Bcl-XL and Bcl-2 interaction

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.

ACIE 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)

cADPR agonist synthesis

Barry Potter (not Harry Potter) and colleague in the UK have reported in JOC on the synthesis of a cyclic adenosine 5′-phosphate receptor (cADPR) agonist.

JOC paper

Bexarotene and Alzheimer’s

Many people have probably already heard of this report in Science of an anti-cancer drug, bexarotene, being effective against treating Alzheimer’s disease.

 

Science paper

Vitamin D receptor agonist

Hiroyuki Kagechika and co-workers have published in JACS on a Tokyo Medical and Dental University p-carborane containing vitamin D analog that can bind to the vitamin D receptor as an agonist.

JACS paper

Arabilin synthesis

Kathlyn Parker and colleague have reported in JACS on a synthesis of arabilin, an androgen receptor antagonist that can potentially treat prostate cancer (IC50 of 11 micromolar towards AR).  A 1,7-hydride shift occured in their key Stille coupling to afford the correct isomer.

JACS paper

Kynurenine is a ligand for the AH receptor

Michael Platten and co-workers from the German Cancer Research Center have reported in Nature on the role of kynurenine (Kyn), which is the TDO (tryptophan-2,3-dioxygenase) enzyme product of tryptophan. They report that Kyn is an endogenous ligand for the aryl hydrocarbon receptor, which is a transcription factor with a very complex story behind it.

 

Nature paper

QSAR studies for androgen receptor

Jose Manuel Garcia de la Vega (Universidad Autonoma de Madrid) and co-workers have reported in the Journal of Steroid Biochemistry and Molecular Biology on some QSAR studiesfor androgen analogs acting on androgen receptors.  If you were ever curious about how drug design works, this paper may illustrate a good example of the computational chemist’s approach.

 

JSBMB paper