antibiotics derivatives for use in pharmacy, cosmetology and pharmacy. n The essence of the invention: a new derivatives of antibiotics based on supramolecular structures and a method for their preparation, characterized in that the supramolecular structures are obtained by combinatorial synthesis of an antibiotic from one source molecule with two or more groups available in the reaction for covalent modification, at least with two different modifiers simultaneously, this creates a mixture of modified derivatives of the original molecule, with a maximum variety of derivatives with forming new supramolecular structure, and as biologically active substances to create pharmaceutical compositions use such supramolecular structure without separation into individual components, and in the reaction a combinatorial mixture of modified derivatives of the original molecule is formed antibiotic, the maximum number of combinations. n Technical result: modified combinatorial derivatives of antibiotics with antimicrobial and antifungal activity against multiresistant and pan drug resistance strains of microorganisms and fungi. Means have a wide spectrum of action, and the supramolecular and combinatorial structure of their tens and hundreds of derivatives eliminates the resistance of microorganisms.

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    主要参考文献


    1: Pavithrra G, Rajasekaran R. Identification of Effective Dimeric Gramicidin-D Peptide as Antimicrobial Therapeutics over Drug Resistance: In-Silico Approach. Interdiscip Sci. 2018 Sep 4. doi: 10.1007/s12539-018-0304-5. [Epub ahead of print] doi: 10.1016/j.bpj.2018.07.004. Epub 2018 Jul 11.
    3: Firsov AM, Pogozheva ID, Kovalchuk SI, Kotova EA, Antonenko YN. Effect of Site-Specific Intermolecular Lysine-Tryptophan Interactions on the Aggregation of Gramicidin-Based Peptides Leading to Pore Formation in Lipid Membranes. J Membr Biol. 2018 Jul 11. doi: 10.1007/s00232-018-0040-0. [Epub ahead of print] doi: 10.1140/epje/i2018-11644-5. doi: 10.1016/j.ejmech.2018.02.053. Epub 2018 Feb 21. doi: 10.1021/acs.analchem.7b02961. Epub 2018 Jan 16. pii: E422. doi: 10.3390/nano7120422.
    9: Chen D, Qin W, Wen G, Shi B, Liu Z, Wang Y, Zhou Q, Quan J, Zhou B, Bu X. Dissociation of haemolytic and oligomer-preventing activities of gramicidin S derivatives targeting the amyloid-β N-terminus. Chem Commun (Camb). 2017 Dec 14;53(100):13340-13343. doi: 10.1039/c7cc08180d. doi: 10.1039/c7sm01539a. doi: 10.1021/acs.joc.7b02177. Epub 2017 Nov 7. doi: 10.1016/j.bpj.2017.08.049.

    合成参考文献


    参考文献:10.1177/1087057116635503
    摘要:Voter AF, Manthei KA, Keck JL. A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. J Biomol Screen. 2016 Jul;21(6):626–33.
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