De novo development of small cyclic peptides that are orally bioavailable [PDF]
Cyclic peptides can bind challenging disease targets with high affinity and specificity, offering enormous opportunities for addressing unmet medical needs. However, as with biological drugs, most cyclic peptides cannot be applied orally because they are
Merz, Manuel Leonardo +9 more
core +1 more source
Comparing the paths of Hedgehog release in artificial and natural settings
FEBS Letters, EarlyView.Hh morphogens require solubilization factors to overcome their tight association with the plasma membrane and signal to distant cells, but the precise functions of these factors are controversial. Here, we use published in vivo observations as the most relevant evidence to test their suggested functions and discuss contradictions and gaps between in ...
Janna Puschmann, Kay Grobe
wiley +1 more source
Characterisation of the anti-inflammatory and anti-proliferative effects of natriuretic peptides in rodents. [PDF]
, 2007 Natriuretic peptides are a family of vasoactive hormones that play important roles in cardiovascular homeostasis. These peptides exert biological effects primarily via activation of guanylate cyclase (GC)-coupled natriuretic peptide receptors (NPR) that ...
Panayiotou, C.M.
core
How structural disorder and polyelectrolyte properties of prothymosin α enable its large interactome
FEBS Letters, EarlyView.In this review, complexes of the fully disordered and highly negatively charged prothymosin α are collected, described, and discussed. Linked to its poly‐electrostatic character, prothymosin α engages a large interactome through multiple different binding modes ranging from fully disordered complexes to short linear motif (SLiM)‐driven interactions ...
Ketty C. Tamburrini +3 more
wiley +1 more source
The Calbindin-D28k binding site on inositol monophosphatase may allow inhibition independent of the lithium site of action [PDF]
, 2011 Among numerous reported biochemical effects the lithium-inhibitable enzyme inositol-monophosphatase (IMPase) remains a viable target for lithium's therapeutic mechanism of action.
Galila Agam +8 more
core
Tumour–host interactions in Drosophila: mechanisms in the tumour micro‐ and macroenvironment
Molecular Oncology, EarlyView.This review examines how tumour–host crosstalk takes place at multiple levels of biological organisation, from local cell competition and immune crosstalk to organism‐wide metabolic and physiological collapse. Here, we integrate findings from Drosophila melanogaster studies that reveal conserved mechanisms through which tumours hijack host systems to ...
José Teles‐Reis, Tor Erik Rusten
wiley +1 more source
Mechanisms and therapeutic opportunities of the ribotoxic stress response in cancer
Molecular Oncology, EarlyView.Cancer cells' high translational demand creates opportunities to therapeutically target ribosome function. Ribosome stalling and collisions activate ZAKα and the ribotoxic stress response (RSR), which can trigger rapid, p53‐independent apoptosis in cancer.
Anastassiya Kim +7 more
wiley +1 more source
, 2017 Cyclic peptides are increasingly employed as chemical tools in biology and drug discovery. They have gained a lot of interest as alternative sources of new drugs to traditional small molecules. This book introduces cyclic peptides and provides a thorough
Naismith, James Henderson +1 more
core +2 more sources
Cyclic, Cell-Penetrating Peptides Tailor-Made for the Creation of Peptide Libraries with Intrinsic Cell Permeability [PDF]
, 2020 The discovery of high-affinity peptides to many intracellular targets has become feasible through the development of diverse macrocyclic peptide libraries. But lack of cell permeability is a key feature hampering the use of these peptides as therapeutics.
Koushambi, Mitra +5 more
core +1 more source
The VHL tumor suppressor at the crossroad of protein folding, aggregation, and cancer
Molecular Oncology, EarlyView.Mutations, environmental stress, and chaperone dysfunction can destabilize pVHL, promoting its conversion from the native folded state into amyloid‐like assemblies. This transition may contribute to protein storage, cell dormancy, survival, and drug resistance.
Lara Abad +2 more
wiley +1 more source