Abstract:
Described herein are silyl monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. Such multimer forming associations of monomers may be promoted by the proximal binding of the monomers to their target biomolecule(s). In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer, (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.
Abstract:
Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.
Abstract:
The invention relates to SMYD3 methyltransferase (SMYD3), SMYD3 binding pockets or SMYD3-like binding pockets. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to SMYD3 methyltransferase protein, complexes of SMYD3 methyltransferase protein, homologues thereof, or SMYD3-like protein or protein complexes.
Abstract:
The present invention provides a method for treating tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of an anticancer agent and an IGFlR inhibitor compound of Formula (I) combination, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The invention also encompasses a pharmaceutical composition that is comprised of an anticancer agent and IGFlR inhibitor compound of Formula (I) combination with a pharmaceutically acceptable carrier. The IGFl R inhibitor is represented by Formula (I): wherein X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , R 1 , and Q 1 are defined herein.
Abstract:
Compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , R 1 , and Q 1 are defined herein, inhibit kinase enzymes and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer. The compounds are also useful in the treatment of inflammation, allergy, asthma, disease and conditions of the immune system, disease and conditions of the nervous system, cardiovascular diseases, disease and conditions of the eye, dermatological diseases, osteoporosis, diabetes, multiple sclerosis, and infections.
Abstract translation:式(I)化合物及其药学上可接受的盐,其中X 1,X 2,X 3,X 4, X SUB 5,SUB 6,SUB 7,SUB 1和SUP 1 本文定义为抑制激酶,并可用于治疗和/或预防过度增殖性疾病如癌症。 这些化合物还可用于治疗炎症,变态反应,哮喘,疾病和免疫系统疾病和病症,神经系统疾病和病症,心血管疾病,眼睛疾病和病症,皮肤病,骨质疏松症,糖尿病,多发性硬化症 和感染。
Abstract:
The present invention provides compounds of Formula (I), including pharmaceutically acceptable salts and/or prodrugs thereof, where G, R 2 , and R 3 are defined as described herein.
Abstract:
Method and apparatus for converting the kinetic energy of a moving fluid stream into useful work by using a cascade of thin aero of hydro foils (2) positioned therein. The foils may be provided with at least two degrees of freedom and adjacent foils move out of phase. The foils are subjected to fluid induced oscillations known as flutter. Barriers (3, 43) may be positioned downstream, above, or at the sides of the apparatus for increasing efficiency. A system of fly wheels (17, 18) to increase inertia of the foils may be used with the hydrofoils. A cascade of aero of hydro foils may be mechanically oscillated.
Abstract:
Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer, (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.