摘要:
The invention discloses a direct interaction between D-type cyclins and a novel myb-like transcription factor, DMP1, which specifically interacts with cyclin D2. The present invention also provides evidence that D-type cyclins regulate gene expression in an RB-independent manner. Also included is DMP1, the transcription factor composed of a central DNA-binding domain containing three atypical myb repeats flanked by highly acidic segments located at its amino- and carboxyterminal ends. The invention includes amino acid sequences coding for DMP1, and DNA and RNA nucleotide sequences that encode the amino acid sequences. A use of DMP1 as a transcription factor is disclosed due to its specificity in binding to oligonucleotides containing the nonamer consensus sequence CCCG(G/T)ATGT. In this aspect of the invention, DMP1 when transfected into mammalian cells, activates the transcription of a reporter gene driven by a minimal promoter containing concatamerized DMP1 binding sites.
摘要:
The invention discloses a direct interaction between D-type cyclins and a novel myb-like transcription factor, DMP1, which specifically interacts with cyclin D2. The present invention also provides evidence that D-type cyclins regulate gene expression in an RB-independent manner. Also included is DMP1, the transcription factor composed of a central DNA-binding domain containing three atypical myb repeats flanked by highly acidic segments located at its amino- and carboxyterminal ends. The invention includes amino acid sequences coding for DMP1, and DNA and RNA nucleotide sequences that encode the amino acid sequences. A use of DMP1 as a transcription factor is disclosed due to its specificity in binding to oligonucleotides containing the nonamer consensus sequence CCCG(G/T)ATGT. In this aspect of the invention, DMP1 when transfected into mammalian cells, activates the transcription of a reporter gene driven by a minimal promoter containing concatamerized DMP1 binding sites.
摘要:
The invention discloses a direct interaction between D-type cyclins and a novel myb-like transcription factor, DMP1, which specifically interacts with cyclin D2. The present invention also provides evidence that D-type cyclins regulate gene expression in an RB-independent manner. Also included is DMP1, the transcription factor composed of a central DNA-binding domain containing three atypical myb repeats flanked by highly acidic segments located at its amino- and carboxyterminal ends. The invention includes amino acid sequences coding for DMP1, and DNA and RNA nucleotide sequences that encode the amino acid sequences. A use of DMP1 as a transcription factor is disclosed due to its specificity in binding to oligonucleotides containing the nonamer consensus sequence CCCG(G/T)ATGT. In this aspect of the invention, DMP1 when transfected into mammalian cells, activates the transcription of a reporter gene driven by a minimal promoter containing concatamerized DMP1 binding sites.
摘要:
Members of the InK4 (Inhibitors of CDK4) family inhibit the activities of specific cyclin D-dependent kinases (CDK4 and/or CDK6), thereby arresting cell cycle progression in G1 phase and preventing chromosomal DNA replication. Disclosed herein are novel mammalian InK4 family members, having apparent molecular masses of 18,000 and 19,000 daltons, designated "InK4c-p18" and "InK4d-p19," respectively, or simply "p18" and "p19." In particular, the invention provides p19 genes and proteins isolated from murine or human cells and p18 genes and proteins from murine cells. When constitutively expressed in cells, p19 inhibits cyclin D-dependent kinase activity in vivo and induces G1 phase arrest. Materials and methods disclosed herein include (1) nucleic acids that encode p18 or p19; (2) methods for detecting nucleic acids encoding p18 or p19 proteins; (3) methods for producing p18 or p19 proteins using nucleic acids that encode p18 or p19, respectively; (4) purified pl8 or p19 proteins and peptide fragments, oligopeptides, or fusion proteins derived therefrom; (5) methods of inhibiting cells from replicating their chromosomal DNA using purified p18 or p19 proteins or derivatives thereof; (6) antibodies that specifically bind p18 or p19; (7) methods for detecting p18 and p19 proteins; (8) methods of stimulating cell growth by blocking p18 or p19 expression via antisense oligonucleotides; (9) methods of gene therapy using nucleic acids that encode p18 or p19; and (10) methods of making transgenic non-human animals that have alterations in the gene encoding p18 or p19, or in both genes.
摘要:
A quinoxalinone derivative of the formula (I): or a pharmaceutically acceptable salt or ester thereof, wherein; X is NH, S or the like; Y is O or the like; the partial structure is, for example, the formula: B1, B2, . . . , Bn-1 and Bn, (in which n is 4, 5 or 6) are each independently CH, N or the like; B′1, B′2, . . . , B′n-1 and B′n (in which n is 4, 5 or 6) are each independently hydrogen or the like; and R is hydrogen, lower alkyl or the like.
摘要:
An MR/FIR light detector is disclosed herein that has extraordinarily high degree of sensitivity and a high speed of response. The detector includes an MR/FIR light introducing section (1) for guiding an incident MR/FIR light (2), a semiconductor substrate (14) formed with a single-electron transistor (14) for controlling electric current passing through a semiconductor quantum dot (12) formed therein, and a BOTAI antenna (6, 6a, 6b, 6c) for concentrating the MW/FIR light (2) into a small special zone of sub-micron size occupied by the semiconductor quantum dot (12) in the single-electron transistor (14). The quantum dot (12) forming a two-dimensional electron system absorbs the electromagnetic wave concentrated efficiently, and retains an excitation state created therein for 10 nanoseconds or more, thus permitting electrons of as many as one millions in number or more to be transferred with respect to a single photon absorbed.
摘要:
The invention relates to combination anticancer therapy with certain Akt inhibitor and other anticancer agents such as anticancer antimetabolites, anticancer antibiotics, plant-derived anticancer agents, anticancer platinum-coordinated complex compounds, anticancer camptothecin derivatives and anticancer tyrosine kinase inhibitors.
摘要:
The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc.The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.
摘要翻译:本发明涉及通式(I)的化合物:其中Ar1是任选取代的芳基或杂芳基; R 1是任选取代的低级烷基,低级烯基,低级炔基或环低级烷基,或者是任选具有取代基的芳基,芳烷基或杂芳基; R2是氢原子,低级烷基,低级烯基或低级炔基,或者是任选具有取代基的芳基,芳烷基或杂芳基; R3是氢原子或低级烷基; R4是氢原子,卤素原子,羟基,低级烷基或-N(R1k)R1m基团; T和U是氮原子或次甲基等。本发明的化合物具有优异的韦尔激酶抑制作用,因此可用于药物领域,特别是治疗各种癌症。
摘要:
A quinoxalinone derivative of the formula (I): or a pharmaceutically acceptable salt or ester thereof, wherein; X is NH, S or the like; Y is O or the like; the partial structure is, for example, the formula: B1, B2, . . . , Bn−1 and Bn, (in which n is 4, 5 or 6) are each independently CH, N or the like; B′1, B′2, . . . , B′n−1 and B′n (in which n is 4, 5 or 6) are each independently hydrogen or the like; and R is hydrogen, lower alkyl or the like.
摘要:
The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc. The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.
摘要翻译:本发明涉及通式(I)的化合物:其中Ar1是任选取代的芳基或杂芳基; R 1是任选取代的低级烷基,低级烯基,低级炔基或环低级烷基,或者是任选具有取代基的芳基,芳烷基或杂芳基; R2是氢原子,低级烷基,低级烯基或低级炔基,或者是任选具有取代基的芳基,芳烷基或杂芳基; R3是氢原子或低级烷基; R4是氢原子,卤素原子,羟基,低级烷基或-N(R1k)R1m基团; T和U是氮原子或次甲基等。本发明的化合物具有优异的韦尔激酶抑制作用,因此可用于药物领域,特别是治疗各种癌症。