Naturalproductman’s Blog

Hey, is that a natural product?!

Archive for the ‘Enzymes’ Category

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 »

Carbamoyltransferase TobZ

Posted by naturalproductman on March 2, 2012

Milton Stubbs and co-workers have reported in ACIEE on

carbamoyl transferase

ACIEE paper

Posted in Enzymes, Mechanistic, Proteins | 4 Comments »

Half chair transition state

Posted by naturalproductman on February 17, 2012

Andrew Bennet and co-workers from Simon Fraser University have reported in JACS on a transition state study of a sialidase enzyme.

sialidase

JACS paper

Posted in Enzymes, Glucoside, Isotope effects, Mechanistic, Methodology, Proteins | Leave a Comment »

Sirtuin 5 inhibitors

Posted by naturalproductman on January 21, 2012

Hening Lin and co-workers at Cornell have reported in JACS on some sirtuin 5 inhibitors.

peptide

JACS paper

Posted in Enzymes, Histone deacetylase, Methodology, Protein Targets, Proteins, Sirtuin 5 | Leave a Comment »

TS analog complexed with protein and water

Posted by naturalproductman on January 17, 2012

Vern Schramm and co-workers at Albert Einstein College of Medicine have reported in JACS on the observation of a complex between a transition state analog and an enzyme, methylthioadenosine/S-adenosylhomocysteine nucleosidase through mass spectrometry.

transition state

JACS paper

Posted in Chemical Biology, Enzymes, Mass Spectrometry, Mechanistic, Proteins | Leave a Comment »

DNA repair enzymes

Posted by naturalproductman on January 11, 2012

Sheila David and co-workers at UC Davis have reported in JACS on the DNA repair activities of Fpg and hOGG1 glycosylases.

DNA

JACS paper

Posted in Chemical Biology, Enzymes, Nucleic acids, Proteins | Leave a Comment »

 
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