The true test of validation comes only when a selective inhibitor for the chosen target is advanced to the clinic and shown to be efficacious in the appropriate human disease. However, advancing the wrong target to this stage is a costly mistake. 

Genomic applications map: Guide to terms in these glossaries    Site Map
Related glossaries include: 
Applications Drug discovery & development   Functional genomics
Informatics: In silico & molecular modeling
Technologies Gene amplification & PCR   Genetic Manipulation & Disruption   Microarrays   Molecular Imaging

antisense cleavers & blockers: Pharmaceutical biology

cellular signaling networks: Metabolic profiling

chemical ligand studies: Drug discovery & development

clinical antibodies:  See therapeutic antibodies

Related terms: monoclonal antibodies

compound profiling: Biology has considerable experience with gene and protein- centered informatics, but chemistry is at an earlier stage of developing databases that are truly compound- centric. The historical paradigm of identifying and optimizing hits for potency, and then looking to evaluate and optimize for ADME and toxicity properties is quickly shifting to a more parallel approach that considers ADME/Tox properties at an earlier stage. This concept is epitomized by methods for differentiating between drug- like and non- drug- like compounds, the use of which is increasing significantly. Moving compound profiling earlier means that many more compounds must be assessed, which is both the value and the challenge of this shift. 

compound validation: Assays & screening

concept validation: Model & other organisms

Discovery on target  October 15-18, 2007 - Boston, Massachusetts

difficult targets:  Topics include: High Content Screening, FLIM/FRET assays, advances in fluorescent probes and biosensors, increasing multiplexing, label free screening, screening in primary and live cells, screening in model organisms, screening in tissues, screening in stem cells, high content toxicity screening, high content neuronal screening. Screening Difficult Targets: New Approaches to Cellular Screening, January 15-17, 2008 • San Francisco, CA

disease targets: The critical strategy for a pharmaceutical company going forward is one that uses pharmacogenomics and biomedical informatics to better define disease targets. ...  Pharmacogenomics is key to gaining a better definition of disease, a better stratification of patients and improved disease staging. Until these are clear, and until some form of biomedical informatics is put into place, therapeutic design is going to be flawed by poorly defined targets. 

Google = about 3,250, Aug, 24, 2002; about 12,900 June 10, 2004; about 104,000 Nov 13, 2006

Broader term: target Related term: drug target

diversity, diversity screening: Drug discovery & development

drug target:  Good drugs are potent and specific; that is, they must have strong effects on a specific biological pathway and minimal effects on all other pathways. Confirmation that a compound inhibits the intended target (drug target validation) and the identification of undesirable secondary effects are among the main challenges in developing new drugs. Matthew J. Morton et. al, Drug target validation and identification of secondary drug target effects using DNA Microarrays,  November 1998 4 (11): 1293 - 1301, Nov. 1998

Google = about 10,700, Aug, 24, 2002; about 16,500 June 16, 2003; about 33,500 June 10, 2004; about 586,000 Nov 13, 2006

Related terms:  molecular drug targets, target families, targets

drug targeting:  A strategy aiming at the delivery of a compound to a particular tissue of the body. [IUPAC Medicinal Chemistry] 

Google = about  6,150, Aug, 24, 2002; about 15,200 June 10, 2004; about 295,000 Nov 13, 2006

Related terms: target, target validation. Narrower terms: gene target, protein target

druggable targets: "We have historically fewer innovative targets per year", said Christopher Lipinski, formerly of Pfizer, showing that only 24 innovative drugs with new targets have been launched between 1994 and 2001 "Many more druggable targets may have emerged in these eight years, but there are not enough druglike molecules to match them", Lipinski said. Horizon Symposia 4 Charting Chemical Space, 2004 . http://www.nature.com/horizon/chemicalspace/highlights/s3_nonspec2.html

emerging targets: The report assesses the issues in target-based drug discovery and development as well as several specific issues that are common to these and other complex diseases with high unmet medical need. … Evaluation of leading emerging targets in terms of signaling pathways and therapeutic strategies. Insight Pharma Reports Emerging Targets in Disease with High Unmet Needs, 2006

gene target: Having identified a potential gene target (and, by inference, its protein product), one may wish to: (a) sequence the gene in a large number of affected and normal individuals to identify functional and diagnostic polymorphisms associated with the disease; or (b) rapidly screen the protein product for interactions with entities within the chemical portfolio of the company. Clearly, these needs are addressed by very different approaches and technological platforms, all of which may be defined as high throughput genomic strategies. 

Google = about  1,080, Aug, 24, 2002; about 4,070 May 12, 2004; about 96,900 Nov 13, 2006 

gene targeting: Genetic manipulation & disruption

G.O.T. Summit Getting Optimized Targets   Microarrays, Genomic Sample Prep, Proteomic Sample Prep   May 19- 21, 2008 Boston MA

g- protein coupled receptors: Pharmaceutical biology

GPCR's: See G protein coupled receptors

G-protein: One of a group of proteins involved in signal transduction - the intercellular or intracellular transfer of activation or inhibition signals through a so- called signaling pathway. within cells. [National Institute of General Medical Sciences (NIGMS)] 

Narrower terms: G- protein coupled receptor GPCR,  orphan G- protein coupled receptors, GPCRomics

G-protein-coupled receptors GPCRs:  About 50% of existing drugs work by targeting G-protein coupled receptors (GPCRs), which remain an actively investigated class of drug targets. GPCRs represent the largest protein family in the human genome, and it is believed that about half of all GPCRs are pharmaceutically relevant. GPCRs are involved in many therapeutic areas including cardiovascular disease, inflammatory disease, CNS disorders, and metabolic disease. However, the functions of many GPCRs remain unknown, as do the natural ligands of many of these receptors. The lack of structural information makes it difficult to identify novel hits for GPCRs. G-Protein Coupled Receptor Drug Discovery April 29-30, 2008 • La Jolla, CA

The largest family of cell surface receptors  involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC F- PROTEINS  MeSH 2004 "receptors, g-protein coupled".

Related terms: G protein GPCRomics; Narrower term: orphan G-protein coupled receptors

Haplo-Insufficiency Profiling HIP: The objective of this project is to provide an automated system for haploinsufficiency profiling (HIP) screens. The screen system is a pool of gene deleted yeast grown against a drug at a concentration that inhibits the yeast pool growth rate to 80% of wild type (wt). For high throughput and automation the screens are grown in 48 or 96 well plates.  Yeast screen robot for Haplo Insufficiency Profiling (HIP) Genome Technology Center, Stanford Univ School of Medicine, 2007 http://med.stanford.edu/sgtc/technology/yeastscreen_robot.html 

HDAC inhibitors: Histone Deacetylase Inhibitors Discovery on Target, Oct 16- 17, 2007, Boston MA 

homology: Functional genomics

immunogenicity assessment: Therapeutic antibodies and proteins in clinical development or on the market to some extent have the potential to be immunogenic. The formation of antibodies to these therapeutic agents may; 1) have no clinical consequence, 2) cause mild to severe adverse effects in patients, and/or 3) effect the efficacy of the agent due to neutralization of drug activity or effects on drug pharmacodynamics and pharmacokinetics. Development of a preclinical and clinical plan to evaluate for the presence of an immune response by assay detection and surveillance of clinical symptoms, suggestive of an immune response, is essential during drug development. Assessment of Immunogenicity in Clinical Trials, April 30- May 1, 2008 • Boston, MA

immunotargeting: 

Google = about 25,100 Nov 13, 2006; about 40,400 May 24, 2007

Narrower term: vascular immunotargeting 

ion channels: Gated, ion-selective glycoproteins that traverse membranes. The stimulus for channel gating can be a membrane potential, drug, transmitter, cytoplasmic messenger, or a mechanical deformation. Ion channels which are integral parts of ionotropic neurotransmitter receptors are not included. MeSH 1979 

Ion Channels,  Discovery on Target, Oct 17- 18, 2007, Boston MA

kinase pipelines:  Protein kinases constitute a large family of proteins that is now firmly established as a major class of drug targets for the pharmaceutical industry. The sequencing of the human genome has led to the identification of 518 protein kinases encoded within it—the human kinome. This constitutes one of the largest and most druggable classes of targets for the pharmaceutical industry, with the number of kinases exceeding the number of G-protein coupled receptors in the human genome.  Insight Pharma Reports Kinase Therapeutic Pipelines: An assessment of Targets and Agents in Development  2007

kinase inhibitors:  kinase inhibitors: Discovery on Target, Oct 16- 17, 2007, Boston MA  

See also protein kinases

medicinal chemistry:  Medicinal & Pharmaceutical Chemistry

molecular drug targets: Disease associated genes or proteins.

Google = about  82, Aug, 24, 2002; about 201 June 10, 2004; about 2,060 Nov 13, 2006

molecular profiling: Expression gene and protein

molecular targets:  Collections of genes organized by pathways and by ontology (functional classification) permitting aggregate evaluation of anomalies (overexpression, underexpression, mutation). Molecular Targets, Cancer Molecular Analysis Project, National Cancer Institute http://cmap.nci.nih.gov/Targets

Can include antibodies, enzymes, receptors.

Google = about 12, 200, Aug. 24, 2002; about 42, 600 June 10, 2004; about 658,000 Nov. 13, 2006; about 832, 000 May 24, 2007

Related terms: Pharmaceutical biology

molecular targeting: The idea behind molecular targeting is to design drugs that specifically attack the molecular pathways that cause disease, without disrupting the normal functions in our cells and tissues. Drugs developed using this approach can be less toxic and more effective than current medicines. Molecular Targeting, PhRMA, innovation.org http://www.innovation.org/index.cfm/FutureofInnovation/NextWaveofInnovation/Molecular_Targeting

molecular targets for cancer prevention, molecular targets for cancer treatment, Molecular Targets Laboratory Initiative: Cancer genomics

monoclonal antibodies MAbs: Pharmaceutical biology

nuclear hormone receptor modulators:  Nuclear hormone receptors  Discovery on Target, Oct 16- 17, 2007, Boston MA

See also receptors, cytoplasmic and nuclear

oligonucleotide based therapeutics:    Discovery on Target, Oct 16- 17, 2007, Boston MA 

oncogene: Cancer genomics

pain targets: The need for new pain therapeutics remains great, largely due to the inadequacy of existing drugs on the market.  In response, several new pain targets are being aggressively pursued with discovery programs in Pharma and Biotech.  This meeting will showcase several of the leading programs targeting vanilloid cannabinoid, and purinergic receptors and some additional coverage of nicotinic, glutaminergic and bradykinin receptor modulators. Targeting Pain with Novel Therapeutics part of the World Pharmaceutical Congress, May 12- 13 2008 Philadelphia PA

predictive biosimulation: In Silico & Molecular Modeling

protein families, protein structure: Protein structure  Critical to determining whether a drug target is druggable

protein kinases: A family of enzymes that catalyze the conversion of ATP and a protein to ADP and a phosphoprotein. EC 2.7.1.37.  MeSH, 1980  

Current knowledge from from academia, biotech and the pharmaceutical industry with data and case studies of new targets and methods used to discover novel kinase inhibitors and to explore the kinome. In order to stay ahead of the competition in the field it is necessary to keep updated on the current state of the art on lead compounds as well as on the newest developments in structure based drug design and the current assay technologies. In addition, moderated discussions on target validation, on how to bring sense into the chemical space and on how to analyze the flood of data available will be presented. Protein Kinase Targets: Drug Discovery & Design  June 23-25, 2008 • Boston, Massachusetts

More than 500 human kinases have been identified, making them significant drug discovery targets. Kinase modulation has drawn increasing attention not only from pharmaceutical and biotech companies, but also from firms involved in target validation and candidate screening. Several kinase inhibitors are just now reaching the market, and many more candidates are in the development pipeline.  Insight Pharma Reports, Kinases: From Targets to Therapeutics report, 2003

Protein kinase evolution, SUGEN, 2002 http://www.kinase.com/evolution/
Protein kinase resource, San Diego Supercomputer Center, US  http://www.kinasenet.org/pkr/Welcome.do;jsessionid=F06E8FA79BE231648391BDCEFE33402C 

Related terms: kinase inhibitors,  Combinatorial libraries & synthesis;; Drug discovery & development; -Omes & -omics kinome,  kinomics

protein- protein interactions: Proteomics

protein targets: The purpose of the "PDB ligands" link is to give, at a glance, a quick way of determining if compounds in the selected SOM cluster have any "known" protein targets and if any homologous human proteins exists. The PDB ligands link from each cluster page provides connections to structural data as deposited in the Protein Data Bank (PBD). PDB Ligands Summary,  http://spheroid99.ncifcrf.gov/ManPages/ManPdbLigands.cfm 

Google = about 2,340 Aug. 24, 2002; about 3,790 Aug. 27, 2003; about 7,710 June 10, 2004; 133,000 Nov 13, 2004; about 154,000 May 25, 2007

Related terms: structure- based design; NMR  site-directed NMR analysis; Microarrays small molecule microarrays 

prototypes: Drug discovery & development

receptors, cytoplasmic and nuclear: Proteins in the cytoplasm or nucleus that specifically bind signaling molecules and trigger changes which influence the behavior of cells. The major groups are the steroid hormone receptors (RECEPTORS, STEROID), which usually are found in the cytoplasm, and the thyroid hormone receptors (RECEPTORS, THYROID HORMONE), which usually are found in the nucleus. Receptors, unlike enzymes, generally do not catalyze chemical changes in their ligands. MeSH 1994

See also nuclear hormone receptors

recombinant antibodies: Recombinant Antibodies hold great promise as biotherapeutics and as reagents for diagnostics and drug discovery. They have proven themselves superb tools in both genomics and proteomics, promising continued growth in this research area. All of these trends place a tremendous emphasis on the development of new approaches for faster antibody development, improved methods of selection and optimization, alternatives for production, and evaluation for novel applications.  PEGS Recombinant Antibodies April 29- May 1, 2008, Boston MA

RNAi  interference: Genetic Manipulation & Disruption

RNAi target validation: As new research unravel the complex cellular pathways of RNA interference (RNAi), new technology platforms are being developed to exploit those RNAi-related mechanisms for use in early drug discovery. Drug discovery units in most companies now routinely use RNAi screening for identifying and validating potential drug targets in various therapeutic areas. The screens themselves, using small interfering RNA (siRNA) or short hairpin (shRNA) libraries, have become more sensitive, high-throughput and large-scale. However, is RNAi screening being done in a manner that’s most efficient and effective in generating valid drug targets? Can there be further improvements in assay design and experimental protocols to minimize off-target effects and obtain reliable data? RNAi for Target validation How to Best Utilize RNAi Screening Technologies for Target Discovery June 9-10, 2008 • San Francisco, CA

RNAi therapeutics: RNA

retargeting: A conceptual breakthrough in gene therapy would be gene transfer vector that could be systemically applied, allowing targeted gene transfer into a predetermined cell type.  C. Haynes et. al, Modified envelope glycoproteins to retarget retroviral vectors, Current Gene Therapy 3(5): 405- 410, Oct. 2003

Related term: Molecular Medicine gene therapy

systems biology: Genetic Manipulation & Disruption

target:   Molecules in the body that may be addressed by drugs to produce a therapeutic effect. (Also used to refer to the material -- DNA or RNA - that one exposes to the probes on a microarray so that hybridization can be measured subsequently. CHI High- Content Analysis Market Outlook report, 2004  

A molecule that may interact with a drug or drug candidate. Pharmaceutical industry expert Jürgen Drews (now chairman of International Biomedicine Management Partners, Inc. and formerly of Hoffman La Roche) has noted that all drug therapy is currently based on 500 molecular targets. He expects genomics to add thousands of new targets.  

Target in a drug screening context often means drug target. See also target (hybridization).

Narrower terms: disease targets, gene target, tractable targets. Related terms: drug targeting,  target validation; Gene amplification & PCR target (hybridization) 

target amplification: Increasing the amount of target nucleic acid, providing more template for the label, to achieve improved detection. Useful for low levels of expression or abundance or very small sample sizes. Target amplification increases the amount of target nucleic acid, providing more template for the label and therefore more signal. This approach helps overcome problems associated with low expression of some genes or small sample sizes. The kinetics of the amplification step, however, must be reproduced exactly in these approaches; otherwise, changes observed on the array could be the result of differential amplification. Target- amplification processes include PCR, Rolling Circle Amplification RCA, Strand Displacement Amplification SDA.  

Related terms: Gene amplification & PCR

target characterization: Requires evidence that the potential target actually plays a role in the disease process, and that modulation of the target may ameliorate or reverse a disease phenotype. A potential target which may be a validated target. 

Google = about 666, Aug. 24, 2002; about 1,780 June 10, 2004; about 26,100 Nov 13, 2006

Related terms:  target identification, target qualification, target validation

target credentialing: Identification of target molecules, evidence of modification of the target molecule, and measurement of desired effect. [Clinical Radioresistance of Primary Glial Tumors, Radiation Biology, Progress Review groups, National Cancer Institute, NIH, US, 2001 ]http://prg.nci.nih.gov/brain/radiationbiology.html

There are now agents in clinical trial or about to enter clinical trial that have been designed against a specific molecular target. The putative target for a number of these agents has also been associated with radioresistance. Such agents will be evaluated for their ability to modify tumor cell radiosensitivity. Critical to these studies will be the establishing a causal relationship between the agent-induced modification of the target and radiosensitization. This will serve to validate (or invalidate) a given molecule as a target for radiosensitization (target credentialing) and establish a "marker" for the use in the potential design of a clinical trial. Although initial studies will be performed using tumor cell lines and normal cells in vitro, agents found to be effective in vitro will then be evaluated using in vivo models.  Molecular Radiation Therapeutics Branch, National Cancer Institute http://www3.cancer.gov/rrp/mrtb.html 

Google = about 9, Aug. 24, 2002; about 24 June 10, 2004; about 49 Nov 13, 2006; about 71 Oct 8, 2007

target discovery:  Key issues driving growth in this area include the use of model organisms in drug discovery and development, specifically in target discovery and evaluation, drug screening, and preclinical studies. CHA, Cambridge Healthtech Advisors Model Animal Systems: Emerging Applications and Commercial Opportunities in Drug Discovery and Development, report, 2004

Chemical Biology and Chemical Genomic approaches, which utilize specially designed small molecule libraries to explore biology, can address biological questions that are not amenable to genetic manipulation or functional genomics/ proteomics tools and have been gaining wide- spread popularity in both academic and commercial circles.  Developing assays, drug- like libraries of compounds and cells lines to facilitate high- throughput cell- based screening of small organic molecules to identify novel targets and pathways are important tasks.

Google = about 4,960 Aug. 24, 2002; about 14,700 June 10, 2004; about 191,000 Nov 13, 2006; about 187,000 Oct 8, 2007

target discovery in silico: In silico & Molecular modeling

target evaluation: The shift from traditional to genomics-and proteomics-based drug discovery has fundamentally changed the way researchers view the subject of targets. After decades of focusing on a few hundred relatively well-characterized therapeutic targets, drug developers are now finding that the genomics revolution has presented them with the opposite dilemma: thousands of prospective targets about which little is known. Insight Biopharma Reports, Powering Discovery through Target Evaluation: Moving beyond the validation paradigm, 2005 http://www.insightpharmareports.com/reports/2005/52_TargetValidation/overview.asp 

Can cover the range of target- winnowing strategies, from target identification to target validation.

Google = about  1,650, Aug. 24, 2002; about 1,780 Aug. 27, 2003 [not all relevant]; about 2,780 June 10, 2004; about 34,500 Nov 13, 2006; about 38,100 June 25, 2007

target families/target family: Although the sheer numbers of potential targets uncovered through genomics- based methods create an enormous need for target- identification and validation technologies, these numbers also make possible new opportunities, which go way beyond what is possible via traditional drug discovery methods. The limited number of target families addressed by traditional drug discovery methods suggests that these methods are "boxed in" and unable to create the numbers of novel drugs (three to five per year for major companies) that will be necessary to meet pharmaceutical companies' business goals. 

Related terms: Pharmaceutical biology enzymes, g- protein coupled receptors

target gene families: Chemistry chemogenomics

Google = about 95 Nov 13, 2006; about 5,210 June 25, 2007, about 4,370 Oct 8, 2007

target glut:  While an individual company may have four or five times as many targets under analysis now than it did five years ago, most of those targets are completely new or poorly understood. Lack of annotation for genomic data is a major problem in choosing the best targets to pursue for drug development. 

Related terms:  target identification, target screening, target validation; Bioinformatics: information overload; Drug discovery & development druggable genome

target haplotype: Pharmacogenomics

target homology: 

Google = about 400 May 25, 2007

Related terms: RNA,  RNAi

target hopping:  The ability of a certain lead class to interact with multiple members of a target family.  [Chembridge Research Laboratories Collaborations]  http://www.chembridgeresearch.com/collaborations.html

Directed crossover of a compound to a new target. "Chemical genomics advances drug discovery" Genetic Engineering News 22 (13):1 , July 2002 www.messebasel.ch/miptec/ .%5Cpdf%5CGEN_July_Aldridge.pdf

Google = about 27 Aug. 26, 2003; about 30, June 10, 2004; about 70 Apr. 27, 2005; about 485 Nov 13, 2006; about 284 Nov 16, 2007

Related term?:  Assays lead hopping  Chemistry scaffold hopping

target (hybridization):  A molecule (usually a protein gene product, but sometimes a DNA sequence, or, in the case of antisense drugs, an mRNA) that may interact with a drug or drug candidate. [CHI Functional Genomics report]

There are currently at least two nomenclature systems for referring to hybridization partners. Both use common terms ‘probes’ and ‘targets’ … With respect to the nucleic acids whose entwining represents the hybridization reaction, the identify of one is defined - it tends to be tethered to the solid phase, making up the microarray itself. The identity of the other is revealed by hybridization. The strategy of the ‘standard’ microarray therefore parallels that of a reverse dot- blot, in which the probe is immobilized. For this reason, authors of articles appearing in this supplement have been encouraged to describe the tethered nucleic acid as ‘probe’ and the free nucleic acid as ‘target’. [Chipping Forecast supplement "A note on nomenclature" Nature Genetics 21 (1s): 1 Jan 1999] Has this been standardized yet?  See also the note under probes- microarray Microarrays

Instead of target, some people use sample [in the context of microarrays] . We find fault with this usage, though we fall into it occasionally, because the same word often refers to the biological material from which mRNA was extracted (e.g., tissue or serum from patients or laboratory animals). In addition, sample is an important term in statistics, where it has a completely different meaning. (It means the subset of a population that is surveyed for the purpose of estimating properties of the entire population.).

See also target [above] Related terms: Drug discovery & development Sample and sample preparation 

target identification:  Identifying molecules that clearly play a role in a disease process. CHA, Cambridge Healthtech Advisors Model Animal Systems: Emerging Applications and Commercial Opportunities in Drug Discovery and Development, report, 2004

Target identification methods  provide a finer degree of detail than target screening and require evidence that the gene/ protein is correlated with the disease. 

Google = about  14,800, Aug. 24, 2002; about 22,900 Aug. 26, 2003; about 37,600 June 10, 2004; about 494,000 Nov 13, 2006

Related term: RNAi RNA interference

target labelling: Targets for arrays are labelled representations of cellular mRNA pools. Typically reverse transcription from an oligo-dT primer is used … Frequently total RNA pools (rather than mRNA selected on oligo-dT) are labelled, to maximize the amount of message that can be obtained from a given amount of tissue.  DJ Duggan et al “Expression profiling using cDNA microarrays” Nature Genetics 21(1s): 10- 14, Jan 1999

Google Aug. 26, 2003  "target labelling" = about 80; about 136 June 10, 2004; about 530 Nov 13, 2006
 "target labeling" = about 418; Aug 26, 2003; about 943 June 10, 2004; about 19,800 Nov 13, 2006

target molecules: Target genes or target proteins.

Google = about  6,480, Aug. 24, 2002' about 11,300 Aug. 26, 2003; about 21,000 June 10, 2004; about 473,000 Nov 13, 2006 

target prioritization:  Target prioritization is today a bottleneck as a result of the new genomics based drug discovery. Given the exponential increase in targets provided by the new technologies as gene expression analysis, no company can afford to advance all of the targets identified. Our Markets: The Drug Discovery Industry, InNetics http://innetics.com/markets.htm 

Google = about  422, Aug. 24, 2002; about 476 Aug. 26, 2003; about 517 June 10, 2004; about 911 Nov 13, 2006; about 11,000 May 25, 2007

Related terms: Metabolic engineering: networks; Pharmacogenomics 

target product profiles: A tool for planning in the development phase of R&D projects. Insight Pharma Reports, Backup Compound Strategies: Best Practices for Reducing Phase II Risk, 2007 

target proteins:  The project TargId at GMD SCAI focuses on methods to address the arguably most urgent problem: the elucidation of the origins and mechanisms of human diseases, culminating in the identification of potential drug target proteins. Identification of Drug Target Proteins, by Alexander Zien, Robert Küffner, Theo Mevissen, Ralf Zimmer and Thomas Lengauer ERCIM News No.43 - October 2000  http://www.ercim.org/publication/Ercim_News/enw43/zien.html 

Google = about  8,610, Aug. 24, 2002; about 20,000 Aug. 26, 2003; about 36,900 June 10, 2004; about 740,000 Nov 13, 2006, about 863,000 Oct 8, 2007

target qualification: Qualifying that potential target genes or proteins clearly have a role in a disease process.

Google = about  464, Aug. 24, 2002 (not all relevant to pharmaceuticals); about 530 Aug. 26, 2003 (again, not all relevant).

target risks: Drug discovery & Development

target screening: Identifying molecules that may be associated with a disease process (e.g., upregulation of a particular gene identified through gene expression analysis). CHA, Cambridge Healthtech Advisors Model Animal Systems: Emerging Applications and Commercial Opportunities in Drug Discovery and Development, report, 2004

Google = about 799, Aug. 24, 2002; about 1,230 Aug. 26, 2003; about 2,050 June 10, 2004; about 73,600 Nov 13, 2006

Broader term: target, Related terms: target glut, target identification, target validation

target selection: The main purpose of the Bioinformatics Core (BIC) is to select the target for research. The goals of BIC are to develop complete high throughput technology for structural genomics beginning with high throughput computational selection of target proteins, followed by robotic expression and crystallization and fully automated data collection and structure solution. List of Important Definitions, JCSG Joint Center for Structural Genomics http://www.jcsg.org/help/robohelp/Definitions/Target_Selection.htm

target structure:   Protein structure data, in addition to being useful for target evaluation, can also be used to identify and optimize lead compounds, in an approach known as structure-based drug design. In particular, structure-based drug design involves use of structural information describing how a ligand (e.g., a potential drug) interacts with its cellular target in order to design highly specific compounds aimed at those targets. Genomics Provides Crucial Tools for Breaking Bottlenecks in Drug Discovery and Development http://www.healthtech.com/newsarticles/issue11_1.asp

Google = about 8,250 Aug. 26, 2003; about 12,400 June 10, 2004; about 221,000 Nov 13, 2006 [not all relevant]

target validation:  RNAi from target discovery and validation to therapeutic development, Discovery on Target, Oct 25-26, 2007, Boston MA

Target validation involves demonstrating that a molecular target is critically involved in a disease process, and that modulation of the target is likely to have a therapeutic effect. CHA, Cambridge Healthtech Advisors Model Animal Systems: Emerging Applications and Commercial Opportunities in Drug Discovery and Development, report, 2004

Determining which among genes or proteins being investigated as potential drug targets lead to phenotypic changes when modulated, suggesting that they may have value as therapeutic targets. CHI High- Content Analysis Market Outlook report, 2004 

Many people would say a target is truly validated only after proven effective in human trials.  The definition of target validation is clearly evolving, can be seen as "slippery" and clearly means different things to different people. 

Google = about  6,580, Aug. 24, 2002; about 10,300  Aug. 26, 2003; about 17,600 June 10, 2004, about 281,000 April 24, 2006; about 282,000 Nov 13, 2006; about 244,000 May 25, 2007

Related terms: target characterization, target glut, target identification, target screening; Functional genomics: gene function, protein function Pharmaceutical biology antisense; Drug discovery & development hit, lead

target validation- in silico: In Silico & molecular modeling

target validation technologies: A number of technologies including downregulation of gene expression (gene knockdown, antisense, ribozymes and zinc finger proteins), protein inhibition (phage libraries and antibodies), cellular assays, chemical genetics, and combinatorial biology are linked with target validation. The integration of various technologies is another challenge.

Targeted Immunotherapeutics and Vaccines, Aug 21-24 2007, Cambridge MA

targeted mutation: Functional genomics

targeted proteomics: Proteomics categories

targeted therapeutics:  The goal of targeted therapeutics is to create drugs that by the specificity of their design and delivery will make them more effective in treating disease and less toxic.  

therapeutic antibodies: The monoclonal antibody market is one of the fastest growing research areas within the biotech/pharmaceutical industry. Greater than 17 monoclonal antibodies have been approved in the US and European Union for the treatment of immunological, hemostatic, and anti-neoplastic diseases. Last year the PhRMA reported that U.S. companies had approximately 160 monoclonal antibodies in clinical trials or awaiting approval by the FDA. While great advances have been made in the field of monoclonal antibody therapy offering great benefit to patients; hurdles remain. Clinical Development of Therapeutic Antibodies, April 27-May ,2 2008, Boston, MA

tissue biochips: Microarrays categories

tractable targets:  Targets from families such as 7TM receptors, ion channels, kinases and proteases which have produced previous hits.  [Martin J. Valler,  Darren Green  "Diversity screening versus focussed screening in drug discovery " Drug Discovery Today 5(7): July 2000]  

Google = about 175 June 10, 2004; about 586 Nov 13, 2006

Related terms: druggable, low hanging fruits, pharmaceutically tractable

vascular immunotargeting: Vascular immunotargeting is a modern strategy designed for preferential delivery of drugs conjugated with affinity carriers to endothelial cells (1). Several candidate carriers have been proposed, including antibodies directed against angiotensin-converting enzyme, ACE (1, 4, 5), thrombomodulin (6), platelet-endothelial cell adhesion molecule-1, PECAM-1 (7, 8), intercellular adhesion molecule-1, ICAM-1 (9) and caveoli-associated antigens (3, 10). Vascular Immunotargeting to Endothelial Surface in a Specific Macrodomain in Alveolar Capillaries, JUAN CARLOS MURCIANO, D. WIN HARSHAW, LUCIAN GHITESCU, SERGEI M. DANILOV, and VLADIMIR R. MUZYKANTOV , Am. J. Respir. Crit. Care Med., Volume 164, Number 7, October 2001, 1295-1302 http://ajrccm.atsjournals.org/cgi/content/full/164/7/1295

Broader term: immunotargeting

Zebra Fish genomics- target validation: Model & other organisms

Bibliography
Insight Pharma  Model Animal Systems: Emerging Applications and Commercial Opportunities in Drug Discovery and Development, report, 2004
Insight Pharma  Biochemical Pathway and Systems Analysis for Target Identification and Validation report, 2002
Insight Pharma  GPCRs: Mining the Richest Vein in Drug Discovery report, 2003 
IUPAC Compendium of targets of the top 100 commercially important drugs current project 2004-025-1-700 http://www.iupac.org/projects/2004/2004-025-1-700.html 

Alpha glossary index

How to look for other unfamiliar  terms

IUPAC definitions are reprinted with the permission of the International Union of Pure and Applied Chemistry.