Calphostins, novel and specific inhibitors of protein kinase C. II. Chemical structures.

نویسندگان

  • T Iida
  • E Kobayashi
  • M Yoshida
  • H Sano
چکیده

The structures of new antitumor antibiotics, calphostins (UCN-1028) A, B, C, D and I, which are specific and potent inhibitors of protein kinase C, were determined by spectral and chemical studies. All of the antibiotics have a 3,10-perylenequinone skeleton and calphostin D was revealed to be an antipode of isophleichrome.

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Calphostins (UCN-1028), novel and specific inhibitors of protein kinase C. I. Fermentation, isolation, physico-chemical properties and biological activities.

A novel complex of calphostin (UCN-1028), which specifically inhibits protein kinase C (PKC) has been isolated from the culture broth of a fungi Cladosporium cladosporioides. Purification of individual components was carried out by silica gel, non-porus resin Diaion HP-20SS and Sephadex LH-20 chromatography, leading to isolation of five closely related components. A, B, C, D and I. Calphostins ...

متن کامل

Rho Kinase Inhibitors as a Novel Treatment for Glaucoma and Ocular Hypertension

In an elegant example of bench-to-bedside research, a hypothesis that cells in the outflow pathway actively regulate conventional outflow resistance was proposed in the 1990s and systematically pursued, exposing novel cellular and molecular mechanisms of intraocular pressure (IOP) regulation. The critical discovery that pharmacologic manipulation of the cytoskeleton of outflow pathway cells dec...

متن کامل

Activation of calcium/calmodulin-dependent kinase II following bovine rotavirus enterotoxin NSP4 expression

Objective(s): The rotavirus nonstructural protein 4 (NSP4) is responsible for the increase in cytoplasmic calcium concentration through a phospholipase C-dependent and phospholipase C-independent pathways in infected cells. It is shown that increasing of intracellular calcium concentration in rotavirus infected cells is associated with the activation of some members of protein kinases family su...

متن کامل

Synthesis, Characterization, and Theoretical Studies of the New Antibacterial Zn(II) Complexes from New Fluorescent Schiff Bases Prepared by imidazo[4',5':3,4]benzo[1,2-c]isoxazole

The novel fluorescentheterocyclic bidentate ligands have been synthesized by the high yields reaction of 8-(4-chlorophenyl)-3-Iso-butyl-3H-imidazo[4',5':3,4]benzo[1,2-c]isoxazol-5-amine with p-hydroxybenzaldehyde and p-chlorobenzaldehyde. The ligands reacted with Zn(II) ion to gained novel complexes. The optical properties of these structures were checked and the outcomes represented that t...

متن کامل

Application of 3D-QSAR on a Series of Potent P38-MAP Kinase Inhibitors

One of the most applied methods in drug industry for development of new drugs is 3D-QSAR methodology. As p38-mitogen-activated protein kinase (p38-MAPK) plays a crucial role in regulating the production of such proinflammatory cytokines as tumor necrosis factor-α (TNF-α) and interleukin-1, emerging as an attractive target for new anti-inflammatory agents, we used a 3D-QSAR based method of Compa...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:
  • The Journal of antibiotics

دوره 42 10  شماره 

صفحات  -

تاریخ انتشار 1989