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Distinct tRNA Accommodation Intermediates Observed on the Ribosome with the Antibiotics Hygromycin A and A201A.
Aminoethylenes: a tetrahedral intermediate isostere yielding potent inhibitors of the aspartyl protease BACE-1.
The AE isostere class represents a promising advance in the development of BACE-1 inhibitors, and possesses enzymatic and cell assay IC(50)s of 26 nM and 180 nM, respectively.
Novel Pactamycin Analogs Induce p53 Dependent Cell-Cycle Arrest at S-Phase in Human Head and Neck Squamous Cell Carcinoma (HNSCC) Cells
It is demonstrated that pactamycin analogs TM-025 and TM-026 induce senescence and inhibit proliferation of HNSCC cells via accumulation in S-phase through possible contribution of p53.
Capillary electrophoresis: novel tool for simmondsins analysis and its application to jojoba breeding
Biosynthetic studies and genetic engineering of pactamycin analogs with improved selectivity toward malarial parasites.
Deciphering Pactamycin Biosynthesis and Engineered Production of New Pactamycin Analogues
- Takuya Ito, N. Roongsawang, T. Mahmud
- Biology, ChemistryChembiochem : a European journal of chemical…
- 4 September 2009
Pactamycin is an aminocyclopentitol‐derived natural product that has potent antibacterial and antitumor activities. Sequence analysis of an 86 kb continuous region of the chromosome from Streptomyces…
Fragment-based discovery of nonpeptidic BACE-1 inhibitors using tethering.
The ABP ligands represent a new type of nonpeptidic Bace-1 inhibitor motif that has not been described in the aspartyl protease literature and may serve as a starting point for the development of BACE-1-directed Alzheimer's disease therapeutics.
Elucidation of Final Steps of the Marineosins Biosynthetic Pathway through Identification and Characterization of the Corresponding Gene Cluster
- S. Salem, P. Kancharla, G. Florova, Shweta Gupta, Wanli Lu, K. Reynolds
- Chemistry, BiologyJournal of the American Chemical Society
- 27 February 2014
This work presents the first experimentally supported scheme for biosynthesis of marineosin and provides a new biologically active molecule, premarineosin.
Mutasynthesis of fluorinated pactamycin analogues and their antimalarial activity.
- K. H. Almabruk, Wanli Lu, Yuexin Li, Mostafa Abugreen, J. X. Kelly, T. Mahmud
- Chemistry, BiologyOrganic letters
- 22 March 2013
A mutasynthetic strategy has been used to generate fluorinated TM-025 and TM-026, two biosynthetically engineered pactamycin analogues produced by Streptomyces pactum ATCC 27456, providing insights into the biosynthesis of 3-aminobenzoic acid in S. pactum.
Stereospecific Synthesis of 23-Hydroxyundecylprodiginines and Analogues and Conversion to Antimalarial Premarineosins via a Rieske Oxygenase Catalyzed Bicyclization
- P. Kancharla, Wanli Lu, S. Salem, J. X. Kelly, K. Reynolds
- Chemistry, BiologyThe Journal of organic chemistry
- 7 November 2014
This study presents the first example of oxidative bicyclization mediated by a Rieske oxygenase, a key step in the tailoring process of the biosynthesis of marineosins, using a marG heterologous expression system.