Bhagwanth, Swapna Mishra, Ram K Johnson, Rodney L
Published in
Beilstein journal of organic chemistry
A variety of stable, small-molecule peptidomimetic ligands have been developed to elucidate the mechanism by which the neuropeptide Pro-Leu-Gly-NH(2) (PLG) modulates dopaminergic neurotransmission. Photoaffinity labeling ligands based upon PLG peptidomimetics have been used to establish that PLG binds to the D(2) dopamine receptor at a site that is...
McMurray, John S Mandal, Pijus K Liao, Warren S Klostergaard, Jim Robertson, Fredika M
Published in
JAK-STAT
Herein we review our progress on the development of phosphopeptide-based prodrugs targeting the SH2 domain of STAT3 to prevent recruitment to cytokine and growth factor receptors, activation, nuclear translocation and transcription of genes involved in cancer. We developed high affinity phosphopeptides (K I = 46-200 nM). Corresponding prodrugs inhi...
Foy, Kevin C Miller, Megan J Moldovan, Nicanor Carson, William E 3rd Kaumaya, Pravin T P
Published in
Oncoimmunology
Overexpression of HER-2 and VEGF plays a key role in the development and metastasis of several human cancers. Many FDA-approved therapies targeting both HER-2 (Trastuzumab, Herceptin) and VEGF (Bevacizumab, Avastin) are expensive, have unacceptable toxicities and are often associated with the development of resistance. Here, we evaluate the dual an...
Nieto-Ortega, Belén Nebot, Vicent J Miravet, Juan F Escuder, Beatriu Navarrete, Juan T López Casado, Juan Ramírez, Francisco J
Published in
The journal of physical chemistry letters
We elucidate the supramolecular organization in the form of microsize fibrils of gels formed by a l-Valine peptidomimetic compound. Analysis was based on circular dichroism spectroscopies, vibrational (VCD) and electronic (CD), supported by microscopy (atomic force and scanning electron). We show how the VCD spectra give account of the micrometric ...
Conn, P. Jeffrey Kuduk, Scott D. Doller, Darío
Published in
Annual Reports in Medicinal Chemistry
Terms such as “nondruggable GPCRs” describe a unique group of GPCRs having strong biological hypothesis validation, but for which medicinal chemistry efforts based on orthosteric ligands have failed to produce marketed drugs (or even clinical development candidates). These receptors remain attractive as biological targets for new drugs, but a novel...
Banerjee, A Yadav, A
Published in
International journal of biomedical science : IJBS
Ab initio molecular orbital calculations at the Hartree Fock level utilizing 6-31G basis set have been performed on small cyclic peptides and peptidomimetic compounds to explore their utility as carriers of levodopa (L-3,4-dihydroxyphenylalanine) to enhance its brain bioavailability. A cyclic peptidomimetic compound with hydrophobic CH2NH backbone ...
Gulevich, Anton V Koroleva, Lyudmila S Morozova, Olga V Bakhvalova, Valentina N Silnikov, Vladimir N Nenajdenko, Valentine G
Published in
Beilstein journal of organic chemistry
The synthesis of new, artificial ribonucleases containing two amino acid residues connected by an aliphatic linker has been developed. Target molecules were synthesized via a catalytic three-component Ugi reaction from aliphatic diisocyanides. Preliminary investigations proved unspecific nuclease activity of the new compounds towards single-strande...
Chorell, Erik
New strategies are needed to counter the growing problem of bacterial resistance to antibiotics. One such strategy is to design compounds that target bacterial virulence, which could work separately or in concert with conventional bacteriostatic or bactericidal antibiotics. Pilicides are a class of compounds based on a ring-fused 2-pyridone scaffol...
Salomé, N Hansson, C Taube, M Gustafsson-Ericson, L Egecioglu, E Karlsson-Lindahl, L Fehrentz, J A Martinez, J Perrissoud, D Dickson, S L
...
Published in
Journal of neuroendocrinology
In the present study, we explore the central nervous system mechanism underlying the chronic central effects of ghrelin with respect to increasing body weight and body fat. Specifically, using a recently developed ghrelin receptor antagonist, GHS-R1A (JMV2959), we investigate the role of GHS-R1A in mediating the effects of ghrelin on energy balance...
Jabbari, Esmaiel
Published in
Pharmaceutical Research
Peptides produce specific nanostructures, making them useful for targeting in biological systems but they have low bioavailability, potential immunogenicity and poor metabolic stability. Peptidomimetic self-assembled NPs can possess biological recognition motifs as well as providing desired engineering properties. Inorganic NPs, coated with self-as...
