Identification of Limonol Derivatives as Heat Shock Protein 90 (Hsp90) Inhibitors through a Multidisciplinary Approach

The identification of inhibitors of Hsp90 is currently a primary goal in the development of more effective drugs for the treatment of various types of multidrug resistant malignancies. In an attempt to identify new small molecules modulating the activity of Hsp90, we screened a small library of tetranortriterpenes. A high‐affinity interaction with Hsp90 inducible form was uncovered for eight of these compounds, five of which are described here for the first time. By monitoring the ATPase activity and the citrate synthase thermal induced aggregation, compound 1 (cedrelosin A), 3 (7α‐limonylacetate), and 5 (cedrelosin B), containing a limonol moiety, were found to be the most effective in compromising the Hsp90α chaperone activity. Consistent with these findings, the three compounds caused a depletion of c‐Raf and pAkt Hsp90 client proteins in HeLa and MCF/7 cell lines. Induced fit docking protocol and molecular dynamics were used to rationalize the structural basis of the biological activity of the limonol derivatives. Taken together, these results point to limonol‐derivatives as promising scaffolds for the design of novel Hsp90α inhibitors.     

A complete database of photoelectric and photographic multiaperture photometry of galaxies

Summary We present a complete database of photoelectric and photographic multiaperture photoelectric photometry of galaxies. The database contains all data published prior to 1991, in all standard photometric bands from UV to IR. The database contains also some global quantities as, for instance, total magnitudes and color indexes. Paper presented at the V Cosmic Physics National Conference, S. Miniato, November 27–30, 1990.     

Ki-covers. II. Ki-perfect graphs

AK_i is a complete subgraph of size i. A K_i-cover of a graph G(V, E) is a set C of K_i?1s of G such that every K_i in G contains at least one K_i?1 in C . c_i(G) is the cardinality of a smallest K_i-cover of G. A K_i-packing of G is a set of K_is such that no two K_is have i ? 1 nodes in common. p_i(G) is the cardinality of a largest K_i-packing of G. Let F _i(G) denote the set of K_is in G and define c_i(F) and p_i(F) analogously for F ? F _i(G). G is K_i-perfect if ?F ? F _i(G), c_i(F) = p_i(F). The K₂-perfect graphs are precisely the bipartite graphs. We present a characterization of K_i-perfect graphs that is similar to the Strong Perfect Graph Conjecture, and explore the relationships between K_i-perfect graphs and normal hypergraphs. Furthermore, if iA denotes the 0 ? 1 matrix of G where the rows are the elements of F _i?1(G) that belong to at least one K_i and the columns are the elements of F _i(G), then we show that iA is perfect iff G is a K_i-perfect graph. We also characterize the K_i-perfect graphs for which iAis balanced.     

Noise in optical amplifiers

This article presents an application of a recently published probablistic model for traveling wave optical amplification. Both optical signal and amplified spontaneous emission (ASE) noise are modeled as bunches of photons traveling along the amplifying region with size varying according to simple random rules. The results of the theory enable one to obtain a complete and accurate characterization of the signal and noise counting at the amplifier output. On the basis of the above statistics, we find a realistic evaluation of the limits imposed by both quantum and ASE noise on the performances of a receiver including an optical amplifier at a preamplifier stage.     

Conformational freedom of polyamide chains above the melting point

The melting behavior of diamides of general formula (n-C_pH_2p+1)CONH(CH₂)_qNHCO(nC_pH_2p+1) has been investigated by differential scanning calorimetry (DSC). The close similarity of the melting behavior of these low molar mass compounds with that of polymeric amides is discussed in terms of restricted conformational disorder in the amorphous state, due to the high degree of retention of hydrogen bonding.     

Stereocontrolled total synthesis of the chiral building block (3S,4R)-3- [(R)-1-hydroxyethyl]-4-acetyloxy-azetidin-2-one: a useful synthon for the synthesis of (+)-thienamycin,carbapenems and penems.

A total stereocontrolled synthesis of ($\text{1}$), an intermediate in the synthesis of (+)-thienamycin, carbapenems and penems, based on a strategy that uses the S(-)hydroxy ethylbutyrate as chiral building block, is reported.     

Structural and Morphological Investigation of Ce0.6Zr0.4O2 Oxides Synthesized by Sol-Gel Method: Influence of Calcination and Redox Treatments

Ceria-zirconia mixed oxides of nominal composition Ce_0.6Zr_0.4O₂ were prepared by sol-gel method. The structural and morphological modifications of these materials due to calcination and redox treatments up to 1000°C were studied by X-ray diffraction (XRD) and Rietveld refinements, specific surface area measurements (BET), oxygen storage capacity (OSC), TEM and SEM analyses. The materials maintain high OSC after several hours of treatments at 1000°C in oxidizing and reducing atmosphere, showing good resistance to the thermal ageing. An improvement of the OSC is manifested after repetitive redox cycles, even though textural characterization shows that reduction/oxidation processes induce sintering of the crystallites.