Search results for: 'proteas'

To address both chemical and IP considerations in self-immolating linker applications , we propose shifting from the commonly used Val-Cit-PAB linker to the less explored Gly-Gly-Phe-Gly-formyl motif.

You missed our workshop featuring Prof. Thierry Brigaud? Watch the Recording!

Use the possibilities of Linkerology® to boost the efficacy of your drug! We illustrate how the drug Gepirone (Exxua TM ), a medication to treat major depressive disorders, can be conjugated.

Discover photocages – photosensitive protecting groups that are removed by irradiation with light of a defined wavelength, thus restoring the original, “active” state.

Have an additional ace up your sleeve for selective and efficient peptide modification, cyclization, and/or bioconjugation. Explore 2-cyanopyridines for click-like reactions. Get more information!

Beyond cysteines: Unlock targeted side-chain modifications of your peptides and proteins via the introduction of 1,2-aminothiols and subsequent click-like functionalization. 

The targeted delivery and traceless release of drugs is an important concept in pharmacology. Discover the possibilities of payload conjugation to carrier proteins shown for the example drug Elacestrant.

Are you keen on developing novel billion-dollar-selling peptide API blockbusters? Most recent ones use lipophilic Albumin binding moieties. Of course, Iris Biotech has the necessary building blocks!

One molecule, two identities: PNAs are composed of nucleobases arranged on a peptidic backbone. Discover our PNA building blocks as ready-to-use bases suitable for SPPS.

You want to attach your small molecule to a certain carrier? Let’s analyze the functional groups present and discuss Linkerology® possibilities for permanent or trigger-inducible, tracelessly-cleavable linkage.

Discover the cyanobenzothiazole (CBT) click reaction , a not (yet) so well-known biocompatible and bio-orthogonal mechanism faster than the famous azide-alkyne cycloaddition (CuAAC).

Our building block Fmoc-L-Cys(Cam)-OH enables peptides resembling reduced and carbamido-methylated protein fragments by standard SPPS without error-prone modification reactions.

Shine bright like our fluorophores! Learn how our superior fluorogenic protease substrate peptides can enhance your test performance. Click here to gather more information and discover available products!

Peptide therapeutics – fewer injections/lower doses by prolonging their half-life via addition of a lipid modification that promotes binding to serum proteins such as albumin. Read on for recent innovations!

Non-canonical Tryptophan analogs can help to improve your API’s performance in terms of potency, specificity, and stability. We offer various substituted Trp derivatives also available in small quantities for screening.

Maleimides provide versatile options for connecting payloads to proteins and other biomolecules. Discover how our bifunctional thiol reactive crosslinkers can support your project. Read on!

Linkers serve as versatile tools, e.g. during SPPS or for the sophisticated (self-immolative) conjugation of a potent small molecule to a carrier. Check out our selection of over 100 readily available linkers.

Dyes and fluorescent labels are an invaluable tool for diagnostics, medical and biochemical research. Iris Biotech offers labels with excitation ranges from UV to near-IR and various functional groups.

Drug the undruggable – click here to get more information about the use of PROteolysis TArgeting Chimeras (PROTACs®) as a tool for targeted protein degradation and discover available building blocks.

Iris Biotech offers the main building blocks for the synthesis of Liraglutide and Semaglutide and commonly observed impurities as well as reference standards. Read on for more information!

Interested in the introduction of Sarcosine (N-methylglycine), e.g. for hydrophilicity increase of your derivative of choice or for PEG replacement? Check-out our available Sarcosine building blocks!

Herein we are presenting 2-(Fmoc-amino)-3,3-diMe-pent-4-enoic acid (FAA5040), a protease stable Ile/Leu surrogate suitable for further modification via its side chain double bond.

The peptide-based ADC linkers Val-Cit and Val-Ala are efficiently cleaved by lysosomal proteases and benefit from increased serum stability and effective payload-release in targeted cells.

With the approval of several COVID-19 vaccines and drugs in recent months, hope is growing that the current pandemic will end soon.

Read on to find out more about Iris Biotech’s Linkerology® portfolio including substituted pyridyldithiols as building blocks for the reversible chemical conjugation to sulfhydryls.

The highly lipophilic, bulky adamantyl motif is a promising and validated building block to increase the drug-qualities of lead compounds without increasing their toxicity.

The new disulfide-based protecting group sec-isoamyl mercaptan (SIT) is fully compatible with Fmoc- and Boc-SPPS and can easily be removed reductively upon addition of dithiothreitol.

Enzymatically-activatable probes based on 7-amino-4-methylcoumarin (AMC) represent versatile tools for the detection and localization of proteolytic enzyme activities. Read on to find out more.

One approach for the design of bioactive peptides with improved pharmacological properties is the derivatization of amino acid building blocks with fluorine. Find out more about the advantages of fluorinated peptides.

Mpro is a key enzyme of coronaviruses (coronaviridae) and thus an attractive drug target. Iris Biotech offers fluorescent substrates, which can be used to perform various types of screenings and to identify potential inhibitors of COVID-19.

Iris Biotech presents its selection of Val-Cit-based linkers, a dipeptide motif frequently utilized for the development of ADCs with increased serum stability and high cleavage efficiency.

Iris Biotech presents (functionalized) fullerenes of different core size (C60 vs. C70) as versatile tools for multiple functionalization. Read more about their unique properties and fields of applications.

Sidechain-derivatized amino acids have shown great potential in enhancing select properties of peptide lead compounds. Find the most recent additions to our portfolio of amino acids bearing additional aryl and alkyl groups in their side chains.

Protease inhibitors are molecules that inhibit protease function by binding either reversibly or irreversibly to the enzyme.

The use of bioactive peptides has increased over the recent years as they attracted attention for their use as therapeutic agents.

α-Methyl and alkyl-amino acids can be produced by a number of platforms, where the (2S,4S)-4-methyl-2-phenyloxazolidin-5-one scaffold is one of the most popular one.

The incorporation of trifluoromethyl group carrying building blocks into peptides results in increased chemical and thermal stability, increased resistance to degradation by proteases, and enhanced lipophilicity.

Trypsin (EC 3.4.21.4), an endopeptidase and natural protease found in the digestive system, cleaves peptide chains and proteins predominantly at the carboxyl side of the amino acids Lys and Arg (except when followed by Pro).

The polymers in this context are a polymeric linear structures with n repeating units of monomers. Depending whether the polymer is consisting of one single molecular weight (only one n existing) or of a range of compounds with an average mass and a distribution of n around a mean value, polymers are referred to as “monodisperse” or “polydisperse”.

Polyglutamates are well known to be highly biocompatible, biodegradable and multifunctional polymers, which have already been used as building blocks in polymer drug conjugates and polymeric micelles.

Small drug molecules and also large biomolecules like proteins or antibodies suffer rapid clearance from human body.

The classic FRET pair EDANS and DABCYL is now available linked to Fmoc amino acid building blocks that can be readily used in SPPS. Conveniently synthesize your own custom protease substrates!

Asymmetric Rhodamine 110 protease substrates are used for the determination of protease kinetics. The asymmetric structure of these dyes greatly simplifies the determination of enzyme kinetics, while the properties of Rhodamine 110 facilitate an uncomplicated readout.

The Fmoc-L-Phe-Aca pseudo-dipeptide is a useful reporter group for the successful internalization of CPPs. Phe quenches the fluorescence of Aca. Internalization of the peptide containing Phe-Aca leads to proteolytic cleavage of the Phe-Aca bond and thus to fluorescence.

Surprising behavior of NXO-peptides. It is a significant property of peptides that oxalo-retro azapeptides have the same donor and acceptor distances and properties for hydrogen bridge formation as a tripeptide fragment and therefore induce beta-sheet formation at this position.

Cleavable dipeptide linkers like Val-Ala and Val-Cit rely on processes inside the cell to liberate the payload, as they undergo rapid hydrolysis in the presence of lysosomal extracts or purified human cathepsin B.

Aminoisobutyric acid (Aib) and its homologues are a strong helix promoters in peptide mimetics. Aib-containing model peptides are already used in cancer treatment, antimicrobial peptides and cell penetrating peptides (CPP). We offer Aib and its homologues positioning the dimethyl fragment either close to the N- or to the C-terminus.

1,4-substituted 1,2,3-triazole are isosteric to peptide bonds and result in peptide mimetics which even retain activity e.g. in case of certain tyrosinease inhibitors. We offer custom synthesis of Alkyne Amino Acid Analogues as building blocks for triazol formation via Click conjugation. Side chains can represent all natural amino acids or unusual residues. In combination with our alpha-azido acids we can offer the whole range of building blocks to design Click-peptide bond analogues for every proteinoge...

GABA is a neurotransmitter in the central nervous system of mammals and its deficiency is associated with severe neurological disorders. Statine, a GABA analogue, occurs in several peptide APIs. Derivatives of gamma-amino acid analogues are of continued vital interest for a variety of applications in medicinal chemistry. We have a tool box available to offer a broad range of substituted gamma-amino acids and statines on custom synthesis basis.

September 2nd - 7th, 2012 Athens, Greece Megaron Conference Centre   With more than 550 submitted abstracts and more than 500 already registered participants coming from more than 40 different countries, the 32nd European Peptide Symposium assures an exciting scientific program.

Abstract: A considerable number of biologically active naturally occurring products are peptides, depsipeptides, and peptide conjugates.