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Open AccessJournal ArticleDOI

Rapamycin (ay-22, 989), a new antifungal antibiotic i. taxonomy of the producing streptomycete and isolation of the active principle

Claude Vezina, +2 more
- 01 Oct 1975 - 
- Vol. 28, Iss: 10, pp 721-726
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TLDR
From its characteristic ultraviolet absorption spectrum rapamycin can be classified as a triene and its activity is compared with that of amphotericin B, candicidin and nystatin.
Abstract
A streptomycete was isolated from an Easter Island soil sample and found to inhibit Candida albicans, Microsporum gypseum and Trichophyton granulosum. The antibiotic-producing microorganism was characterized and identified as Streptomyces hygroscopicus. The antifungal principle was extracted with organic solvent from the mycelium, isolated in crystalline form and named rapamycin. Rapamycin is mainly active against Candida albicans; minimum inhibitory concentration against ten strains ranged from 0.02 to 0.2 mug/ml. Its apparent activity against Microsporum gypseum and Trichophyton granulosum is lower because of its instability in culture media on prolonged incubation required by these fungi. No activity was observed against gram-positive and gram-negative bacteria. Acute toxicity in mice is low.

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Journal ArticleDOI

Mammalian target of rapamycin and head and neck squamous cell carcinoma

TL;DR: In in vivo and in vitro studies, mTOR inhibitor suppresses tumor growth and sensitizes HNSCC to radiation, cytotoxic agents and epidermoid growth factor receptor inhibitors.
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The tyrosine89 residue of yeast FKBP12 is required for rapamycin binding.

TL;DR: To identify missense mutations that define amino acid (aa) residues in RBP1 involved in drug sensitivity, over 250 independent RmR rbp1 mutants were selected and genetically characterized and screened them for bothRBP1-specific mRNA and protein expression.
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Rapamycin enhances chemotherapy-induced cytotoxicity by inhibiting the expressions of TS and ERK in gastric cancer cells.

TL;DR: Results strongly indicate that the mTOR inhibitor can enhance the potentiation of TXT and 5‐Fu or S‐1 and can serve as a new therapeutic tool for advanced and recurrent gastric cancer patients.
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Molecular Mechanisms Controlled by mTOR in Male Reproductive System

TL;DR: The latest findings concerning mTOR activity in testes, particularly its role on spermatogonial stem cell (SSC) maintenance and differentiation, as well as in the physiology of Sertoli cells (SCs), responsible for blood–testis barrier maintenance/restructuring and the nutritional support of sperMatogenesis, highlight a crucial role for mTOR in determining the male reproductive potential.
Journal ArticleDOI

Creating Diverse Target-Binding Surfaces on FKBP12: Synthesis and Evaluation of a Rapamycin Analogue Library

TL;DR: Results show that FKBP12 binds to most of the rapalogs with high affinity (K(I) values in the nanomolar to low micromolar range), creating a large repertoire of composite surfaces for potential recognition of macromolecular targets such as proteins.
References
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Journal Article

Protein Measurement with the Folin Phenol Reagent

TL;DR: Procedures are described for measuring protein in solution or after precipitation with acids or other agents, and for the determination of as little as 0.2 gamma of protein.
Journal ArticleDOI

Methods for characterization of Streptomyces species

TL;DR: The methods used by collaborators in the ISP for emendation of descriptions of type and neotype strains of the genus Streptomyces (Actinomycetales) are presented.
Journal ArticleDOI

Simplified, Accurate Method for Antibiotic Assay of Clinical Specimens

TL;DR: Serum specimens are tested directly rather than diluting them to a narrow range of antibiotic concentrations, possible because of a procedure for calculations that recognizes the curvilinear relationship between zone sizes and antibiotic concentrations.
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