HOME >> BIOLOGY >> NEWS
Better Binding Through Chemistry

HHMI and Stanford scientists chose as their drug target a basic protein molecular subunit known as an "SH2 domain," which mediates protein-protein interactions that cause some diseases. This domain is regarded as a choice target for drug development because it is found in tyrosine kinases, enzymes that are critical components of the molecular machinery involved in cancer, osteoporosis, and inflammation. Despite its high profile among rational drug designers at pharmaceutical companies, the SH2 domain has proven to be an intractable drug target.

As their drug candidates, Crabtree and his colleagues chose peptides that contained the amino acid phosphotyrosine, which bind to the SH2 domain. The researchers hooked these peptides to a small linker molecule that sticks tightly to a human protein, FKBP.

Experiments with numerous peptide-linker combinations showed that certain combinations bound to the SH2 domain up to three times more tightly than did the peptide alone. These studies also demonstrated that it was possible to optimize binding by adjusting the linker segment so that it would place FKBP at just the right angle to produce the best fit with the target protein.

Medicinal chemists already take advantage of the fact that many drugs bind to blood-borne proteins such as serum albumin, which thereby allows small molecules to remain in circulation far longer than normal. Now, there is the potential to use another set of proteins to improve a drug's ability to bind to its target. "There are a great many candidate presenting proteins that exist inside and outside the cell, offering a wide variety of options for drug designers," says Crabtree.


'"/>

Contact: Jim Keeley
keeleyj@hhmi.org
301-215-8858
Howard Hughes Medical Institute
2-Mar-1999


Page: 1 2 3

Related biology news :

1. Better living through urban ecology
2. Better techniques needed to predict earthquake hazards, UC study finds
3. Better model of cancer development sheds light on potential angiogenesis target
4. Natural Science and Public Health: Prescription for a Better Environment
5. Better computer modeling provides a new look at large biomolecules
6. UF nutritionist: Better to vow to eat healthy for new year
7. Better "bugs" lead to cheaper ethanol from biomass
8. Diet and cancer prevention: a sampler of story ideas for 5-a-Day for Better Health Week
9. Some Atlantic Coast Beaches Are Shrinking While Floridas Beaches Better Off Than Most
10. New Polyester Products Perform Better And Are Easy To Recycle
11. Urine Tests Will Do Better Than Pelvic Exams To Save Teens From Serious Effects Of Sexually Transmitted Diseases, UCSF Analysis Shows

Post Your Comments:
*Name:
*Comment:
*Email:


(Date:5/9/2019)... ... May 09, 2019 , ... Akadeum Life Sciences today announced ... its microbubble technology. Unlike magnetic-based products, microbubbles use buoyancy to gently separate cells ... who participated in an early access program has been very encouraging and has ...
(Date:5/8/2019)... ... May 08, 2019 , ... ... diameter of 200 microns and a lead-in fiber of 100 microns. With dimensions ... standard and positioning itself as the world leader in the development of fiber ...
(Date:5/2/2019)... (PRWEB) , ... May 01, 2019 , ... ... that give families insight into their future children, announces a new publication titled, ... in the journal of Pregnancy and Child Health. Previous studies had only shown ...
Breaking Biology News(10 mins):
(Date:4/25/2019)... ... April 24, 2019 , ... Inference Solutions ... service organizations, today announced global availability of Inference Studio’s latest version, which makes ... sizes to harness the power of Google’s Contact Center AI (CCAI). ...
(Date:4/15/2019)... ... April 15, 2019 , ... Sirrus, Inc., ... $2 million bench plant expansion to increase production of methylene malonate monomers and ... and construction of Sirrus’ full-scale production facility, which is scheduled to break ground ...
(Date:4/9/2019)... ... April 09, 2019 , ... USDM ... capacity of life sciences organizations to accelerate innovation and maximize productivity, announces that ... the past 12 months. , USDM’s Cloud Assurance is a managed ...
(Date:4/8/2019)... SAN FRANCISCO (PRWEB) , ... April 08, 2019 , ... ... to accredited investors a $15 million preferred equity investment in the privately held pharmaceutical ... dysfunction. Its leading drug, Lorexys, is targeted at female hypoactive sexual dysfunction disorder and ...
Breaking Biology Technology:
Cached News: