Npgrj_nchembio_94 418..424
نویسندگان
چکیده
Leucascandrolide A and neopeltolide are structurally homologous marine natural products that elicit potent antiproliferative profiles in mammalian cells and yeast. The scarcity of naturally available material has been a significant barrier to their biochemical and pharmacological evaluation. We developed practical synthetic access to this class of natural products that enabled the determination of their mechanism of action. We demonstrated effective cellular growth inhibition in yeast, which was substantially enhanced by substituting glucose with galactose or glycerol. These results, along with genetic analysis of determinants of drug sensitivity, suggested that leucascandrolide A and neopeltolide may inhibit mitochondrial ATP synthesis. Evaluation of the activity of the four mitochondrial electron transport chain complexes in yeast and mammalian cells revealed cytochrome bc1 complex as the principal cellular target. This result provided the molecular basis for the potent antiproliferative activity of this class of marine macrolides, thus identifying them as new biochemical tools for investigation of eukaryotic energy metabolism.
منابع مشابه
NF- B Family of Transcription Factors: Central Regulators of Innate and Adaptive Immune Functions
INTRODUCTION .......................................................................................................................................................414 NFB AND REGULATION OF THE IMMUNE SYSTEM ................................................................................415 Proand Antiapoptotic Functions of NFB ......................................................................
متن کاملNeurologic complications of cancer and cancer therapy.
When neurologic complications occur as a result of systemic cancer and cancer treatment, they can be more disabling for patients than their primary cancer and significantly impair functioning in varied domains. However, recognizing neurologic signs and symptoms as complications of cancer and its treatment can pose a challenge for healthcare providers. Oncology nurses must develop a high index o...
متن کاملPlasmids, drug resistance, and gene transfer in the genus Streptococcus.
INTRODUCTION .......................................................... 409 PURIFUICATION OF PLASMID DEOXYRIBONUCLEIC ACID FROM STREPTCOCCI ......................................................... 412 CONJUGATION AND PLASMID TRANSFER ......... ........................ 413 SEX PHEROMONES IN STREPTOCOCCUS FAECALIS ....... ................ 415 RESISTANCE TRANSFER IN THE ABSENCE OF PLASMID DEOXYRI...
متن کاملPhytotherapy - new developments and insights into practice.
Service 424 Latest Publications You Should Not Miss Kraft, K. (Rostock) Gesellschaftsmitteilungen 427 Schweizerische Medizinische Gesellschaft für Phytotherapie (SMGP) 430 News/Ticker 431 Tagungen und Kongresse 374 Impressum 435 Inhalt Band 21, 2014 401 Quality and Safety of Chinese Medicine Drugs in Germany – an Update Hempen, N.; Huber, R. (Freiburg i.Br.) Essay 413 An Approach to the Concept...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
دوره شماره
صفحات -
تاریخ انتشار 2008