CAS: 71800-36-7; Lys-[des-Arg9]Bradykinin

专利信息

专利号:WO-0217958-A1
优先权日:2000-08-29
标 题:Agent for influencing angiogenesis
发明人：BADER MICHAEL; PESQUERO JOAO BOSCO; MADEDDU PAOLO; EMAMUELI COSTANCA
权利人:MAX DELBRUECK CENTRUM; BADER MICHAEL; PESQUERO JOAO BOSCO; MADEDDU PAOLO; EMAMUELI COSTANCA
摘要:The invention relates to an agent for influencing angiogenesis, i.e. the new formation of blood vessels. The application areas for this agent are the medical field and the pharmaceutical industry. The aim of the invention is to discover new agents for influencing angiogenesis and to provide corresponding substances that can be used in the medical field to produce said agents. The inventive agent is characterised in that it influences angiogenesis, i.e. promotes or inhibits the latter. The promotion of angiogenesis is achieved, for example, by increasing the synthesis of the B1 receptor (transcription-mediated amplification, e.g. by cytokines), or by increasing its activity (agonistic substances). The inhibition of angiogenesis is achieved, for example, by antagonists of the kinin B1 receptor, such as des-Arg<9>-Leu<8>-bradykinin (DALBK) or non-peptide substances and by inhibiting the synthesis of the protein, e.g. using glucucorticoids.

专利号:WO-9807746-A1
优先权日:1996-08-19
标题:B1-bradykinin receptor antagonists and use thereof
发明人：REGOLI DOMENICO; PLANTE GERARD E; GOBEIL FERNAND; NEUGEBAUER WITOLD A; ZUCCOLLO ADRIANA; CATANZARO ORLANDO L
权利人:UNIV SHERBROOKE; REGOLI DOMENICO; PLANTE GERARD E; GOBEIL FERNAND; NEUGEBAUER WITOLD A; ZUCCOLLO ADRIANA; CATANZARO ORLANDO L
摘要:The present invention relates to novel antagonists to a B1-bradykinin (B1-BK) receptor which have a good affinity and selectivity therefor, some of which being at least partially resistant to enzymatic degradation. The synthesis of the B1 receptors is induced during inflammation. Symptoms associated with inflammation (elevated hydrostatic pressure and plasma leakage or extravasation) have been observed in diabetic animal models (streptozotocin-induced diabetes (STZ)) as well as in spontaneously hypertensive rats (SHR). The present inventors confirm the presence of B1-BK receptors in these two models. B1-BK antagonists abolished the vasocontraction induced by B1-BK in SHR and STZ, and reduced the glycemia of diabetic animals to normal levels. The present B1-antagonists are useful for treating any condition wherein B1-receptor is expressed, particularly during inflammation, and more particularly wherein B1-receptor expression results in diabetic vasculopathy, other diabetic symptoms associated with an insulitis and a post-capillary resistance building as a consequence of the presence of a B1-receptor.

专利号:US-11407837-B2
优先权日:2017-09-11
标 题 :GPCR binding proteins and synthesis thereof
发明人：GLANVILLE JACOB
权利人:TWIST BIOSCIENCE CORP
摘要:Provided herein are methods and compositions relating to G protein-coupled receptor (GPCR) libraries having nucleic acids encoding for a scaffold comprising a GPCR binding domain. Libraries described herein include variegated libraries comprising nucleic acids each encoding for a predetermined variant of at least one predetermined reference nucleic acid sequence. Further described herein are protein libraries generated when the nucleic acid libraries are translated. Further described herein are cell libraries expressing variegated nucleic acid libraries described herein.

专利号:US-7041785-B1
优先权日:1996-08-19
标题 :B1-bradykinin receptor antagonists and use thereof
发明人：REGOLI DOMENICO; PLANTE GERARD E; GOBEIL FERNAND; NEUGEBAUER WITOLD A; ZUCOLLO ADRIANA; CATANZARO ORLANDO L
权利人:UNIV SHERBROOKE
摘要:The present invention relates to novel antagonists to a B 1 -bradykinin (B 1 -BK) receptor which have a good affinity and selectivity therefor, some of which being at least partially resistant to enzymatic degradation. The synthesis of the B 1 receptors is induced during inflammation. Symptoms associated with inflammation (elevated hydrostatic pressure and plasma leakage or extravasation) have been observed in diabetic animal models (streptozotocin-induced diabetes (STZ)) as well as in spontaneously hypertensive rats (SHR). The present inventors confirm the presence of B 1 -BK receptors in these two models. B 1 -BK antagonists abolished the vasocontraction induced by B 1 -BK in SHR and STZ, and reduced the glycemia of diabetic animals to normal levels. The present B 1 -antagonists are useful for treating any condition wherein B 1 -receptor is expressed, particularly during inflammation, and more particularly wherein B 1 -receptor expression results in diabetic vasculopathy, other diabetic symptoms associated with an insulitis and a post-capillary resistance building as a consequence of the presence of a B 1 -receptor.