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Competitor Analysis: Protein Kinase C (PKC) Inhibitors
La Merie, Jan 2009, Pages: 21
The present Competitive Intelligence Report about new developments in the pipeline of inhibitors of the protein kinase C (PKC) provides a competitor evaluation in the field of R&D projects from preclinical stages up to advanced clinical phases of PKC Inhibitors as of January 2009.
The serine/threonine protein kinase C (PKC) family consists of at least 11 mammalian isozymes belonging to a larger subclass of protein kinases termed the adenine-guanine-cytosine (AGC) kinases. PKCs are important components of intracellular signal transduction pathways and have been implicated in regulating a wide variety of biological functions and processes, ranging from cell growth, differentiation and apoptosis to synaptic plasticity and from neuronal injury to cellular immune responses. PKCs are known for their broad range of tissue- and cell-specific distribution and differential sub cellular location. PKCs can be grouped into three categories: classical or conventional PKCs (subtypes alpha, beta and gamma), novel PKCs (delta, epsilon, eta, theta and my) and atypical PKCs (zeta, tau/lambda). PKC isoformes with functional importance in T and B cell signaling are PKC alpha & PKC theta and PKC beta & PKC delta, respectively. The essential role of PKC theta is derived from the observation that it is the only isoform that is selectively translocated to the T-cell/antigen presenting cell contact site immediately after cell-cell interaction. PKC theta is crucial for IL-2 production, a prerequisite for the proliferation of T cells, whereas PKC alpha in T cells is required for proliferation and IFN-gamma production. B cells require PKC beta for proper antigen receptor function and PKC delta for the induction of tolerance. These PKC isoforms in B and T cells are considered attractive targets for autoimmune diseases. PKC inhibitors and activators have gained considerable interest as specific therapies of a number of different diseases, depending on PKC isozyme. The publication of the catalytic domain crystal structure of protein kinase C theta has raised considerable interest in rational drug design and small molecule drug discovery of selective inhibitors of PKC theta which has been implicated in T-cell mediated disease processes including inflammation and autoimmunity.
The report includes a compilation of current active projects in research and development of subtype-selective and multi-PKC inhibitors as well as of PKC activators, for the treatment of diabetic retinopathy, cancer, transplanted rejection, psoriasis, heart failure, neuropathic pain and more.
In addition, the report lists company-specific pipelines of PKC inhibitors. Competitor projects are listed in a tabular format providing information on:
- Drug Codes
- Target / Mechanism of Action
- Class of Compound
- Company
- Product Category
- Indication
- R&D Stage and additional comments with a hyperlink leading to the source of information.
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