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     
Biology  Functional genomics
Chemistry  Libraries & Synthesis
Informatics: In silico & molecular modeling
Technologies Gene amplification & PCR   Genetic Manipulation & Disruption   Microarrays & protein arrays   Molecular Imaging

antisense cleavers & blockers: Pharmaceutical biology

biotherapeutic targets: See ligand binding assays

cellular signaling networks: Metabolic profiling

channel blocker, channel opener: See IUPAC Provisional glossary Biomolecular Screening  See also ion channels

chemical ligand studies: Drug discovery & development

chemogenomics:  British Journal of Pharmacology, 2007 http://www.nature.com/bjp/journal/v152/n1/full/0707308a.html 

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.  http://www.healthtech.com/Conferences/2007/cpf/index.asp 

compound validation: Assays & screening

concept validation: Model & other organisms

copy number variation: SNPs and other genetic variations

Discovery on target  Nov, 2010 - Boston, Massachusetts 

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, about 41,900 June 25, 2009

Broader term: target Related term: drug target

diversity, diversity screening: Drug discovery & development

drug target, drug targets:  How many drug targets are there?, John P Overington, et. al, Nature Reviews Drug Discovery, 2006 http://www.nature.com/nrd/journal/v5/n12/pdf/nrd2199.pdf 

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 "drug target" = about 10,700, Aug, 24, 2002; about 16,500 June 16, 2003; about 33,500 June 10, 2004; about 586,000 Nov 13, 2006, about 513,000 Aug 18, 2008 [typo in 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

efficacy targets: Molecular targets throuogh which the drug mediates its approved therapeutic activities. John P Overington et. al How many drug targets are there? Nature Reviews Drug Discovery, 5 (12): 993-996 Dec 2006 http://www.nature.com/nrd/journal/v5/n12/pdf/nrd2199.pdf 

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- 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: Though G protein-coupled receptors (GPCRs) represent the most common target of drugs on the market, many of those drugs were developed before we knew much about GPCRs. In the past decade scores of GPCRs have been discovered and now we even have crystal structures of a few of these hard-to-express membrane proteins. The new GPCR frontier has opened exciting possibilities for drug development along with a whole set of challenges.  GPCR Based Drug Discovery, Discovery on Target Nov 2010 Boston MA  

Current advances in functional screening methodologies, medicinal chemistry, and structure-based drug design have generated large increases in the number and diversity of GPCR drug targets. Furthermore, basic research advances have opened the way for still further exploitation of this target class. Insight Pharma Reports, GPCRS: Dawn of a new era? 2008

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 (HDACi) are a promising new class of therapeutic agents demonstrating significant efficacy and safety in pre-clinical and clinical studies. In recent years a number of novel and structurally diverse HDACi have been identified and the competition to get to the market has intensified. Although, being tested mainly as anti-tumor agents for cancer, many companies are now starting to explore the use of HDACi for treating CNS, immunology and inflammatory disorders.  . HDAC Inhibitors Discovery on Target Nov 2010 Boston MA  

homology: Functional genomics

hypothetical drug targets:

immunotargeting: 

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

Narrower term: vascular immunotargeting 

ion channels:  Ion Channel Modulator Pipelines  Insight Pharma Reports, September 2009 Table of Contents | Tables and Figures | Executive Summary

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 are now established as an important target group for developing pharmaceutical therapeutics. To successfully move forward in this area, many challenges had to be overcome and several strategies are now in place to validate new targets and to improve and generate new leads. New techniques such as high-throughput screening, new patch-clamp methods, new imaging and updated cell based assays are providing information on new structural leads, on selectivity and on mechanism of action, as well as on emerging new therapeutic areas. I Ion channels as therapeutic targets, Discovery on Target Nov 2010 Boston MA   

kinase inhibitor chemistry: Kinase inhibitors have matured into key targets in drug discovery. They play an important role in cancer therapeutic developments and have recently been established as novel targets for metabolic diseases, pain treatment and CNS therapeutics.  While a lot of knowledge is available about the biology of kinases, what the industry needs now is to explore the chemical space.  More information on the structure, binding sites and binding interaction of kinases is necessary in order to optimize leads and to develop novel inhibitors.
Kinase Inhibitor Chemistry April 28-29, 2010 • San Diego, CA Program | Register | Download Brochure  

kinase inhibitors:  Next-Gen Kinase Inhibitors - Oncology and Beyond June 21-23, 2010 • Cambridge, MA Program | Register | Download Brochure

kinase therapeutics: The number of kinase inhibitors entering clinical development has increased significantly in recent years. In addition to major pharmaceutical and biotech companies, an increasing number of emerging companies are focusing on their development. By 2020, small-molecule kinase inhibitors could generate annual revenues > $25 billion. Kinase Therapeutics: Pipeline Assessment and Commercial Prospects January 2010

Related terms:  kinase inhibitors, protein kinases

molecular drug targets: Current Drug Targets aims to cover the latest and most outstanding developments on the medicinal chemistry and pharmacology of molecular drug targets e.g. disease specific proteins, receptors, enzymes, genes. Current Drug Targets scope note, Bentham Science http://www.bentham.org/cdt/index.htm 

Disease associated genes or proteins.

Google = about  82, Aug, 24, 2002; about 201 June 10, 2004; about 2,060 Nov 13, 2006, about 938 Aug 17, 2008

Molecular Pharmacopeia http://www.nature.com/focus/molecularpharmacopoeia/sponsors/index.html 

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: Drug discovery & development

nuclear hormone receptor modulators: 

See also receptors, cytoplasmic and nuclear

oligonucleotide based therapeutics: 

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. Targeting Pain with Novel Therapeutics part of the World Pharmaceutical Congress, May  2009 Philadelphia PA

pharmacology driven assays for current targets: Drug discovery scientists need to get more from their assays and their data. The availability  of multidimensional assays, new  information regarding the pharmacology  of compound/target relationships, and balancing the need for high content with the speed of high throughput are all concerns for the drug discovery scientists. 
Pharmacology Driven Assays for Current Targets June 16-17, 2010 • Philadelphia, PA Program | Register | 

phosphoinositide 3 kinase PI3K:  Phosphoinositide 3-kinases  (PI3K) are major therapeutic targets  in developing tumor treatments, due to their influence of  various signaling pathways and cell functions such as cell growth.  In the last few years, new applications for non-tumor related diseases are slowly emerging. Discovery on Target  Advances in Targeting Phosphoinositide 3 Kinase (PI3K) Pathways  November 2-3, 2010 • Boston, MA

predictive biosimulation: In Silico & Molecular Modeling

protease inhibitors:  Proteases constitute one of the largest potential drug target enzyme families, with 647 human gene products incorporating protease sequences and mutated proteases having been identified.  In addition, there are many more proteases found in viruses, bacteria, and parasites, which are also potential drug targets. The therapeutic promise of protease inhibitors has been most clearly demonstrated by angiotensin-converting enzyme (ACE) and HIV drugs.  Developments reviewed in this report indicate that more protease inhibitors, several having significant commercial potential, will reach the market over the next three to four years. Insight Pharma Reports, Protease inhibitors: Innovation drives drug pipeline, 2009 

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  

Targeting kinase inhibitors and developing novel drug designs has become very attractive for the pharmaceutical industry. Numerous drugs are in phase 3 and beyond and due to the complexity of the kinome, there are still many opportunities for developing novel inhibitors.  Protein Kinase Targets: Drug Discovery & Design June 2009 Cambridge MA  

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

putative drug targets: 

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 

RNAi  interference: Genetic Manipulation & Disruption

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:  Medicinal  chemistry of targeted directed masterkeys, Drug Discovery Today, 2003  doi:10.1016/S1359-6446(03)02781-8   

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

http://www.nigms.nih.gov/News/Reports/psi_targetselect.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:  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. 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 credentialing, 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 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 Targets Database: http://xin.cz3.nus.edu.sg/group/cjttd/ttd.asp  Computational Science Dept, Science Faculty, National University of Singapore 

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, thrombomodulin, platelet-endothelial cell adhesion molecule-1, PECAM-1  intercellular adhesion molecule-1, ICAM-1 and caveoli-associated antigens  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
Cytokine Therapeutics: A Vibrant Pipeline and Active Approved Market Full Report | Executive Summary  Feb 2007
GPCRs: Dawn of a New Era? Full Report | Executive Summary  Oct 2008
Ion Channel Modulators  2009 August
Kinase Therapeutics: Pipeline Assessment and Commercial Prospects January 2010
Protease Inhibitors: Innovation Drives Drug Pipeline Full Report | Executive Summary Feb 2009
Insight Pharma Reports, RNAi therapeutics 2005     Target evaluation: Moving beyond target validation, 2005
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
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.