Dipartimento di Scienza e Tecnologia del Farmaco

Descrizione del progetto

Membri:

Barbara Buccinnà (Dip. Oncologia)
Elisa Lupino (Dip. Oncologia)
Marco Piccinini (Dip. Oncologia)
Cristina Ramondetti (Dip. Oncologia)

Members of other units:

Salam Al-Karadaghi
Jean Marie Contreras
Joel Sussman
Yoav Peleg
Israel Silman
Björn Walse
Bo Svensson
Schächtele Christoph
Bruno Giethlen
Michael Kubbuttat

Partners:
SARomics Biostructures (S)
Prestwick Chemical (F)
ProQinase (D)
University of Turin (DSTF and Department of Oncology - I) mettere link
Israel Structural Proteomics Center (ISPC) at the Weizmann Institute of Science (Israel)
TechMedIll platform of the University of Strasbourg

Sponsors:
EU 7th Framework Program “Research for the Benefit of SMEs

Description
Targeting kinases has become one of the most important therapeutic opportunities for treating cancer, diabetes, inflammatory diseases and more. The TAKTIC Consortium, funded with €1.149 million / 24 months, brings together the unique and proprietary technologies of three SMEs and their knowhow in the field of drug discovery. To this are coupled the extensive expertise in medicinal chemistry, kinase biochemistry and biology of the University of Turin as well as the state-of-the-art high throughput platform for protein expression and crystallization of the Israel Structural Proteomics Centre. The merging of the highly complementary capabilities of the six partners within the TAKTIC Consortium enables an efficient and versatile kinase drug discovery platform that will target some challenging and medically important kinases.

The University of Turin is involved in TAKTIC with two groups: the Medicinal Chemistry Unit, coordinated by Dr. Marco L. Lolli and based in the Department of Science and Drug Technologies (DSTF), and the Biochemistry Unit coordinated by Dr. Marco Piccinini, and based in the Department of Oncology.

DSTF will be responsible of the synthesis of compound clusters during each optimization cycle. The unit is carefully designed to be able to produce around 20 new compounds during each cycle, which has a duration of 6 weeks, starting from the fourth month until the end of the project. The unit has strong expertise in advanced stepwise organic synthesis and in combinatorial chemistry, which will allow it to accomplish the tasks in the most efficient way. DSTF will also be involved in the analysis of the results from the primary screen in order to select the best possible starting compounds. In addition, during each of the optimisation cycles, DSTF will be involved in the analysis of the generated data and in the design of the compounds for the subsequent cycles. To ensure the uniqueness of the synthesised compounds, during the optimisation cycles particular attentions will be paid to the use of the principles of bioisosterism.

TAKTIC started in February 2013.

Keywords:
Oncology, kinases, NFkB, bioisosterism, Crystallography, Fragement-based Drug Design, Ligand-based Drug Design

Links:
MEDSYNTH
TAKTIC (7FP-SME PROJECT)

Aree/Progetti collegati:

MedChemSynth (MeDS)

Organic Chemistry @ Pharmacy (OCP)