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- Publications
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Development of a Novel Backbone Cyclic Peptide Inhibitor of the Innate Immune TLR/IL1R Signaling Protein MyD88
- Shira Dishon, A. Schumacher, +6 authors G. Nussbaum
- Chemistry, Medicine
- Scientific Reports
- 21 June 2018
MyD88 is a cytoplasmic adaptor protein that plays a central role in signaling downstream of the TLRs and the IL1R superfamily. We previously demonstrated that MyD88 plays a critical role in EAE, the… Expand
The role of molecular physicochemical properties and apolipoproteins in association of drugs with triglyceride‐rich lipoproteins: in‐silico prediction of uptake by chylomicrons
- P. Gershkovich, Joseph Fanous, Bashir Qadri, Avihai Yacovan, S. Amselem, A. Hoffman
- Chemistry
- 1 January 2009
Objectives The uptake of drugs by chylomicrons is a key element in both intestinal lymphatic transport and postprandial alterations in the disposition profile of lipophilic drugs. The aim of this… Expand
Tailoring of integrin ligands: probing the charge capability of the metal ion-dependent adhesion site.
- Markus Bollinger, Florian Manzenrieder, +11 authors H. Kessler
- Chemistry, Medicine
- Journal of medicinal chemistry
- 9 January 2012
Intervention in integrin-mediated cell adhesion and integrin signaling pathways is an ongoing area of research in medicinal chemistry and drug development. One key element in integrin-ligand… Expand
Overcoming the Lack of Oral Availability of Cyclic Hexapeptides: Design of a Selective and Orally Available Ligand for the Integrin αvβ3.
- Michael Weinmüller, F. Rechenmacher, +13 authors H. Kessler
- Chemistry, Medicine
- Angewandte Chemie
- 18 December 2017
A highly systematic approach for the development of both orally bioavailable and bioactive cyclic N-methylated hexapeptides as high affinity ligands for the integrin αvβ3 is based on two concepts: a)… Expand
Enhancing Oral Bioavailability of Cyclic RGD Hexa-peptides by the Lipophilic Prodrug Charge Masking Approach: Redirection of Peptide Intestinal Permeability from a Paracellular to Transcellular…
- Adi Schumacher-Klinger, Joseph Fanous, +7 authors A. Hoffman
- Chemistry, Medicine
- Molecular pharmaceutics
- 5 July 2018
Hydrophilic peptides constitute most of the active peptides. They mostly permeate via tight junctions (paracellular pathway) in the intestine. This permeability mechanism restricts the magnitude of… Expand
The role of molecular physicochemical properties and apolipoproteins in association of drugs with triglyceride-rich lipoproteins: in-silico prediction of uptake by chylomicrons.
- P. Gershkovich, Joseph Fanous, Bashir Qadri, A. Yacovan, S. Amselem, A. Hoffman
- Medicine
- The Journal of pharmacy and pharmacology
- 2009
OBJECTIVES
The uptake of drugs by chylomicrons is a key element in both intestinal lymphatic transport and postprandial alterations in the disposition profile of lipophilic drugs. The aim of this… Expand
Superiority of the S,S conformation in diverse pharmacological processes: Intestinal transport and entry inhibition activity of novel anti-HIV drug lead.
- Joseph Fanous, Avi Swed, +5 authors A. Hoffman
- Chemistry, Medicine
- International journal of pharmaceutics
- 30 November 2015
Chirality is an important aspect in many pharmacological processes including drug transport and metabolism. The current investigation examined the stereospecific transport and entry inhibitory… Expand
Quantitative contribution of efflux to multi-drug resistance of clinical Escherichia coli and Pseudomonas aeruginosa strains
- Olivier Cunrath, D. Meinel, +11 authors D. Bumann
- Biology, Medicine
- EBioMedicine
- 1 March 2019
Background Efflux pumps mediate antimicrobial resistance in several WHO critical priority bacterial pathogens. However, most available data come from laboratory strains. The quantitative relevance of… Expand
Lösung des Problems mangelnder oraler Verfügbarkeit cyclischer Hexapeptide: Entwicklung eines selektiven, oral verfügbaren Liganden für das Integrin αvβ3
- Michael Weinmüller, F. Rechenmacher, +13 authors H. Kessler
- Chemistry
- 18 December 2017
The Calbindin-D28k binding site on inositol monophosphatase may allow inhibition independent of the lithium site of action
- A. Hoffman, Yftah Tal-Gan, +6 authors C. Gilon
- Chemistry
- 6 September 2011
Among numerous reported biochemical effects the lithium-inhibitable enzyme inositol-monophosphatase (IMPase) remains a viable target for lithium's therapeutic mechanism of action. Calbindin-D28k… Expand