Naturalproductman’s Blog

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Archive for the ‘Proteins’ Category

Erythropoietin synthesis

Posted by naturalproductman on December 13, 2013

Danishefsky and co-workers reported in Science on the synthesis of erythropoietin after 1000 steps. Just kidding.

Science paper

Posted in Proteins, Total Synthesis | 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 »

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 »

Type 2 diabetes therapeutic?

Posted by naturalproductman on October 23, 2012

Here’s a study by Zhong-Yin Zhang and co-workers at Indiana University on a PTP-MEG2 inhibitor.

diabetes 2

JACS paper

Posted in Chemical Biology, Diabetes Type 2, Diseases, Methodology, Protein Targets, protein tyrosine phosphatase 1B (PTP1B), 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 »

 
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