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Study of ocular pharmacology, pharmacodynamics, and toxicology is challenging due to the inherent ocular barriers to drug penetration, small ocular tissue sizes and volumes, and sensitive ocular structures. Additionally, wide variation of ocular sizes and physiology among anim ...

Ocular diseases such as glaucoma and macular degeneration can greatly impact the quality of patients’ lives, with the possibility of loss of vision. The development of orally available drugs that can reach the posterior segment of the eye is hampered by the anatomy of the eye. In this chapter, we desc ...

Using biodegradable polymeric nanoparticles as model systems for drug and gene delivery, this chapter describes commonly used methods for preparing and characterizing nanoparticles. This chapter focuses on emulsion solvent evaporation-based methods for encapsulating ...

The unique anatomy and physiology of the eye make it a highly protected organ. Drug delivery to the eye has become a major challenge to ocular pharmacologists and drug delivery scientists. Designing an effective therapy for ophthalmic disorders, especially for the chronic posterior segm ...

The MIMETIBODY™ platform was developed to expand the opportunities for application of biotherapeutics. While the utility of antibodies as antagonists has been well demonstrated, their application as agonists has been more challenging. For steric reasons, antibodies may be less we ...

Regulatory proteases modulate proteomic dynamics with a spectrum of specificities against substrate proteins. Substrate phage display is one of the key methodologies in producing substrate sequence information in vitro. Factor Xa, a key regulatory protease in the blood coagula ...

Recent use of hetero-dimerization to improve the affinity of peptide ligands has made peptides an attractive alternative to small molecules and proteins. Using this strategy, we have developed peptides with affinities comparable to antibodies and specificities often better than ...

Recent successes in the development of small-molecule antagonists of protein–protein interactions designed based on co-crystal structures of peptides bound to their biological targets confirm that short peptides derived from interacting proteins can be high-value ligands ...

Display of peptides on filamentous phage, phage display, is an in vitro selection technique well suited for identification of therapeutic peptide binders for a huge variety of protein targets. The peptides are identified in a process where phage libraries are subjected to affinity selec ...

In this chapter, we describe the construction of T7 bacteriophage (phage)-displayed peptide libraries and the diversity analyses of random amino acid sequences obtained from the libraries. We used commercially available reagents, Novagen’s T7Select system, to construct the lib ...

Peptides are increasingly emerging as human therapeutic drugs. By screening very large phage display libraries, novel bioactive peptides that bind to the target of interest with desired biological properties can be identified. Peptides that are obtained in this fashion become the ba ...

The concept of phage display is based on insertion of random oligonucleotides at an appropriate location within a structural gene of a bacteriophage. The resulting phage will constitute a library of random peptides displayed on the surface of the bacteriophages, with the encoding genoty ...

Cystine-stabilized mini-proteins are important scaffolds in the combinatorial search of binders for molecular recognition. The structural determinants of a cystine-stabilized scaffold are the critical residues determining the formation of the native disulfide-bond ...

Fourier transform infrared (FTIR) spectroscopy provides data that are widely used for secondary structure characterization of peptides. A wide array of available sampling methods permits structural analysis of peptides in diverse environments such as aqueous solution (incl ...

Circular dichroism measures the difference between the absorbance of left- and right-handed circularly polarized light, and can be used to monitor the secondary structure of peptides (far UV) and the tertiary structure of larger polypeptides (near UV). This technique is especially use ...

In peptides, steady-state fluorescence can be used to measure the intrinsic fluorescence of Trp, Tyr, and Phe residues, as well as associated dyes, which can change upon exposure to different environmental conditions. This technique can be thus used to detect changes in the conformational s ...

UV absorption spectroscopy is commonly used with peptides for determining concentration and enzyme activity, but high-resolution UV spectra can also provide information on peptide secondary and tertiary structure and association behavior. New developments using tempera ...

Protein prenylation involves the addition of a farnesyl (C15) or geranylgeranyl (C20) isoprenoid moiety onto the C-terminus of approximately 2 % of all mammalian proteins. This hydrophobic modification serves to direct membrane association of the protein. Due to the finding that the on ...

Peptides are highly selective, high-affinity ligands for a diverse array of disease targets, but suitably derivatizing them for application as diagnostic or therapeutic agents often presents a significant challenge. Covalent modification with metal chelates frequently res ...

The main goal in modern biomedicine is to develop specific diagnostic and therapeutic agents for different diseases. Especially in cancer research tumor targeted molecules are the key factor in the development of new anti-tumor drugs. In addition, the early diagnosis of the disease is an imp ...