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    • 14. 发明授权
    • Soluble recombinant αvβ3 adhesion receptor
    • 可溶性重组αv&bgr 3粘附受体
    • US08067197B2
    • 2011-11-29
    • US10460672
    • 2003-06-13
    • Simon L. GoodmanBeate DiefenbachDetelv GüssowRaj MehtaEilish CullenAlex Brown
    • Simon L. GoodmanBeate DiefenbachDetelv GüssowRaj MehtaEilish CullenAlex Brown
    • C12N15/09C07H21/04
    • C07K14/70557C12N2799/026
    • The invention relates to a novel purified recombinant αVβ3 adhesion receptor which shows an unimpaired ligand binding activity, and a process for preparing said soluble non-membrane bound receptor in excellent yields by recombinant techniques using a baculovirus-insect cell expression system. The so-synthesized soluble receptor may be used very easily as screening tool for new therapeutic compounds which may inhibit the natural αVβ3 adhesion receptor. Such therapeutic compounds which can be discovered very easily, fast and without health risk by means of the soluble receptors according to the invention may be, for example, RGD peptides or non-peptidic compounds mimicking the natural ligand epitopes. The invention relates, furthermore, to a corresponding process for preparing recombinant full-length αVβ3 adhesion receptor in excellent yields, additionally using detergents to dissolve the membrane bound receptor from the surface of the host cell.
    • 本发明涉及一种新型纯化的重组αVb-3粘附受体,其显示出未受损的配体结合活性,以及​​通过使用杆状病毒 - 昆虫细胞表达系统的重组技术以优异的产率制备所述可溶性非膜结合受体的方法。 如此合成的可溶性受体可以非常容易地用作可能抑制天然αV和bgr 3粘附受体的新的治疗化合物的筛选工具。 可以通过本发明的可溶性受体非常容易,快速且没有健康风险发现的这种治疗化合物可以是例如RGD肽或模仿天然配体表位的非肽化合物。 此外,本发明还涉及以优异的产率制备重组全长αV&bgr 3粘附受体的相应方法,另外使用洗涤剂从宿主细胞表面溶解膜结合受体。
    • 15. 发明授权
    • Cyclic adhesion inhibitors
    • 环状粘连抑制剂
    • US6001961A
    • 1999-12-14
    • US694387
    • 1996-09-16
    • Alfred JonczykSimon GoodmanBeate DiefenbachArne SutterGunter HolzemannHorst KesslerMichael Dechantsreiter
    • Alfred JonczykSimon GoodmanBeate DiefenbachArne SutterGunter HolzemannHorst KesslerMichael Dechantsreiter
    • A61K38/00A61K38/04A61K38/12A61P9/00A61P31/04A61P35/00A61P35/04A61P39/00A61P43/00C07K1/113C07K7/64C07K7/00
    • C07K7/64A61K38/00
    • The invention relates to novel cyclopeptides of the formula Icyclo-(nArg-nGly-nAsp-nD-nE) I,in whichD and E in each case independently of one another are Gly, Ala, .beta.-Ala, Asn, Asp, Asp(OR), Arg, Cha, Cys, Gln, Glu, His, Ile, Leu, Lys, Lys(Ac), Lys(AcNH.sub.2), Lys(AcSH), Met, Nal, Nle, Orn, Phe, 4-Hal-Phe, homo-Phe, Phg, Pro, Pya, Ser, Thr, Tia, Tic, Trp, Tyr or Val, which amino acid residues can also be derivatized,R is alkyl having 1-18 carbon atoms,Hal is F, Cl, Br, I,Ac is alkanoyl having 1-10 carbon atoms, aroyl having 7-11 carbon atoms or aralkanoyl having 8-12 carbon atoms,n denotes no substituent or an alkyl radical R, benzyl or an aralkyl radical having 7-18 carbon atoms on the alpha-amino function of the relevant amino acid residue,with the proviso that at least one amino acid residue has a substituent n and that, where residues of optically active amino acids and amino acid derivatives are involved, both the D and the L forms are included, and also their physiologically acceptable salts.These compounds act as integrin inhibitors and can be used in particular for the prophylaxis and treatment of disorders of the circulation, angiogenic disorders, microbial infections and in tumor therapy.
    • 本发明涉及式I环 - (nArg-nGly-nAsp-nD-nE)I的新型环肽,其中D和E各自独立地为Gly,Ala,β-Ala,Asn,Asp,Asp (OR),Arg,Cha,Cys,Gln,Glu,His,Ile,Leu,Lys,Lys(Ac),Lys(AcNH 2),Lys(AcSH),Met,Nal,Nle,Orn, -Phe,Phe-Phe,Phg,Pro,Pya,Ser,Thr,Tia,Tic,Trp,Tyr或Val,该氨基酸残基也可被衍生化,R是具有1-18个碳原子的烷基,Hal是F, Cl,Br,I,Ac是具有1-10个碳原子的烷酰基,具有7-11个碳原子的芳酰基或具有8-12个碳原子的芳烷酰基,n表示没有取代基或烷基R,苄基或具有7- 相关氨基酸残基的α-氨基官能团上的18个碳原子,条件是至少一个氨基酸残基具有取代基n,并且当涉及光学活性氨基酸和氨基酸衍生物的残基时,D 并且包括L形式,也包括它们的生理学 可接受的盐。 这些化合物用作整联蛋白抑制剂,特别可用于预防和治疗循环障碍,血管生成障碍,微生物感染和肿瘤治疗。