Abstract:
The invention consists substantially of combinatorial, protein-marker molecule libraries, having groups that may be chemically and photochemically activated, with or without reporter groups, connected in different diversity points or spatial arrangements via side chains around a common molecular core. The invention consists furthermore of combinatorial libraries of marker units having chemically or photochemically reactive marker groups, reporter groups, and various other types of side chains attached variably to a common molecular, preferably lysine-based, structural core. The invention consists furthermore of a method for combinatorial chemical tethering, where a side chain having a terminal functional group, preferably an amino group, and to which a marker group is optionally attached, is introduced in optimal position ensuring structural diversity and protein binding effectiveness. The invention contributes to simplifying complexity of proteome in different tissues and to the identification of protein markers for diagnosis by alternating different labeling pattern in healthy and diseased tissues.
Abstract:
The chromatography purification system (10) for automated chromatography separation of a plurality of different components in a sample and collection the fraction of at least one target component comprises a fluid streaming unit (11), a chromatography column (12) for receiving a sample and separating the components of the sample, a sample injection valve (18) for injecting the sample, a detector (14) coupled to the chromatography column (12) for receiving the sample and outputting a signal indicating the presence of at least one component in the sample flowing through it, a waste reservoir (17), a fraction collector (16) for dispensing the collected fractions into fraction containers and a system controller (20) for controlling the operation of the fluid streaming unit (11) and the fraction collector (16). The system further comprises a selector (22) for receiving the sample from the detector (14), selecting a predetermined number of target components with a predetermined property from the at least one component of the sample, directing the fraction of the at least one selected target component to the fraction collector (16) and discharging the remaining part of the sample into the waste reservoir (17).
Abstract:
Compounds inhibiting phosphatidylinositol 3-kinase (PI 3-K) activities and methods of preparing and using thereof in treating diseases are disclosed. Compounds inhibiting PI 3-K activity and methods of using PI 3-K inhibitory compounds to inhibit cancer cell grwoth or to treat disorders of immunity and inflammation, in which PI 3-K plays a role in leukocyte function are also provided.
Abstract translation:公开了抑制磷脂酰肌醇3-激酶(PI 3-K)活性的化合物及其制备和用于治疗疾病的方法。 还提供了抑制PI3-K活性的化合物和使用PI3-K抑制性化合物抑制癌细胞生长或治疗免疫和炎症疾病的方法,其中PI3-K在白细胞功能中起作用。 p >
Abstract:
The invention consists substantially of combinatorial, protein-marker molecule libraries, having groups that may be chemically and photochemically activated, with or without reporter groups, connected in different diversity points or spatial arrangements via side chains around a common molecular core. The invention consists furthermore of combinatorial libraries of marker units having chemically or photochemically reactive marker groups, reporter groups, and various other types of side chains attached variably to a common molecular, preferably lysine-based, structural core. The invention consists furthermore of a method for combinatorial chemical tethering, where a side chain having a terminal functional group, preferably an amino group, and to which a marker group is optionally attached, is introduced in optimal position ensuring structural diversity and protein binding effectiveness. The invention contributes to simplifying complexity of proteome in different tissues and to the identification of protein markers for diagnosis by alternating different labeling pattern in healthy and diseased tissues.
Abstract:
Compounds inhibiting phosphatidylinositol 3-kinase (PI 3-K) activities and methods of preparing and using thereof in treating diseases are disclosed. Compounds inhibiting PI 3-K activity and methods of using PI 3-K inhibitory compounds to inhibit cancer cell growth or to treat disorders of immunity and inflammation, in which PI 3-K plays a role in leukocyte function are also provided.
Abstract:
Compounds inhibiting phosphatidylinositol 3-kinase (PI 3-K) activities and methods of preparing and using thereof in treating diseases are disclosed. Compounds inhibiting PI 3-K activity and methods of using PI 3-K inhibitory compounds to inhibit cancer cell growth or to treat disorders of immunity and inflammation, in which PI 3-K plays a role in leukocyte function are also provided.
Abstract:
This invention involves a small hybrid sheet (chip), used to miniaturize chemical, biochemical, and biological processes, characterized by that it consists of mono or multilayer sheet (chip) comprising the following directly connected units: a) a unit used for synthesis and work-up of compounds and the transport of raw materials, reagents, and final products; b) a unit used for the analysis of compounds and transport of raw materials, reagents, and final products; c) a unit used for execution of biological assays of compounds and the transport of raw materials, reagents, and final products; and d) preferably an electronic unit, more preferably a semi conductor chip into which the following have been burnt: (i) the software source code of at least one computer program for the realization of a function algorithm between biological activity and the chemical structure of compounds; whose input is the chemical structure and biological activity of one or more compounds, and whose output is the chemical structure(s) of one or more further compounds likely to display the desired degree of biological activity, (ii) the software source code of a synthesis program whose input is the chemical formula(e) of one or more compounds obtained as the output of part (i), and whose output provides the laboratory synthesis protocols for these compounds (iii) the software source code of a control program whose input is the one or more laboratory synthesis protocols obtained as the output of the previous step (ii), and whose output provides the control program for the unit described in subsection a). (iv) and finally, preferably the software source code of a control program that controls the operation of the units described under subsections (a) through (d), including launch, shut down, and optimization of these units, preferably the software source code of a control program that controls the biological assay by means of a threshold to be attained during the assay. The small hybrid sheet (chip) may be applied to the production, analysis, and assay of biologically active compounds, and to the measurement of their metabolism, toxicity, and other adaptable biological interactions.
Abstract:
Compounds inhibiting phosphatidylinositol 3-kinase (PI 3-K) activities and methods of preparing and using thereof in treating diseases are disclosed. Compounds inhibiting PI 3-K activity and methods of using PI 3-K inhibitory compounds to inhibit cancer cell grwoth or to treat disorders of immunity and inflammation, in which PI 3-K plays a role in leukocyte function are also provided.
Abstract:
The subject of the invention is a method for production of an active solid support suitable for anchoring drug molecules through covalent bonds, using the following methods a.) a solid support prepared in advance, preferably by pre-treatment in the presence of strong bases or acids, then reacted with a polyamine-functionalized alcoxy-silane derivative, preferably 3-[2-(2-aminoethylamino)ethylamino]propyl trimethoxy-silane, followed by washing and drying, b1) the solid support obtained in the procedure described above in Section a.) will be reacted with (I) where Z: = bond or a -CO or -CNR 1 group and group 121 is an alkyl, aralkyl or aryl group; B: = bond or a - (CH 2 ) n - or -(CH 2 ) n O-(CH 2 ) n or O - (CH 2 ) n - or -NH(CH 2 ) n - group; A: = a branched or unbranched alkyl or substituted aryl or aralkyl group containing 1-5 carbon atoms; D: = a halogen or -O-A group and n = 0, 1, 2, ... integer - with a bi-functional reagent, preferably reacted with acryloyl/chloride or 1,4-butanediol diacrylate in the presence of an organic or inorganic scavenger or b2) the support prepared using the method described in part (a) is reacted with a bi-functional reagent, preferably 1,4-butanediol diglicidyl-ether or epichlorohydrin, in the presence of an organic or inorganic scavenger containing terminal epoxy groups and an amino-group reactive functional subgroup. The invention also includes the active solid support produced using the several methods described above, as well as application of the active solid support described above for production of chemical microarrays and combinatorial chemical microarrays. The invention further comprises a method for immobilization of what have been termed organic molecules of low molecular weight, having a size less than 1500 Da, preferably between 250 and 750 Da. This is achieved by anchoring an unmodified drug or drug candidate molecule to the active solid support described above by adding the appropriate functional groups of the drug or drug candidate molecule, preferably executed using a micron-sized robotized binding technique.
Abstract:
The subject of the invention is a method for production of an active solid support suitable for anchoring drug molecules through covalent bonds, using the following methods a.) a solid support prepared in advance, preferably by pre-treatment in the presence of strong bases or acids, then reacted with a polyamine-functionalized alcoxy-silane derivative, preferably 3-[2-(2-aminoethylamino)ethylamino]propyl trimethoxy-silane, followed by washing and drying, b1) the solid support obtained in the procedure described above in Section a.) will be reacted with (I) where Z: = bond or a -CO or -CNR 1 group and group 121 is an alkyl, aralkyl or aryl group; B: = bond or a - (CH 2 ) n - or -(CH 2 ) n O-(CH 2 ) n or O - (CH 2 ) n - or -NH(CH 2 ) n - group; A: = a branched or unbranched alkyl or substituted aryl or aralkyl group containing 1-5 carbon atoms; D: = a halogen or -O-A group and n = 0, 1, 2, ... integer - with a bi-functional reagent, preferably reacted with acryloyl/chloride or 1,4-butanediol diacrylate in the presence of an organic or inorganic scavenger or b2) the support prepared using the method described in part (a) is reacted with a bi-functional reagent, preferably 1,4-butanediol diglicidyl-ether or epichlorohydrin, in the presence of an organic or inorganic scavenger containing terminal epoxy groups and an amino-group reactive functional subgroup. The invention also includes the active solid support produced using the several methods described above, as well as application of the active solid support described above for production of chemical microarrays and combinatorial chemical microarrays. The invention further comprises a method for immobilization of what have been termed organic molecules of low molecular weight, having a size less than 1500 Da, preferably between 250 and 750 Da. This is achieved by anchoring an unmodified drug or drug candidate molecule to the active solid support described above by adding the appropriate functional groups of the drug or drug candidate molecule, preferably executed using a micron-sized robotized binding technique.