Gaining Insights into Specific Drug Formulation Additives for Solubilizing a Potential Anti-Alzheimer Disease Drug B4A1.

The pharmacological profiles of small molecule drugs are often challenged by their poor water solubility. Sequence-defined peptides attached to poly(ethylene glycol) (PEG) offer opportunities to overcome these difficulties by acting as drug-specific formulation additives. The peptide-PEG conjugates enable specific, noncovalent drug binding via tailored peptide/drug interactions as well as provide water solubility and drug shielding by well-solvated PEG-blocks.

λ-Orthogonal pericyclic macromolecular photoligation.

A photochemical strategy enabling λ-orthogonal reactions is introduced to construct macromolecular architectures and to encode variable functional groups with site-selective precision into a single molecule by the choice of wavelength. λ-Orthogonal pericyclic reactions proceed independently of one another by the selection of functional groups that absorb light of specific wavelengths. The power of the new concept is shown by a one-pot reaction of equimolar quantities of maleimide with two polymers carrying different maleimide-reactive endgroups, that is, a photoactive diene (photoenol) and a nitrile imine (tetrazole).

Ambient temperature ligation of diene functional polymer and peptide strands onto cellulose via photochemical and thermal protocols.

In the present contribution, two novel ambient temperature avenues are introduced to functionalize solid cellulose substrates in a modular fashion with synthetic polymer strands (poly(trifluoro ethyl methacrylate), PTFEMA, Mn = 4400 g mol(-1) , Đ = 1.18) and an Arg-Gly-Asp (RGD) containing peptide sequence. Both protocols rely on a hetero Diels-Alder reaction between an activated thiocarbonyl functionality and a diene species.

Spatially controlled photochemical peptide and polymer conjugation on biosurfaces.

An efficient phototriggered Diels-Alder conjugation is utilized to graft in an effective and straightforward approach poly(trifluoro ethyl methacrylate) (Mn = 3700 Da, Đ = 1.27) and a model peptide (GIGKFLHS) onto thin hyaluronan films and cellulose surfaces. The surfaces were functionalized with an o-quinodimethane moiety - capable of releasing a caged diene - via carbodiimide mediated coupling.