4AZ1: Crystal Structure Of The Trypanosoma Cruzi Protein Tyrosine Phosphatase Tcptp1, A Potential Therapeutic Target For Chagas' Disease

Chagas' disease, a neglected tropical affliction transmitted by the flagellated protozoan Trypanosoma cruzi, is prevalent in Latin America and affects nearly 18 million people worldwide, yet few approved drugs are available to treat the disease. Moreover, the currently available drugs exhibit severe toxicity or are poorly effective in the chronic phase of the disease. This limitation, along with the large population at risk, underscores the urgent need to discover new molecular targets and novel therapeutic agents. Recently, the T. cruzi protein tyrosine phosphatase TcPTP1 has been implicated in the cellular differentiation and infectivity of the parasite and is therefore a promising target for the design of novel anti-parasitic drugs. Here, we report the X-ray crystal structure of TcPTP1 refined to a resolution of 2.18A, which provides structural insights into the active site environment that can be used to initiate structure-based drug design efforts to develop specific TcPTP1 inhibitors. Potential strategies to develop such inhibitors are also discussed.
PDB ID: 4AZ1Download
MMDB ID: 105186
PDB Deposition Date: 2012/6/22
Updated in MMDB: 2012/11
Experimental Method:
x-ray diffraction
Resolution: 2.18  Å
Source Organism:
Similar Structures:
Biological Unit for 4AZ1: dimeric; determined by author and by software (PISA)
Molecular Components in 4AZ1
Label Count Molecule
Proteins (2 molecules)
Tyrosine Specific Protein Phosphatase
Molecule annotation
Chemicals (6 molecules)
* Click molecule labels to explore molecular sequence information.

Citing MMDB