keyword
MENU ▼
Read by QxMD icon Read
search

Sudemycin

keyword
https://www.readbyqxmd.com/read/27371337/retracted-article-complex-effect-of-rna-spliceosome-inhibition-on-amyloid-precursor-protein-expression
#1
Ning Zhang, Ling He, Helin Feng, Yan Kong, Jin Wang, Jinming Zhang
No abstract text is available yet for this article.
December 2016: Neurochemical Research
https://www.readbyqxmd.com/read/26171237/pharmacodynamic-assays-to-facilitate-preclinical-and-clinical-development-of-pre-mrna-splicing-modulatory-drug-candidates
#2
Yihui Shi, Amanda S Joyner, William Shadrick, Gustavo Palacios, Chandraiah Lagisetti, Philip M Potter, Lidia C Sambucetti, Stefan Stamm, Thomas R Webb
The spliceosome has recently emerged as a new target for cancer chemotherapy and novel antitumor spliceosome targeted agents are under development. Here, we describe two types of novel pharmacodynamic assays that facilitate drug discovery and development of this intriguing class of innovative therapeutics; the first assay is useful for preclinical optimization of small-molecule agents that target the SF3B1 spliceosomal protein in animals, the second assay is an ex vivo validated, gel-based assay for the measurement of drug exposure in human leukocytes...
August 2015: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/26068951/the-splicing-modulator-sudemycin-induces-a-specific-antitumor-response-and-cooperates-with-ibrutinib-in-chronic-lymphocytic-leukemia
#3
Sílvia Xargay-Torrent, Mónica López-Guerra, Laia Rosich, Arnau Montraveta, Jocabed Roldán, Vanina Rodríguez, Neus Villamor, Marta Aymerich, Chandraiah Lagisetti, Thomas R Webb, Carlos López-Otín, Elias Campo, Dolors Colomer
Mutations or deregulated expression of the components of the spliceosome can influence the splicing pattern of several genes and contribute to the development of tumors. In this context, we report that the spliceosome modulator sudemycin induces selective cytotoxicity in primary chronic lymphocytic leukemia (CLL) cells when compared with healthy lymphocytes and tumor cells from other B-lymphoid malignancies, with a slight bias for CLL cases with mutations in spliceosome-RNA processing machinery. Consistently, sudemycin exhibits considerable antitumor activity in NOD/SCID/IL2Rγ-/- (NSG) mice engrafted with primary cells from CLL patients...
September 8, 2015: Oncotarget
https://www.readbyqxmd.com/read/25519886/htlv-1-infected-cd4-t-cells-display-alternative-exon-usages-that-culminate-in-adult-t-cell-leukemia
#4
Morgan Thénoz, Céline Vernin, Hussein Mortada, Maroun Karam, Christiane Pinatel, Antoine Gessain, Thomas R Webb, Didier Auboeuf, Eric Wattel, Franck Mortreux
BACKGROUND: Reprogramming cellular gene transcription sustains HTLV-1 viral persistence that ultimately leads to the development of adult T-cell leukemia/lymphoma (ATLL). We hypothesized that besides these quantitative transcriptional effects, HTLV-1 qualitatively modifies the pattern of cellular gene expression. RESULTS: Exon expression analysis shows that patients' untransformed and malignant HTLV-1(+) CD4(+) T-cells exhibit multiple alternate exon usage (AEU) events...
2014: Retrovirology
https://www.readbyqxmd.com/read/24623796/sudemycin-e-influences-alternative-splicing-and-changes-chromatin-modifications
#5
Paolo Convertini, Manli Shen, Philip M Potter, Gustavo Palacios, Chandraiah Lagisetti, Pierre de la Grange, Craig Horbinski, Yvonne N Fondufe-Mittendorf, Thomas R Webb, Stefan Stamm
Sudemycin E is an analog of the pre-messenger RNA splicing modulator FR901464 and its derivative spliceostatin A. Sudemycin E causes the death of cancer cells through an unknown mechanism. We found that similar to spliceostatin A, sudemycin E binds to the U2 small nuclear ribonucleoprotein (snRNP) component SF3B1. Native chromatin immunoprecipitations showed that U2 snRNPs physically interact with nucleosomes. Sudemycin E induces a dissociation of the U2 snRNPs and decreases their interaction with nucleosomes...
April 2014: Nucleic Acids Research
https://www.readbyqxmd.com/read/24325474/optimization-of-antitumor-modulators-of-pre-mrna-splicing
#6
Chandraiah Lagisetti, Gustavo Palacios, Tinopiwa Goronga, Burgess Freeman, William Caufield, Thomas R Webb
The spliceosome regulates pre-mRNA splicing, which is a critical process in normal mammalian cells. Recently, recurrent mutations in numerous spliceosomal proteins have been associated with a number of cancers. Previously, natural product antitumor agents have been shown to interact with one of the proteins that is subject to recurrent mutations (SF3B1). We report the optimization of a class of tumor-selective spliceosome modulators that demonstrate significant in vivo antitumor activity. This optimization culminated in the discovery of sudemycin D6, which shows potent cytotoxic activity in the melanoma line SK-MEL-2 (IC50 = 39 nM) and other tumor cell lines, including JeKo-1 (IC50 = 22 nM), HeLa (IC50 = 50 nM), and SK-N-AS (IC50 = 81 nM)...
December 27, 2013: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/21531567/radiosynthesis-of-antitumor-spliceosome-modulators
#7
Tinopiwa Goronga, Vincent A Boyd, Chandraiah Lagisetti, Cynthia Jeffries, Thomas R Webb
A set of novel antitumor agents (the sudemycins) has recently been described that are analogs of the natural product FR901464. We report the radiosynthesis of two of these antitumor drug lead compounds, using a three step procedure: (1) ester hydrolysis, (2) Lindlar's catalyst/tritium gas to give a (S,Z)-4-acetoxypent-2-enoic acid derivative, and finally (3) amide bond formation. These labeled analogs are useful in developing a better understanding of the pharmacological properties of this new class of therapeutic lead compounds...
September 2011: Applied Radiation and Isotopes
https://www.readbyqxmd.com/read/21344922/sudemycins-novel-small-molecule-analogues-of-fr901464-induce-alternative-gene-splicing
#8
Liying Fan, Chandraiah Lagisetti, Carol C Edwards, Thomas R Webb, Philip M Potter
Two unrelated bacterial natural products, FR901464 and pladienolide B, have previously been shown to have significant antitumor activity in vivo. These compounds target the SF3b subunit of the spliceosome, with a derivative of pladienolide (E7107) entering clinical trials for cancer. However, due to the structural complexity of these molecules, their research and development has been significantly constrained. We have generated a set of novel analogues (Sudemycins) that possess the pharmacophore that is common to FR901464 and pladienolide, via a flexible enantioselective route, which allows for the production of gram quantities of drug...
June 17, 2011: ACS Chemical Biology
1
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"