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aptagen - aptamers
Who We Are

Aptagen, LLC is a global leader in aptamer development with over 25 years of experience generating high affinity and specifically-binding aptamers for small molecules, proteins, cells, and tissues. We produce state-of-the-art target-recognition elements for diagnostics, therapeutics, and bio-industrial applications. Explore above to learn more about how aptamers can help you!

Top companies put their trust in us as we continue to exceed expectations.

penn state
IBM
harvard
nestle
genentech
merck Merck Sharp & Dohme
medimmune
md_anderson_cancer_center
gene link
general electric
covidien
cephalon
biogen_idec
bio_rad
heavy

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Our Process

  • How we work
How we work
Phase 1: Screening/Selection
Description
Target Type

Iterative rounds of screening an initial random library against a target for positive selection, and counter-selection against a counter-target for specificity. 


Client Materials: Please note that the Client will need to provide the target(s) for Aptagen. It is highly recommended that countertarget(s) is also provided for enrichment of highly specific apta-sensors. A Material Acquisition Form must be completed for background information on the target, any associated hazards, and handling requirements.

Small Targets: Small Molecules or Peptides


Large Targets: Proteins, Biomarkers, Cells, Tissues


Deliverable: The most promising monoclonal apta-sensor candidates are identified using proprietary bioinformatics. A full Progress/Analysis Report on a handful of the most likely candidates based on sequence homology, frequency, and motif analysis.

Small Molecules or Peptides

Proteins or high MW Biomarkers

Cell Based

Ex Vivo (tissue)

Whole Animal

thin
Phase II: Sequencing and Bioinformatics
Description
Deliverable

The enriched polyclonal pool is sequenced and thousands of apta-sensor sequences are provided. Client will have access to all the data generated from the polyclonal apta-sensor pool in Phase I (hundreds to thousands of sequences).

Deliverable: The most promising monoclonal apta-sensor candidates are identified using proprietary bioinformatics. A full Progress/Analysis Report on a handful of the most likely candidates based on sequence homology, frequency, and motif analysis.

Phase III: Synthesis of Candidates
Description
Deliverable

Monoclonal apta-sensor oligo candidate(s) are synthesized, purified, and QC. Projects are typically based on unmodified apta-sensors.

Note: This Phase is at the Client’s discretion whether Aptagen performs the work or is performed by another provider.

Deliverable: 1 nmole of purified apta-sensors for Phase IV

Phase IV: Validation of Candidates
Description
Assay Type

Each tested for assessing Kd affinities, signal-to-background, LOD, targeting, or EC50/IC50, etc..

Note: This Phase is at the Client’s discretion whether Aptagen performs the work or is performed by another provider.

ForteBio, Thermophoresis, Dot Blot, Gel-shift assay, or ELONA (ELISA), Microscopy, Flow Cytometry, or Imaging, etc

Deliverable: Full Report on Kd Affinities and Specificities.

Phase V: Optimization (optional)
Description
Deliverable:

At the Client’s discretion, Aptagen may ‘multimerize’ apta-sensors to further enhance functional properties of apta-sensor candidate(s) while truncating or minimizing the length of the oligo to reduce large-scale manufacturing costs and processing time downstream. Aptagen’s proprietary in silico algorithm searches and explores ‘sequence space.’  Inquire. Project specific. The Optimization Phase may not be necessary for research purposes. This phase entails truncation of apta-sensor oligos to reduce production costs for commercialization or ‘multimerization’ of apta-sensors to further increase affinity/avidity. This Phase may trigger only if Client believes Optimization a) is cost effective to minimize production costs while maximizing activity for large-scale commercial use and/or, b) widens the claims in Client’s IP to strengthen the coverage of all possible apta-sensor sequence variants.

Deliverable: Full Report on Kd Affinities

and Specificities. Aptagen validates

monoclonal candidates.

At least one (1) aptamer candidate must

meet Anticipated Milestone Outcome.

Order from nearly 500 different Aptamers.

Apta-index

CELL-TARGETING APTAMER LIGANDS!

Click here to obtain a quote for R&D Project

Brochures:

Perspective_Aptamers_as_Drugs.pdf (103.9 KB)

Aptabody_Narrative.pdf (136.5 KB)

Aptagen_Selection_Data.pdf (331.2 KB)

The Problem: Drug candidates that prove positive in “test tube” (or in vitro) assays may face substantial problems when tested in animals, a necessary prerequisite before human clinical trials. These problems include absorption, distribution, metabolism, excretion, and toxicity.

The Solution: Aptagen’s technique, involving molecules called aptamers, overcomes the limitation of the traditional pharmaceutical drug discovery process. The unique chemistry of modified aptamers, unlike other forms of drugs currently used, permits the selection of drug candidates in whole animal models, bypassing the “test tubes” entirely, and taking drug development one step closer to human clinical trials. By using an animal model with the disease state of interest, specific knowledge of the pathology or disease condition is not needed. An added benefit is the significant reduction in the number of animals needed for drug evaluation before entering into human clinical trials.

Using the current antibody method; for every drug that makes it to market, hundreds of promising candidates that worked in-vitro (on the lab bench) fail during animal ADMET studies (absorption, distribution, metabolism, excretion, and toxicity). From lab bench to pharmacy shelves it takes from seven to fifteen years and costs $4B with an average failure rate of 80%. Half of this time and approximately 70% of all associated biopharmaceutical R&D costs are spent on in-vitro development.

Because aptamers (synthetic antibodies) are an in-vivo (directly tested in the animal model) approach, they avoid the majority of the bench testing, saving several years and approximately 35% of the R&D cost. The unique chemistry of aptamers, unlike other forms of drugs currently used, permits the natural selection of drug candidates in whole animal models, bypassing the test tube entirely. By using an animal model with the disease state of interest, Aptagen need not possess specific knowledge of the pathology or disease condition in question. As an added benefit, because this approach reduces the false starts, there are actually fewer animals needed for drug evaluation.

Aptamers are biorecognition elements or ligands that bind with high affinity and specificity to virtually any target or antigen on cells, tissues, and within biological fluids. But what if the identity of the target, antigen, or biomarker is unknown? If provided with a set of samples considered positive and a separate set of samples considered negative based on a clinical diagnosis, aptamers can be selected to respond specifically to the positive set of samples over the negative, even though the biomarker is not known.  However, by employing these positive-responsive aptamer ligands in a pull-down assay, followed by mass-spec analysis, the ‘positive biomarker(s)’ can be identified.

WHAT ARE APTAMERS?

Aptamers (synthetic antibodies) are stable DNA or RNA ligands that bind with high affinity and specificity to target antigens such as small molecules, peptides, proteins, cells, and tissues. For example, aptamers have been generated that exhibit greater than 10,000-fold binding affinity for theophylline over caffeine, which differ only by a few atoms. Aptamer products can be used as research agents, diagnostics, biosensors, and tools for biomarker or drug discovery. Aptamers can also be used for bioindustrial applications and targeted therapeutics.

Antibody problems? Have difficult targets to develop effective ligands or antibodies? What if an antibody doesn’t exist for your target or antigen? 

No problem. Let Aptagen provide you with an alternative – the aptamer. You’ve heard about this new technology. Now, try it.

What is an APTABODY?

An aptabody™ is a supramolecular form of an aptamer ligand containing a wide variety of functional groups. The aptamer component acts as a scaffold to hold into place one or more functional groups such as amino acids, fatty acids, carbohydrates, small molecules and/or metals in a unique orientation in 3-D space.


The order and proximity of these functional groups play a role in enhanced functionalities ranging from higher affinity and specificity over “naked” aptamers, to enzyme biomimetics, improved molecular targeting in vivo, cellular trafficking, pharmacokinetics/dynamics, and drug-like properties.

NOTE: Conventional antibodies have a chemical alphabet of the naturally occurring amino acids. Aptabodies™, by definition, have a chemical alphabet of all amino acids, fatty acids, as well as synthetic compounds, co-factors, metal ions, etc…

RAPID APPROACH TO DRUG DISCOVERY!

From lab bench to pharmacy shelves, drug discovery takes up to fifteen years and costs $4B with an average failure rate of 80%. Half of this time and approximately 70% of all associated biopharmaceutical R&D costs are spent on in-vitro development alone.Over a century ago, Paul Ehrlich described the ideal drug, famously known as a ‘magic bullet,’ in which it specifically targets the disease site and would not harm healthy tissue. Aptagen has developed the concept of a ‘replicating magic bullet’ called an aptamer. Aptamer technology has a shorter development time compared to traditional methods, and can be used to increase the specificity and improve delivery of existing drug compounds resulting in the next generation of pharmaceuticals with improved pharmacodynamics and pharmacokinetics.The unique chemistry of aptamers, unlike other forms of drugs currently used, permits the natural selection of drug candidates in whole animal models, bypassing the test tube entirely, saving several years and approximately 35% of the R&D cost. By using an animal model with the disease state of interest, Aptagen need not possess specific knowledge of the pathology or disease condition in question. As an added benefit, because this approach reduces the false starts, there are actually fewer animals needed for drug evaluation.

Aptagen’s rapid fast-track approach to drug discovery bypasses the ‘test tube’ in pre-clinical development, taking it one step closer to human clinical trials. In Vitro Assays  —–>  In Vivo Studies  ——>  Clinical Trials

The Problem: Drug candidates that prove positive in “test tube” (or in vitro) assays may face substantial problems when tested in animals, a necessary prerequisite before human clinical trials. These problems include absorption, distribution, metabolism, excretion, and toxicity.

The Solution: Aptagen’s technique, involving molecules called aptabodies™ (patent pending), overcomes the limitation of the traditional pharmaceutical drug discovery process. The unique chemistry of aptabodies™, unlike other forms of drugs currently used, permits the selection of drug candidates in whole animal models, bypassing the “test tubes” entirely, and taking drug development one step closer to human clinical trials. By using an animal model with the disease state of interest, specific knowledge of the pathology or disease condition is not needed. An added benefit is the significant reduction in the number of animals needed for drug evaluation before entering into human clinical trials.

BENEFITS: overcome delivery issues * * identify unknown biomarkers * * tailor PK/PD properties * * rescue failed drug candidates from targeting/specificity issues .

Spending too much time and capital on the trial-and-error approach to Drug Discovery? On average, only one in a thousand drug candidates make it to human clinical trials. The cost and time associated with the traditional method of drug development is expensive and quite slow (7 to 15 years and almost $1 Billion). However, Aptagen’s technology significantly reduces the unpredictability, cost, and time for drug discovery and development.

Over a century ago, Paul Ehrlich described the ideal drug, famously known as a ‘magic bullet,’ in which it specifically targets the disease site and would not harm healthy tissue. However, finding these magic bullets with drug-like properties involves a trial and error approach and is extremely slow. Aptagen has developed the concept of a ‘replicating magic bullet’ called an aptabody™. The aptabody™ technology has a shorter development time compared to traditional methods of drug development, and can be used to increase the specificity and improve delivery of existing drug compounds resulting in the next generation of pharmaceuticals with improved pharmacodynamics and pharmacokinetics.

Brochures

AptagenDrugDevelopmentServices.pdf (2.1 MB)

Cost-BenefitChart.pdf (734.1 KB)

Apta-beacons & Apta-sensors

NO CAPTURING. NO WASHING. JUST READ… IN MINUTES!

Aptagen’s “No Capturing. No Washing. Just READ” assay is a radical advancement in diagnostic technology. Aptagen, LLC has developed a sensitive diagnostic platform that can detect virtually any target or antigen (from small molecules to protein biomarkers and cells) in a variety of sample matrices. Unlike current diagnostic formats, such as the traditional ELISA method and the more recently popular Luminex® approach, Aptagen’s Apta-Beacon™ assay eliminates the need for multiple target manipulation steps.

The Apta-Beacon™ platform requires neither capturing nor washing of sample(s), streamlining the analysis to quickly provide results with higher sensitivity.

The demo kit showcases the specificity of the colorimetric assay by detecting difficult small molecule targets, theophylline versus caffeine, which only differ by a single methyl group. The assay is also available in a fluorescent format for greater sensitivity.

Order kit

Apta-Beacon (GQ-EXPAR, TMB) Demonstration Kit

What Are Peptimers™?

Peptimers™ are peptide-based aptamers: high affinity ligands composed of amino acid building blocks instead of the nucleic acid bases that make up RNA or DNA aptamers.  Peptimers™ are another option offered by Aptagen to continually ‘Advance Aptamer Applications’. 

Unlike single-chain antibodies generated by the phage display or biopanning process, peptimers™ are discovered through a process similar to aptamer SELEX, called mRNA display.

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