An acylation cycle regulates localization and activity of palmitoylated Ras isoforms
…, M Lumbierres, J Kuhlmann, H Waldmann… - …, 2005 - science.sciencemag.org
We show that the specific subcellular distribution of H-and Nras guanosine triphosphate–
binding proteins is generated by a constitutive de/reacylation cycle that operates on
palmitoylated proteins, driving their rapid exchange between the plasma membrane (PM) …
binding proteins is generated by a constitutive de/reacylation cycle that operates on
palmitoylated proteins, driving their rapid exchange between the plasma membrane (PM) …
From protein domains to drug candidates—natural products as guiding principles in the design and synthesis of compound libraries
…, IR Vetter, H Waldmann - Angewandte Chemie …, 2002 - Wiley Online Library
In the continuing effort to find small molecules that alter protein function and ultimately might
lead to new drugs, combinatorial chemistry has emerged as a very powerful tool. Contrary to
original expectations that large libraries would result in the discovery of many hit and lead …
lead to new drugs, combinatorial chemistry has emerged as a very powerful tool. Contrary to
original expectations that large libraries would result in the discovery of many hit and lead …
Chemical strategies for generating protein biochips
…, CM Niemeyer, H Waldmann - Angewandte Chemie …, 2008 - Wiley Online Library
Protein biochips are at the heart of many medical and bioanalytical applications. Increasing
interest has been focused on surface activation and subsequent functionalization strategies
for immobilizing these biomolecules. Different approaches using covalent and noncovalent …
interest has been focused on surface activation and subsequent functionalization strategies
for immobilizing these biomolecules. Different approaches using covalent and noncovalent …
Charting biologically relevant chemical space: a structural classification of natural products (SCONP)
…, A Odermatt, P Ertl, H Waldmann - Proceedings of the …, 2005 - National Acad Sciences
The identification of small molecules that fall within the biologically relevant subfraction of
vast chemical space is of utmost importance to chemical biology and medicinal chemistry
research. The prerequirement of biological relevance to be met by such molecules is fulfilled …
vast chemical space is of utmost importance to chemical biology and medicinal chemistry
research. The prerequirement of biological relevance to be met by such molecules is fulfilled …
A functional screen implicates microRNA-138-dependent regulation of the depalmitoylation enzyme APT1 in dendritic spine morphogenesis
…, B Rengarajan, C Drepper, H Waldmann… - Nature cell …, 2009 - nature.com
The microRNA pathway has been implicated in the regulation of synaptic protein synthesis
and ultimately in dendritic spine morphogenesis, a phenomenon associated with long-
lasting forms of memory. However, the particular microRNAs (miRNAs) involved are largely …
and ultimately in dendritic spine morphogenesis, a phenomenon associated with long-
lasting forms of memory. However, the particular microRNAs (miRNAs) involved are largely …
Inhibitors of protein tyrosine phosphatases: Next‐generation drugs?
L Bialy, H Waldmann - Angewandte Chemie International …, 2005 - Wiley Online Library
The protein tyrosine phosphatases (PTPs) constitute a family of closely related key
regulatory enzymes that dephosphorylate phosphotyrosine residues in their protein
substrates. Malfunctions in PTP activity are linked to various diseases, ranging from cancer …
regulatory enzymes that dephosphorylate phosphotyrosine residues in their protein
substrates. Malfunctions in PTP activity are linked to various diseases, ranging from cancer …
Highly enantioselective synthesis and cellular evaluation of spirooxindoles inspired by natural products
…, H Preut, S Ziegler, D Rauh, H Waldmann - Nature …, 2010 - nature.com
In biology-oriented synthesis the underlying scaffold classes of natural products selected in
evolution are used to define biologically relevant starting points in chemical structure space
for the synthesis of compound collections with focused structural diversity. Here we describe …
evolution are used to define biologically relevant starting points in chemical structure space
for the synthesis of compound collections with focused structural diversity. Here we describe …
Small molecule inhibition of the KRAS–PDEδ interaction impairs oncogenic KRAS signalling
…, G Triola, A Wittinghofer, PIH Bastiaens, H Waldmann - Nature, 2013 - nature.com
The KRAS oncogene product is considered a major target in anticancer drug discovery 1, 2,
3. However, direct interference with KRAS signalling has not yet led to clinically useful drugs
3, 4, 5, 6, 7, 8. Correct localization and signalling by farnesylated KRAS is regulated by the …
3. However, direct interference with KRAS signalling has not yet led to clinically useful drugs
3, 4, 5, 6, 7, 8. Correct localization and signalling by farnesylated KRAS is regulated by the …
Protecting group strategies in organic synthesis
M Schelhaas, H Waldmann - … Chemie International Edition in …, 1996 - Wiley Online Library
The choice of protecting groups is one of the decisive factors in the successful realization of
a complex, demanding synthetic project. The protecting groups used influence the length
and efficiency of the synthesis and are often responsible for its success or failure. A wide …
a complex, demanding synthetic project. The protecting groups used influence the length
and efficiency of the synthesis and are often responsible for its success or failure. A wide …
Activation of the Raf-MEK-ERK pathway is required for neutrophil extracellular trap formation
…, S Hess, H Prinz, A Zychlinsky, H Waldmann - Nature chemical …, 2011 - nature.com
The signaling mechanisms leading to the formation of neutrophil extracellular traps (NETs),
relevant in infections, sepsis and autoimmune diseases, are poorly understood. Neutrophils
are not amenable to studies with conventional genetic techniques. Using a new chemical …
relevant in infections, sepsis and autoimmune diseases, are poorly understood. Neutrophils
are not amenable to studies with conventional genetic techniques. Using a new chemical …