Vegfrecine

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…

JNP paper

Not just isolating small molecules anymore…

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.

OL paper

HIV-1 reverse transcriptase structure with catechol diether

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

JACS paper

New drugs?

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)

Manoalide vs. HCV

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.

JNP paper

Carbamoyltransferase TobZ

Milton Stubbs and co-workers have reported in ACIEE on

ACIEE paper

Half chair transition state

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

JACS paper

Sirtuin 5 inhibitors

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

JACS paper

TS analog complexed with protein and water

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.

JACS paper

DNA repair enzymes

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

JACS paper