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Target Analytical Report - CCKBR


Description: The cholecystokinin 2 receptor (CCKBR; CCK2R) is a member of the rhodopsin-like G protein-coupled receptor family that mediates important physiological functions by binding cholecystokinin (CCK) and gastrin peptides.

The CCK2R is present in the central nervous system, where it regulates anxiety/panic attacks, dopamine release, and nociception. In the periphery, it regulates acid, histamine, and leptin secretion as well as cell growth and differentiation.

CCKBR has been reported to be associated with various tumours. Given the clinical importance of CCK2R-mediated functions, great interest has been devoted to the identification of efficient and selective CCK2 ligands. The predominant brain cholecystokinin receptor (CCK-B/gastrin) has been implicated in mediating many of the central effects of cholecystokinin, including anxiety, panic attacks, satiety, and analgesia, suggesting it is an important pharmacologic target.

Today, the drug discovery research sector faces tremendous internal and external pressure due to the huge investments required in terms of money and time in order to produce meaningful information from the huge data sources available on a molecule. This process involves increased involvement from cross functional domains like Molecular Biology, Bioinformatics and Medicinal Chemistry, which has made the process both cumbersome and complicated.

This current report on CCKBR1 addresses the above problem as a compilation of manually curated information that is derived from the following sources:

- Public domain databases such as SwissProt, UniProt, Entrez PubMed, OMIM, etc
- In-house databases
- Curated information from journal articles and reviews
- Chemistry information from patents
- Company websites

Competitive landscape

The competitive landscape information is obtained by analysis of manually selected patents in the area of small molecules acting on the target


Contents: 1 Introduction
1.1 Scope of the Report
1.2 Methodology
1.3 The Target

2 Biology Information
2.1 Gene Identity
2.2 Genomic context
2.3 Gene, mRNA transcript, and protein sequence
2.4 SNPs linked to gene
2.5 Gene Orthologues and Paralogues
2.6 miRNA targeting the gene
2.7 Cellular localization
2.8 Protein function
2.9 Biological process
2.10 Protein Family
2.11 Protein Domains
2.12 Tissue specificity
2.13 Post translational modification
2.14 Protein Interactions
2.15 Pathways

3 Disease Association
3.1 Expression profile in Disease state
3.2 Mutations in disease pathology
3.3 Interactions/pathways in disease pathology

4. Experimental Source
4.1 Knockout mice strains
4.2 siRNA for knock-down studies
4.3 Antibodies for the target

5 Structural Biology
5.1 Crystal structure information

6 Chemistry Information
6.1 Chemotypes available for the Target
6.2 Regions critical for ligand binding

7 Competitive Landscape
7.1 Patenting activity

8 Drug Clinical Candidates


Summary: The Target Analytical Report of CCKBR is a compilation providing seamlessly mined chemical, biological and target related data in an integrated manner. The objective of this report is to provide focused information around a target to help with the evaluation of the target with respect to the following.

- Science (interdisciplinary areas of chemistry, biology, pharmacology, structural biology)
- IP/Competitive landscape
- Suitability of the target to the drug discovery program

This Report is a comprehensive report on the available information from the following:

- Patents (US, WIPO and EP)
- Journal articles and reviews
- Public domain databases
- Company websites (News letters)

The uniqueness of this service lies in the way it talks about biology to chemists and chemistry to biologists by strongly establishing the cross-domain interactions. The report is designed in such a way that it delivers value to scientists in making decisions quickly based on reliable manually curated information, thereby speeding up time-to-market and increasing the ROI. Our clients are medicinal chemists, computational chemists, and biologists involved in drug design from major pharma and biotech companies.

This report enables to:

- Derive prior information on the target and molecules that act upon the target
- Derive IP and competitive landscape around the target showing compounds involved in active research
- Generate state of art information on the scaffolds and their biological activity presented together
- Rapidly map chemical diversity space
- Prioritize lead molecules for synthesis
- In silico generation of combinatorial chemistry libraries for pharmacophore screening/docking studies
- Focused library generation for prioritization of synthesis
- Understand protein-ligand relationship better
- Explore SAR in virtual and real screens, SAR points allow building of QSAR training sets
- Marketed drugs for the target and those that are in clinical stage

The report is organized into different sections.

- The biology information section contains general details of the CCKBR gene and protein such as nomenclature, isoforms, interacting molecules, functions and involvement in normal pathway.
- The associated disease section contains information regarding altered expression, mutations and altered pathway that leads to pathogenesis of the disease in which it is implicated.
- The structural biology section contains information regarding closely matching and related structures available in PDB.
- The chemistry section contains chemotypes information of compounds active against the target from patents and research articles.
- Competitive landscape information identifies patents and articles related to the target as well as companies and institutions that are active in the target area.
- Drug candidates section contains details of target related FDA approved drugs and those that are in clinical trials.

Thus, the report presented herein facilitates a discovery scientist to make crucial decisions on the target, and also aids in drug design by providing information on small molecule compounds known to be agonists/antagonists for the target along with their activities. In addition it provides valuable information on the Market intelligence around the companies working on this target.


Companies Mentioned - Applied Biosystems - abcam - Aphton Corporation - Chugai Seiyaku Kabushiki Kaisha - Daiichi Pharmaceutical Co. Ltd. - Eli Lilly And Company - Ferring Research Ltd - Fujisawa Pharmaceutical Co.Ltd. - G. D. Searle & Co.(Us) - Glaxo Inc. - Invitrogen - James Black Foundation Limited - Janssen Pharmaceutica - Kyoto Pharmaceutical University - Merck & Co. Inc. - Merck Sharp & Dohme Ltd. - Millipore - New England Medical Center Hospitals Inc. - Nippon Shokubai Co. Ltd. - Pfizer Inc. - Rotta Research Laboratorium S.P.A. - Rottapharm S.P.A. - Sigmaaldrich - Sanofi-Synthelabo - Shionogi & Co.Ltd. - Warner-Lambert Company - Yamanouchi Pharmaceutical Co Ltd - Yoshitomi Pharmaceutical Industries Ltd - Zeria Pharmaceutical Co. Ltd


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