Request for Help

A posting describing the skills and/or resources needed for a given project.

Reduction of Aliphatic Nitro Groups

Published by MatTodd on 26 June 2007 - 9:52am

Subject 

Request for Help

We have been working for a little while on the aza-Henry route to PZQ. We're going to submit a paper to an open access journal on some of this work, but I thought we should post on something we're looking at now, since we've come up against an unexpectedly difficult step and need some help.
We've been trying to reduce an aliphatic nitro group (picture is below). The compound is a model case for PZQ that we've been looking at. This reduction looks to be a very simple reaction, and we did not expect problems.

Google Summer of Code 2007

Published by gtaylor on 20 March 2007 - 4:34pm

Google is now accepting student applications for their 2007 Summer of Code program. I think we can leverage this program to get scientific collaborative enhancements added to The Synaptic Leap to take our collaboration for tropical diseases to the next level.

BackgroundÂ

The Synaptic Leap uses Drupal for our website application. It is an open source PHP/MySql solution designed for optional extension/plugin modules. Historically, google has sponsored quite a few drupal extension module projects in their summer of code program. As such there's advice at the Drupal site on how to go about getting your project approved. Â

Subject 

Request for Help

Community 

general open research

Histone acetyltransferase inhibitors

Published by wjsullivan on 1 December 2006 - 8:30pm

Subject 

Request for Help

Histone acetyltransferases (HATs) and HAT inhibitors
The significance of studying HATs is underscored by an abundance of genetic studies that implicate them in having a role in disease (for reviews, see (10), (6), and (16)).  Consistent with this, some histone deacetylase (HDAC) inhibitors display anti-tumor activity and are being evaluated in clinical trials (8).  In addition to regulating transcription, HATs have crucial functions in modulating other DNA processes (7).  Histone acetylation machinery may also be a viable target for novel anti-infectives (5).
The impact of the various HATs on cellular physiology and disease would greatly benefit from the identification of specific pharmacological inhibitors, but very few have been described to date (11).  Two natural products, anacardic acid and garcinol (a polyprenylated benzophenone), are reported to inhibit both p300/CBP and PCAF in a 5-10 mM range in vitro (1, 2).  In contrast, curcumin displays activity against p300/CBP, but not PCAF (3).  Subsequent studies suggest that anacardic acid may be a broad-spectrum HAT inhibitor, as it also interferes with the MYST HAT Tip60 (13).  Isothiazolones were identified in a high-throughput screen as inhibitors of PCAF and p300 (12), but like the aforementioned compounds, activity against GCN5 was not determined.  Moreover, isothiazolones are strongly reactive with thiol groups and hence are likely to have substantial nonspecific effects.  Two small molecule inhibitors of GCN5 that have been documented include a butyrolactone (4) and MC1626 (2-methyl-3-carbethoxyquinoline) (9).  However, in our hands, the butyrolactone and MC1626 exhibit no inhibition of recombinant yeast GCN5 in a standard in vitro HAT assay (Sullivan, unpublished).  As a positive control, parallel HAT assays showed anacardic acid does inhibit yeast GCN5.
Two reports describe systems that can be used in high-throughput format to identify potential HAT inhibitors (14, 15).
We are interested in acquiring HAT inhibitors, especially those that appear to be selective for distinct types of HATs (i.e. GCN5, MYST).  Not only would these serve as valuable probes to study histone acetylation in eukaryotic cells, they may also hold promise as novel drugs to combat parasitic disease.
References

 

06 Aug

Chagas Community Leader Needed

Published by gtaylor

Community 

general open research

Subject 

Request for Help

We'd like to open a research community for Chagas. We have at least one scientist looking to start an open project for Chagas and we're looking for somebody to be the online champion and leader. General responsibilities include:

  • Writing a research cummunity introduction page, something that will inspire others to pitch in.
  • Identify online news sources for Chagas
  • Identify online tools and resource links for Chagas
  • Evangilize open, collaborative research for Chagas spreading the word helping to get more people participating
  • Monitor the site content people and aiding the community by connecting resources to needs
  • Be generally proactive and vocal, giving The Synaptic Leap constructive criticism helping us to evolve The Synaptic Leap processes and tools

Other volunteers at The Synaptic Leap will set up the menu links and other core research community pages.

Email Ginger if you're interested.

21 Jul

Chikungunya in Mauritius

Published by vishwadev

Community 

general open research

Subject 

Request for Help
Sir/Madam,
 
i recently came across this wonderful site and i am pleased that it is doing a very noble work of doing open source research for non-profit motives.
 
I have a request if you don't mind. I am from a tropical island called Mauritius found in the indian ocean. A few months back our island and our neighbour island reunion got badly struck with the chikungunya disease and it has affected our economy and people very much.
 
No drugs are available apart from pain killers and some of the patients (including my mother) are having ever lasting pain. maybe you could please place chikungunya in your research calendar as no labs are coming with drugs or enough research on this project. Maybe because it is a problem not affecting big european countries...
 
here in Mauritius, for the time being it is under control because it is winter and the insects/vectors are having difficulty to reproduce. But we are dreading the return of summer in November. I wish there were enough reseach in this field but there are not many promising ones at present. Therefore i am very humbly requesting you to put your expertise together and come forward with a research programme on this disease so that it can be controlled or cured.
 
Thank you.
Regards
 
 -prakash
Mauritius 
 
29 May

Jean-Claude's Reactions

Published by MatTodd

Subject 

Request for Help

Jean-Claude Bradley and his team over at UsefulChem have been having a go at two reactions that have relevance to generating drug candidates for malaria. Organic chemists should check out the site if they feel they can help with what's going on. The two reactions are firstly the conversion of adrenaline to catechol aldehyde:

UsefulChem Adrenaline Conversion

and secondly the Ugi synthesis of a DKP along the following lines:

 

UsefulChem DKP Ugi

The resources needed are your input into how to make these reactions go! The Usefulchem team are making good use of YouTube video feeds to provide extra information on what's going on with their attempts.

Cheers,

Mat

 

UsefulChem DKP Ugi

Published by MatTodd on 29 May 2006 - 11:38am

UsefulChem DKP Ugi


Subject 

Request for Help

Image Galleries 

TSL Images

UsefulChem Adrenaline Conversion

Published by MatTodd on 29 May 2006 - 11:36am

UsefulChem Adrenaline Conversion

Subject 

Request for Help

Image Galleries 

TSL Images
13 Mar

Ways to get involved and the Stanford Connection

Published by MatTodd

Community 

general open research

Subject 

Request for Help

A few of us have recently been talking via email about exciting developments at Stanford, and Ginger prompted me to post this on the site so others could comment. Here are the emails, edited down…

Marc originally visited Stanford to talk on what he's doing in the area of neglected diseases (http://www.salilab.org/~marcius/home/?page=talks). His talk was hosted by Achal Acrol.

In response, Achal wrote:

 

“I think it was clear that today's audience was very excited by your talk, and in general through my work with ADEM [Access and Delivery of Essential Medicines] I have noticed a growing interest here at Stanford among young researchers to carry out their training and career development in traditional ways while somehow finding some other way to simultaneously apply those skills/resources to affect some amount of positive change in the world.

 

I see probably the most effective collaboration of our efforts to be that while I continue to sign up labs that would be willing to provide certain resources and services, you could provide us with a wish-list of biological/chemical resources you would need to fully test any of the computational work your team does. In essence I would work to provide (the other 95%) 'beta-testers' that could respond to your computational biologists 'programming core' and perform the wet lab experiments and cell culture and in vivo experiments to verify in an open source manner the efficacy of those agents.

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