5433-54-5Relevant academic research and scientific papers
Dynamic substrate enhancement for the identification of specific, second-site-binding fragments targeting a set of protein tyrosine phosphatases
Schmidt, Marco F.,Groves, Matthew R.,Rademann, Joerg
, p. 2640 - 2646 (2012/05/07)
Protein tyrosine phosphatases (PTPs) are key regulators in living systems and thus are attractive drug targets. The development of potent, selective PTP inhibitors has been a difficult challenge mainly due to the high homology of the phosphotyrosine substrate pockets. Here, a strategy of dynamic substrate enhancement is described targeting the secondary binding sites of PTPs. By screening four different PTPs from bacterial (MptpA) and human origin (PTP1B, HePtp, Shp2) with this assay, specific fragments were identified. One highly specific fragment that binds to the secondary site of Mycobacterium tuberculosis protein tyrosine phosphatase A (MptpA) was characterized in order to validate the assay concept. Finally by covalently linking the secondary fragment to a phosphotyrosine mimetic, a moderately active but highly specific inhibitor of MptpA was obtained.
Convenient synthesis of primary sulfonamides
Greenfield, Alexander,Grosanu, Cristina
body text, p. 6300 - 6303 (2009/04/06)
An efficient protocol for a one-pot synthesis of mono-sulfonamides has been developed. It features utilization of excess of sulfonylating agent followed by base mediated recovery of the primary sulfonamide.
Substituted peptide derivatives
-
, (2013/12/16)
The invention provides a series of novel substituted peptide derivatives of the formulae Ia, Ib and Ic (set out hereinafter) and pharmaceutically acceptable salts thereof, in which the radicals A, R1, R2 and R4-R9 have the meanings defined in the following specification. The compounds of formulae Ia, Ib, and Ic are inhbitors of human leukocytic elastase. The invention also provides pharmaceutical compositions containing a compound of formula Ia, Ib or Ic, or a pharmaceutically acceptable salt thereof and processes and intermediates for the manufacture of compounds of formulae Ia, Ib, and Ic.
