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Resorcylic acid lactones: naturally occurring potent and selective inhibitors of MEK.
A resorcylic acid lactone, L-783,277, isolated from a Phoma sp. (ATCC 74403) which came from the fruitbody of Helvella acetabulum, is a potent and specific inhibitor of MEK (Map kinase kinase).…
L-696,474, a novel cytochalasin as an inhibitor of HIV-1 protease. III. Biological activity.
A novel cytochalasin with a molecular weight of 477 and an empirical formula of C30H39NO4 inhibited HIV-1 protease activity with an IC50 of 3 microM and the mode of inhibition was competitive with respect to substrate (apparent Ki = 1 microM).
Estrogen regulation of epidermal growth factor receptor messenger ribonucleic acid.
It is reported that the increase in uterine EGF receptor levels is due to an increase in the steady-state levels of EGF receptors mRNA in vivo, and this results indicate that E2 regulates the level of E GF receptor by increasing the Steady-state concentration ofEGF receptor RNA in vivo.
Durhamycin A, a potent inhibitor of HIV Tat transactivation.
- H. Jayasuriya, R. Lingham, +9 authors Sheo B. Singh
- Biology, MedicineJournal of natural products
- 4 July 2002
Durhamycin A was discovered as a potent inhibitor (IC(50) = 4.8 nM) of Tat transactivation of HIV transactivation in efforts to discover Tat inhibitors from natural product screening of microbial fermentation extracts.
Selective inhibition of farnesyl-protein transferase blocks ras processing in vivo.
- J. Gibbs, D. Pompliano, +6 authors A. Oliff
- Chemistry, MedicineThe Journal of biological chemistry
- 15 April 1993
These results are the first demonstration that a small organic chemical selected for inhibition of FPTase can inhibit Ras processing in vivo.
Inhibitors of farnesylation of Ras from a microbial natural products screening program
- D. Vilella, Manuel Sánchez, +11 authors F. Peláez
- Biology, MedicineJournal of Industrial Microbiology and…
- 1 December 2000
Ten different families of compounds are identified, all of which selectively inhibit FPTase with a variety of mechanisms, which originated from the fermentations of a number of microorganisms, either actinomycetes or fungi, isolated from different substrates collected in tropical and temperate areas.
Optimization of erythropoietin production with controlled glycosylation-PEGylated erythropoietin produced in glycoengineered Pichia pastoris.
The expression of recombinant human erythropoietin (rhEPO) in glycoengineered P. pastoris is reported, yielding an active biologic that is comparable to those produced in current mammalian host systems.
Four novel bis-(naphtho-γ-pyrones) isolated from Fusarium species as inhibitors of HIV-1 integrase
Abstract Integration of viral DNA into host cell DNA is an essential step in retroviral (HIV-1) replication and is catalyzed by HIV-1 integrase. HIV-1 integrase is a novel therapeutic target and is…
Hinnuliquinone, a C2-symmetric dimeric non-peptide fungal metabolite inhibitor of HIV-1 protease.
- Sheo B. Singh, J. Ondeyka, +9 authors R. Lingham
- Biology, MedicineBiochemical and biophysical research…
- 5 November 2004
Screening of microbial extracts followed by bioassay-guided isolation led to the discovery of a natural hinnuliquinone, a C(2)-symmetric bis-indolyl quinone natural product that inhibited the wild-type and a clinically resistant (A44) strain of HIV-1 protease.
Clavaric acid and steroidal analogues as Ras- and FPP-directed inhibitors of human farnesyl-protein transferase.
We have identified a novel fungal metabolite that is an inhibitor of human farnesyl-protein transferase (FPTase) by randomly screening natural product extracts using a high-throughput biochemical…