Naturalproductman’s Blog

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Archive for the ‘Protein Targets’ Category

Dibefurin synthesis

Posted by naturalproductman on November 8, 2014

Dirk Trauner and co-workers have reported in ACIE on the synthesis of dibefurin.

dibefurin

ACIE paper

Posted in Protein Targets, Total Synthesis | Leave a Comment »

Leiodermatolide synthesis

Posted by naturalproductman on October 28, 2014

Furstner and colleagues have reported in JACS on the synthesis of leiodermatolide.

leiodermatolide

JACS paper

Posted in Cancer, P-glycoprotein, Protein Targets, Total Synthesis | Leave a Comment »

Amdigenols E and G

Posted by naturalproductman on October 25, 2014

Toshiyasu Inuzuka and co-workers from Gifu University have reported in Tetrahedron Letters on the isolation of amdigenols E and G from dinoflagellates, and they had activity against N-type Ca2+ channel opening.
amdigenols E and G

TL paper

Posted in Polyketides, Protein Targets | Leave a Comment »

1-Alaninechlamydocin

Posted by naturalproductman on July 15, 2014

Robert Cichewicz and co-workers from the University of Oklahoma have reported in the Journal of Natural Products on the isolation of a tetrapeptide with HDAC inhibitory activity. This compound was isolated from a fungus in Lake Superior.

peptide

JNP paper

Posted in Cancer, Histone deacetylase, Peptides, Protein Targets | Leave a Comment »

So they made the trophy target, now what?

Posted by naturalproductman on May 29, 2014

Did you ever wonder what happened to palau’amine after they synthesized it? Was it the end of the story there? Well they did publish in the Journal of Natural Products in 2012 on the target of palau’amine and it was an inhibitor for the human 20S proteasome. You may wonder what the proteasome does:  it just degrades proteins (broken down or not needed) through proteolysis. Is that exciting? Well that may be a subjective question. It may be like saying is Coke delicious?

 

JNP paper

 

Posted in Alkaloids, Chemical Biology, Elucidation of natural product bioactivity, Protein Targets | Leave a Comment »

Swinhoeisterol

Posted by naturalproductman on April 3, 2014

Wen Zhang and co-workers from Second Military Medical University in China have reported in Organic Letters on the isolation of swinhoeisterol.
swinhoeisterol

OL paper

Posted in Protein Targets, Seven-Membered Rings, Steroids | Leave a Comment »

Bcl-XL and Bcl-2 interaction

Posted by naturalproductman on April 5, 2013

Thorsten Berg and co-workers at the University of Leipzig have reported in ACIE on the study of some small molecules disrupting the interaction of Bcl-XL and Bcl-2.

apoptosis

ACIE paper

Posted in Protein Targets, Proteins, Receptors | Leave a Comment »

Vegfrecine

Posted by naturalproductman on February 22, 2013

Hayamitsu Adachi and co-workers from BIKAKEN have reported in JNP on a novel VEGF receptor tyrosine kinase inhibitor from bacteria. The only problem I see with this compound – from a toxicologist’s perspective – is that this is a quinone, and thus a very reactive electrophile. If this kind of functional group is used as a drug, who knows what other things it will react with in the body – be it DNA, proteins, etc…
vegfrecine

JNP paper

Posted in Alkaloids, Enzymes, Protein Targets, Proteins | Leave a Comment »

Asperterpenoid A

Posted by naturalproductman on January 31, 2013

Zhigang She and co-workers from Sun-Yat Sen University have reported in Organic Letters on the isolation of asperterpenoid A, which had an IC50 value of 2.2 micromolar against Mycobacterium tuberculosis protein tyrosine phosphatase B (mPTPB).

ABCDE

OL paper

Posted in Protein Targets, protein tyrosine phosphatase 1B (PTP1B), Terpenoids | Leave a Comment »

Siladenoserinols

Posted by naturalproductman on December 29, 2012

Sachiko Tsukamoto and co-workers from Kumamoto University have reported in Organic Letters on the isolation of siladenoserinols A-L, which had inhibitory activity against p53 and HDM2 interaction.

interaction

OL paper

Posted in Cancer, p53, Protein Targets | Leave a Comment »

 
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