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Article ; Online: Design and Biochemical Characterization of Peptidic Inhibitors of the Myb/p300 Interaction.

Jones, Matthew / Grosche, Philipp / Floersheimer, Andreas / André, Jérome / Gattlen, Raphael / Oser, Dieter / Tinchant, Juliette / Wille, Roman / Chie-Leon, Barbara / Gerspacher, Marc / Ertl, Peter / Ostermann, Nils / Altmann, Eva / Manchado, Eusebio / Vorherr, Thomas / Chène, Patrick

Biochemistry

2023 Volume 62, Issue 7, Page(s) 1321–1329

Abstract: The Myb transcription factor is involved in the proliferation of hematopoietic cells, and deregulation of its expression can lead to cancers such as leukemia. Myb interacts with various proteins, including the histone acetyltransferases p300 and CBP. Myb ...

Abstract	The Myb transcription factor is involved in the proliferation of hematopoietic cells, and deregulation of its expression can lead to cancers such as leukemia. Myb interacts with various proteins, including the histone acetyltransferases p300 and CBP. Myb binds to a small domain of p300, the KIX domain (p300
MeSH term(s)	Peptides/pharmacology ; Protein Binding ; Proto-Oncogene Proteins c-myb/antagonists & inhibitors ; Proto-Oncogene Proteins c-myb/chemistry ; E1A-Associated p300 Protein/antagonists & inhibitors ; E1A-Associated p300 Protein/chemistry
Chemical Substances	Peptides ; Proto-Oncogene Proteins c-myb ; E1A-Associated p300 Protein (EC 2.3.1.48)
Language	English
Publishing date	2023-03-08
Publishing country	United States
Document type	Journal Article
ZDB-ID	1108-3
ISSN	1520-4995 ; 0006-2960
ISSN (online)	1520-4995
ISSN	0006-2960
DOI	10.1021/acs.biochem.2c00690
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Article: New aromatase inhibitors from the 3-pyridyl arylether and 1-aryl pyrrolo[2,3-c]pyridine series

Stauffer, Frédéric / Furet, Pascal / Floersheimer, Andreas / Lang, Marc

Bioorganic & medicinal chemistry letters. 2012 Mar. 1, v. 22, no. 5

2012

Abstract: Aromatase inhibition is the new standard of care for estrogen receptor positive breast cancer and has also potential for treatment of other diseases such as endometriosis. Simple and readily available 3-pyridyl arylethers and 1-aryl pyrrolo[2,3-c] ... ...

Abstract	Aromatase inhibition is the new standard of care for estrogen receptor positive breast cancer and has also potential for treatment of other diseases such as endometriosis. Simple and readily available 3-pyridyl arylethers and 1-aryl pyrrolo[2,3-c]pyridines recapitulating the key pharmacophore elements of Letrozole (1) are described and their structure–activity relationships are discussed. Potent and ligand efficient leads such as compound 23 (IC₅₀=59nM on aromatase) have been identified.
Keywords	breast neoplasms ; estrogen receptors ; pharmacology ; pyridines ; structure-activity relationships ; unspecific monooxygenase
Language	English
Dates of publication	2012-0301
Size	p. 1860-1863.
Publishing place	Elsevier Ltd
Document type	Article
ZDB-ID	1063195-1
ISSN	1464-3405 ; 0960-894X
ISSN (online)	1464-3405
ISSN	0960-894X
DOI	10.1016/j.bmcl.2012.01.076
Database	NAL-Catalogue (AGRICOLA)

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Article ; Online: New aromatase inhibitors from the 3-pyridyl arylether and 1-aryl pyrrolo[2,3-c]pyridine series.

Stauffer, Frédéric / Furet, Pascal / Floersheimer, Andreas / Lang, Marc

Bioorganic & medicinal chemistry letters

2012 Volume 22, Issue 5, Page(s) 1860–1863

Abstract	Aromatase inhibition is the new standard of care for estrogen receptor positive breast cancer and has also potential for treatment of other diseases such as endometriosis. Simple and readily available 3-pyridyl arylethers and 1-aryl pyrrolo[2,3-c]pyridines recapitulating the key pharmacophore elements of Letrozole (1) are described and their structure-activity relationships are discussed. Potent and ligand efficient leads such as compound 23 (IC(50)=59nM on aromatase) have been identified.
MeSH term(s)	Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Aromatase/metabolism ; Aromatase Inhibitors/chemistry ; Aromatase Inhibitors/pharmacology ; Breast Neoplasms/drug therapy ; Breast Neoplasms/enzymology ; Female ; Humans ; Models, Molecular ; Pyridines/chemistry ; Pyridines/pharmacology ; Pyrroles/chemistry ; Pyrroles/pharmacology ; Structure-Activity Relationship
Chemical Substances	Antineoplastic Agents ; Aromatase Inhibitors ; Pyridines ; Pyrroles ; pyrrolo(3,2-c)pyridine ; Aromatase (EC 1.14.14.1)
Language	English
Publishing date	2012-03-01
Publishing country	England
Document type	Journal Article
ZDB-ID	1063195-1
ISSN	1464-3405 ; 0960-894X
ISSN (online)	1464-3405
ISSN	0960-894X
DOI	10.1016/j.bmcl.2012.01.076
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Article: 4. The natural products epothilones A and B as lead structures for anticancer drug discovery: chemistry, biology, and SAR studies.

Altmann, Karl-Heinz / Flörsheimer, Andreas / O'Reilly, Terence / Wartmann, Markus

Progress in medicinal chemistry

2004 Volume 42, Page(s) 171–205

MeSH term(s)	Animals ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/metabolism ; Antineoplastic Agents/pharmacology ; Epothilones/chemical synthesis ; Epothilones/metabolism ; Epothilones/pharmacology ; Humans ; Microtubules/drug effects ; Microtubules/metabolism ; Neoplasms/drug therapy ; Neoplasms/metabolism ; Structure-Activity Relationship ; Tubulin/metabolism
Chemical Substances	Antineoplastic Agents ; Epothilones ; Tubulin ; epothilone A (51E07YBX96) ; desoxyepothilone B (T0358E0YUF) ; epothilone B (UEC0H0URSE)
Language	English
Publishing date	2004
Publishing country	Netherlands
Document type	Journal Article ; Review
ZDB-ID	209306-6
ISSN	1875-7863 ; 0079-6468
ISSN (online)	1875-7863
ISSN	0079-6468
DOI	10.1016/S0079-6468(04)42004-9
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Article ; Online: Pharmacokinetic profile of the microtubule stabilizer patupilone in tumor-bearing rodents and comparison of anti-cancer activity with other MTS in vitro and in vivo.

O'Reilly, Terence / Wartmann, Markus / Brueggen, Joseph / Allegrini, Peter R / Floersheimer, Andreas / Maira, Michel / McSheehy, Paul M J

Cancer chemotherapy and pharmacology

2008 Volume 62, Issue 6, Page(s) 1045–1054

Abstract: Introduction: Patupilone is a microtubule stabilizer (MTS) currently in clinical development. Here, we evaluate the anti-cancer activity in vitro and in vivo in comparison to paclitaxel and describe the pharmacokinetics (PK) of patupilone in tumor- ... ...

Abstract	Introduction: Patupilone is a microtubule stabilizer (MTS) currently in clinical development. Here, we evaluate the anti-cancer activity in vitro and in vivo in comparison to paclitaxel and describe the pharmacokinetics (PK) of patupilone in tumor-bearing nude mice and rats. Methods: The potency in vitro of patupilone and two other MTS, paclitaxel and ixabepilone, was determined using human colon carcinoma cell lines with low (HCT-116, HT-29, RKO) and high (HCT-15) P-glycoprotein expression (P-gp), as well as two multi-drug resistance (MDR) model cell pairs, MCF7/ADR and KB-8511 cells and their respective drug-sensitive parental counterparts. The PK of patupilone was investigated in nude mice bearing HCT-15 or HT-29 xenografts and in rats bearing s.c. pancreatic CA20498 tumors or A15 glioma tumors. Anti-cancer activity in vivo was compared to that of paclitaxel using three different human tumor colon models. The retention and efficacy of patupilone was compared in small and large HT-29 xenografts whose vascularity was determined by non-invasive magnetic resonance imaging. Results: Patupilone was highly potent in vitro against four different colon carcinoma cell lines including those showing multi-drug-resistance. In contrast, paclitaxel and ixabepilone displayed significantly reduced activity with markedly increased resistance factors. In both rats and mice, a single i.v. bolus injection of patupilone (1.5-4 mg/kg) rapidly distributed from plasma to all tissues and was slowly eliminated from muscle, liver and small intestine, but showed longer retention in tumor and brain with no apparent elimination over 24 h. Patupilone showed significant activity against three human colon tumor models in vivo, unlike paclitaxel, which only had activity against low P-gp expressing tumors. In HT-29 tumors, patupilone activity and retention were independent of tumor size, blood volume and flow. Conclusions: The high potency of patupilone, which is not affected by P-gp expression either in vitro or in vivo, and favorable PK, independent of tumor vascularity, suggest that it should show significant activity in colorectal cancer and in other indications where high P-gp expression may compromise taxane activity.
MeSH term(s)	ATP-Binding Cassette, Sub-Family B, Member 1/metabolism ; Animals ; Antineoplastic Agents/pharmacokinetics ; Antineoplastic Agents/pharmacology ; Antineoplastic Agents/therapeutic use ; Breast Neoplasms/drug therapy ; Breast Neoplasms/metabolism ; Breast Neoplasms/pathology ; Carcinoma/blood supply ; Carcinoma/drug therapy ; Carcinoma/metabolism ; Carcinoma/pathology ; Cell Line, Tumor/drug effects ; Cell Line, Tumor/metabolism ; Colonic Neoplasms/blood supply ; Colonic Neoplasms/drug therapy ; Colonic Neoplasms/metabolism ; Colonic Neoplasms/pathology ; Drug Resistance, Multiple ; Drug Resistance, Neoplasm ; Epothilones/pharmacokinetics ; Epothilones/pharmacology ; Epothilones/therapeutic use ; Female ; Glioma/drug therapy ; Glioma/metabolism ; Glioma/pathology ; Magnetic Resonance Imaging ; Mice ; Mice, Nude ; Microtubules/drug effects ; Neoplasm Proteins/metabolism ; Paclitaxel/pharmacology ; Paclitaxel/therapeutic use ; Pancreatic Neoplasms/drug therapy ; Pancreatic Neoplasms/metabolism ; Pancreatic Neoplasms/pathology ; Rats ; Rats, Inbred Lew ; Tissue Distribution ; Xenograft Model Antitumor Assays
Chemical Substances	ATP-Binding Cassette, Sub-Family B, Member 1 ; Antineoplastic Agents ; Epothilones ; Neoplasm Proteins ; ixabepilone (K27005NP0A) ; Paclitaxel (P88XT4IS4D) ; epothilone B (UEC0H0URSE)
Language	English
Publishing date	2008-11
Publishing country	Germany
Document type	Comparative Study ; Journal Article
ZDB-ID	6820-2
ISSN	1432-0843 ; 0344-5704 ; 0943-9404
ISSN (online)	1432-0843
ISSN	0344-5704 ; 0943-9404
DOI	10.1007/s00280-008-0695-9
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Zs.A 1420: Show issues

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Article ; Online: Antileukemic Effects of Novel First- and Second-Generation FLT3 Inhibitors: Structure-Affinity Comparison.

Weisberg, Ellen / Roesel, Johannes / Furet, Pascal / Bold, Guido / Imbach, Patricia / Flörsheimer, Andreas / Caravatti, Georgio / Jiang, Jingrui / Manley, Paul / Ray, Arghya / Griffin, James D

Genes & cancer

2011 Volume 1, Issue 10, Page(s) 1021–1032

Abstract: Constitutively activated mutant FLT3 has emerged as a promising target for therapy for the subpopulation of acute myeloid leukemia (AML) patients who harbor it. The small molecule inhibitor, PKC412, targets mutant FLT3 and is currently in late-stage ... ...

Abstract	Constitutively activated mutant FLT3 has emerged as a promising target for therapy for the subpopulation of acute myeloid leukemia (AML) patients who harbor it. The small molecule inhibitor, PKC412, targets mutant FLT3 and is currently in late-stage clinical trials. However, the identification of PKC412-resistant leukemic blast cells in the bone marrow of AML patients has propelled the development of novel and structurally distinct FLT3 inhibitors that have the potential to override drug resistance and more efficiently prevent disease progression or recurrence. Here, we present the novel first-generation "type II" FLT3 inhibitors, AFG206, AFG210, and AHL196, and the second-generation "type II" derivatives and AST487 analogs, AUZ454 and ATH686. All agents potently and selectively target mutant FLT3 protein kinase activity and inhibit the proliferation of cells harboring FLT3 mutants via induction of apoptosis and cell cycle inhibition. Cross-resistance between "type I" inhibitors, PKC412 and AAE871, was demonstrated. While cross-resistance was also observed between "type I" and first-generation "type II" FLT3 inhibitors, the high potency of the second-generation "type II" inhibitors was sufficient to potently kill "type I" inhibitor-resistant mutant FLT3-expressing cells. The increased potency observed for the second-generation "type II" inhibitors was observed to be due to an improved interaction with the ATP pocket of FLT3, specifically associated with introduction of a piperazine moiety and placement of an amino group in position 2 of the pyrimidine ring. Thus, we present 2 structurally novel classes of FLT3 inhibitors characterized by high selectivity and potency toward mutant FLT3 as a molecular target. In addition, presentation of the antileukemic effects of "type II" inhibitors, such as AUZ454 and ATH686, highlights a new class of highly potent FLT3 inhibitors able to override drug resistance that less potent "type I" inhibitors and "type II" first-generation FLT3 inhibitors cannot.
Language	English
Publishing date	2011-07-14
Publishing country	United States
Document type	Journal Article
ZDB-ID	2538519-7
ISSN	1947-6027 ; 1947-6019
ISSN (online)	1947-6027
ISSN	1947-6019
DOI	10.1177/1947601910396505
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Article: Second-site NMR screening and linker design.

Jahnke, Wolfgang / Flörsheimer, Andreas / Blommers, Marcel J J / Paris, C Gregory / Heim, Jutta / Nalin, Carlo M / Perez, Lawrence B

Current topics in medicinal chemistry

2003 Volume 3, Issue 1, Page(s) 69–80

Abstract: One of the prime merits of NMR as a tool for lead finding in drug discovery research is its sensitivity and robustness to detect weak protein-ligand interactions. This sensitivity allows to build up ligands for a given target in a modular way, by a ... ...

Abstract	One of the prime merits of NMR as a tool for lead finding in drug discovery research is its sensitivity and robustness to detect weak protein-ligand interactions. This sensitivity allows to build up ligands for a given target in a modular way, by a fragment-based approach. In this approach, two ligands are seperately identified which bind to the target protein generally weakly, but at adjacent binding sites. In a next step, they are chemically linked to produce a high-affinity ligand. This review discusses methods to detect "second-site" ligands that bind to a protein in the presence of a "first-site" ligand, and methods to elucidate structural details on the spatial orientation of both ligands, so that chemical linkage is based on a large piece of experimental information. Published examples from second-site screening and linker design are summarized, and are complemented by previously unpublished in-house examples.
MeSH term(s)	Drug Design ; Drug Evaluation, Preclinical/methods ; Humans ; Ligands ; Models, Molecular ; Nuclear Magnetic Resonance, Biomolecular/methods ; Pharmaceutical Preparations/chemistry ; Pharmaceutical Preparations/metabolism ; Proteins/chemistry ; Proteins/metabolism ; Spin Labels
Chemical Substances	Ligands ; Pharmaceutical Preparations ; Proteins ; Spin Labels
Language	English
Publishing date	2003
Publishing country	United Arab Emirates
Document type	Journal Article ; Review
ZDB-ID	2064823-6
ISSN	1873-4294 ; 1568-0266
ISSN (online)	1873-4294
ISSN	1568-0266
DOI	10.2174/1568026033392778
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Zs.A 5572: Show issues

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Article: Structural biology contributions to the discovery of drugs to treat chronic myelogenous leukaemia.

Cowan-Jacob, Sandra W / Fendrich, Gabriele / Floersheimer, Andreas / Furet, Pascal / Liebetanz, Janis / Rummel, Gabriele / Rheinberger, Paul / Centeleghe, Mario / Fabbro, Doriano / Manley, Paul W

Acta crystallographica. Section D, Biological crystallography

2006 Volume 63, Issue Pt 1, Page(s) 80–93

Abstract: Chronic myelogenous leukaemia (CML) results from the Bcr-Abl oncoprotein, which has a constitutively activated Abl tyrosine kinase domain. Although most chronic phase CML patients treated with imatinib as first-line therapy maintain excellent durable ... ...

Abstract	Chronic myelogenous leukaemia (CML) results from the Bcr-Abl oncoprotein, which has a constitutively activated Abl tyrosine kinase domain. Although most chronic phase CML patients treated with imatinib as first-line therapy maintain excellent durable responses, patients who have progressed to advanced-stage CML frequently fail to respond or lose their response to therapy owing to the emergence of drug-resistant mutants of the protein. More than 40 such point mutations have been observed in imatinib-resistant patients. The crystal structures of wild-type and mutant Abl kinase in complex with imatinib and other small-molecule Abl inhibitors were determined, with the aim of understanding the molecular basis of resistance and to aid in the design and optimization of inhibitors active against the resistance mutants. These results are presented in a way which illustrates the approaches used to generate multiple structures, the type of information that can be gained and the way that this information is used to support drug discovery.
MeSH term(s)	Animals ; Antineoplastic Agents/pharmacology ; Binding Sites ; Chemistry, Pharmaceutical/methods ; Crystallization ; Crystallography, X-Ray ; Drug Design ; Drug Industry/methods ; Humans ; Leukemia, Myelogenous, Chronic, BCR-ABL Positive/drug therapy ; Models, Chemical ; Models, Genetic ; Models, Molecular ; Molecular Conformation ; Point Mutation
Chemical Substances	Antineoplastic Agents
Language	English
Publishing date	2006-12-13
Publishing country	United States
Document type	Journal Article
ZDB-ID	2020492-9
ISSN	1399-0047 ; 0907-4449
ISSN (online)	1399-0047
ISSN	0907-4449
DOI	10.1107/S0907444906047287
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Article: New aromatase inhibitors from the 3-pyridyl arylether and 1-aryl pyrrolo[2,3-c]pyridine series

Stauffer, Frédéric / Furet, Pascal / Floersheimer, Andreas / Lang, Marc

Bioorganic & medicinal chemistry letters

Volume v. 22,, Issue no. 5

Abstract	Aromatase inhibition is the new standard of care for estrogen receptor positive breast cancer and has also potential for treatment of other diseases such as endometriosis. Simple and readily available 3-pyridyl arylethers and 1-aryl pyrrolo[2,3-c]pyridines recapitulating the key pharmacophore elements of Letrozole (1) are described and their structure–activity relationships are discussed. Potent and ligand efficient leads such as compound 23 (IC₅₀=59nM on aromatase) have been identified.
Keywords	unspecific monooxygenase ; pyridines ; structure-activity relationships ; estrogen receptors ; pharmacology ; breast neoplasms
Language	English
Document type	Article
ISSN	0960-894X
Database	AGRIS - International Information System for the Agricultural Sciences and Technology

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