Strukturbasierte Entwicklung von Inhibitoren der humanen Tyrosinase und der Farnesyltransferase

A Mädel - 2009 - archiv.ub.uni-marburg.de
Im Rahmen eines Industrieprojektes der Firma Beiersdorf wurde in enger Kooperation mit
den Arbeitskreisen von Prof. Klebe und Prof. Röhm die Synthese neuartiger Inhibitoren der …

[引用][C] Farnesyltransferase‐Inhibitoren hemmen das Wachstum von Malaria‐Erregern in vitro und in vivo

J Wiesner, K Kettler, J Sakowski, R Ortmann… - Angewandte …, 2004 - Wiley Online Library
Die Entwicklung von Farnesyltransferase-Inhibitoren als Malariatherapeutika wird dadurch
erschwert, dass die heterologe Expression der Farnesyltransferase von P. falciparum bisher …

[PDF][PDF] Structurally simple farnesyltransferase inhibitors arrest the growth of malaria parasites

MP Glenn, SY Chang, O Hucke… - Angewandte …, 2005 - faculty.washington.edu
The development of antimalarial agents is not only constricted by the parameters common to
the development of all new drugs (efficacy, toxicity, pharmacology), but importantly, must …

[PDF][PDF] Farnesyltransferase inhibitors inhibit the growth of malaria parasites in vitro and in vivo

J Wiesner, K Kettler, J Sakowski, R Ortmann… - Angewandte Chemie …, 2004 - academia.edu
Farnesyltransferase catalyzes the posttranslational modification of numerous proteins
involved in intracellular signal transduction by transferring the farnesyl residue of farnesyl …

Tyrosinase inhibitors: a patent review (2011-2015)

S Ullah, S Son, HY Yun, DH Kim, P Chun… - Expert Opinion on …, 2016 - Taylor & Francis
Introduction: Tyrosinase is responsible for melanin production. The overproduction of
melanin causes many skin disorders. The inhibition of tyrosinase activity would appear to be …

Development of benzophenone‐based farnesyltransferase inhibitors as novel antimalarials

K Kohring, J Wiesner, M Altenkämper… - ChemMedChem …, 2008 - Wiley Online Library
The development of farnesyltransferase inhibitors directed against Plasmodium falciparum
is a strategy towards new drugs against malaria. Previously, we described benzophenone …

Non-thiol farnesyltransferase inhibitors: N-(4-aminoacylamino-3-benzoylphenyl)-3-[5-(4-nitrophenyl)-2 furyl] acrylic acid amides and their antimalarial activity

K Kettler, J Wiesner, K Silber, P Haebel… - European journal of …, 2005 - Elsevier
Water solubility was previously found to be essential for in vivo-antimalarial activity of a
novel type of benzophenone-based farnesyltransferase inhibitors. Introduction of a α-amino …

2-Oxotetrahydroquinoline-based antimalarials with high potency and metabolic stability

VJ Bulbule, K Rivas, CLMJ Verlinde… - Journal of medicinal …, 2008 - ACS Publications
We report a series of novel inhibitors of protein farnesyltransferase based on the 2-
oxotetrahydroquinoline scaffold. We developed an efficient synthesis of these compounds …

Inhibition of farnesyltransferase as a strategy for the development of novel anti-malarials

M Schlitzer - Current Medicinal Chemistry-Anti-Infective Agents, 2005 - ingentaconnect.com
Farnesyltransferase catalyzing the transfer of a farnesyl residue from farnesylpyrophosphate
to the thiol of a cysteine side chain of proteins carrying the C-terminal CAAX-tetrapeptide …

Molecular design of tyrosinase inhibitors: A critical review of promising novel inhibitors from synthetic origins

MTH Khan - Pure and Applied Chemistry, 2007 - degruyter.com
The enzyme tyrosinase is known to be a multifunctional copper-containing enzyme from the
oxidase superfamily, which is the key protein involved in the biosynthesis of the large …