Naturalproductman’s Blog

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Archive for the ‘Enzymes’ Category

Cyclopropanation with iron(III) phthalocyanine

Posted by naturalproductman on May 2, 2015

Emily Balskus and colleague have reported in ACIE on an iron(III) phthalocyanine catalyst that can perform cyclopropanation reactions. Reminds me of the P450 version that was published a few years back.

cyclopropanation
ACIE paper

Posted in Enzymes, Iron, Methodology, Transition Metal | Leave a Comment »

Penitrem biosynthesis

Posted by naturalproductman on April 12, 2015

Hideaki Oikawa and co-workers at Hokkaido University have reported in ACIE on the enzymatic biosynthesis of penitrem.

alkaloid

ACIE paper

Posted in Biosynthesis, Cyclobutanes, Diterpene, Enzymes, Indoles | Leave a Comment »

Corvol ethers A and B biosynthesis

Posted by naturalproductman on March 25, 2015

Jeroen Dickschat and co-workers at Technische Universität Braunschweig have reported in ACIE on some terpene biosynthesis by characterizing a sesquiterpene cyclase enzyme.

terpene
ACIE paper

Posted in Biosynthesis, Enzymes, Sesquiterpenes | Leave a Comment »

Terpene cyclization involving carbons switching

Posted by naturalproductman on March 5, 2015

Tomohisa Kuzuyama and co-workers at the University of Tokyo have reported in ACIE on an mechanistically interesting terpene cyclization involving two carbons switching.

terpene

ACIE paper

Posted in Biosynthesis, Enzymes, Mechanistic, Proteins | Leave a Comment »

Cycloclavine biosynthesis

Posted by naturalproductman on March 5, 2015

Sarah O’Connor and co-workers from the John Innes Centre in the UK have reported in ACIE on the biosynthesis of cycloclavine.

cycloclavine

ACIE paper

Posted in Alkaloids, Biosynthesis, Enzymatic, Enzymes, Methodology | 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 »

Not just isolating small molecules anymore…

Posted by naturalproductman on January 17, 2013

Hideaki Oikawa and co-workers from Hokkaido University have reported in Organic Letters on the isolation of an enzyme that was known to produce some natural products. They expressed and purified the enzyme, incubated the enzyme in the presence of substrates:  geranyl diphosphate (GPP) and isopentenyl diphosphate (IPP), and examined the products.

sesterterpene synthase

OL paper

Posted in Chemical Biology, Enzymes, Methodology, Proteins, Sesterterpenes | Leave a Comment »

HIV-1 reverse transcriptase structure with catechol diether

Posted by naturalproductman on November 19, 2012

Karen Anderson and co-workers at Yale have reported in JACS on a crystal structures of HIV-1 reverse transcriptase with catechol diether drugs.

HIV

JACS paper

Posted in Aromatic, Diseases, Enzymes, HIV, Proteins | Leave a Comment »

New drugs?

Posted by naturalproductman on April 18, 2012

I just wanted to highlight a C and E News article on some new drug candidates disclosed by drug companies…CEN article

In a nut shell:

Lexicon Pharmaceuticals on a diabetes type 2 drug – SGLT2 transporter inhibitor (JMC paper)

Gilead on an anti-inflammatory drug – TLR7 agonist (PNAS paper)

GlaxoSmithKline on a PI3K inhibitor for cancer treatment (Nature Medicine paper)

Bristol-Myers Squibb on a drug for migraine treatment – CGRP antagonist (ACSML paper)

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

Manoalide vs. HCV

Posted by naturalproductman on March 30, 2012

Nobuyoshi Akimitsu and co-workers from the University of Tokyo have reported on the identification of manoalide A as an inhibitor for heptatitis C virus NS3 helicase.
manoalide

JNP paper

Posted in Diseases, Enzymes, Hepatitis C, Protein Targets, Proteins, Terpenes | Leave a Comment »

 
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