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Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor

Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor

by Bröker, Joachim, Waterson, Alex G., Smethurst, Chris, Kessler, Dirk, Böttcher, Jark, Mayer, Moriz, Gmaschitz, Gerhard, Phan, Jason, Little, Andrew, Abbott, Jason R., Sun, Qi, Gmachl, Michael, Rudolph, Dorothea, Arnhof, Heribert, Rumpel, Klaus, Savarese, Fabio, Gerstberger, Thomas, Mischerikow, Nikolai, Treu, Matthias, Herdeis, Lorenz, Wunberg, Tobias, Gollner, Andreas, Weinstabl, Harald, Mantoulidis, Andreas, Krämer, Oliver, McConnell, Darryl B., W. Fesik, Stephen
Published in Journal of medicinal chemistry (10.11.2022)

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Journal Article

Stopping the beating heart of cancer: KRAS reviewed

Stopping the beating heart of cancer: KRAS reviewed

by Herdeis, Lorenz, Gerlach, Daniel, McConnell, Darryl B., Kessler, Dirk
Published in Current opinion in structural biology (01.12.2021)

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Journal Article

Pan-KRAS inhibitor disables oncogenic signalling and tumour growth

Pan-KRAS inhibitor disables oncogenic signalling and tumour growth

by Kim, Dongsung, Herdeis, Lorenz, Rudolph, Dorothea, Zhao, Yulei, Böttcher, Jark, Vides, Alberto, Ayala-Santos, Carlos I., Pourfarjam, Yasin, Cuevas-Navarro, Antonio, Xue, Jenny Y., Mantoulidis, Andreas, Bröker, Joachim, Wunberg, Tobias, Schaaf, Otmar, Popow, Johannes, Wolkerstorfer, Bernhard, Kropatsch, Katrin Gabriele, Qu, Rui, de Stanchina, Elisa, Sang, Ben, Li, Chuanchuan, McConnell, Darryl B., Kraut, Norbert, Lito, Piro
Published in Nature (London) (06.07.2023)

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Journal Article

Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRAS G12C Inhibitor

Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRAS G12C Inhibitor

by Bröker, Joachim, Waterson, Alex G., Smethurst, Chris, Kessler, Dirk, Böttcher, Jark, Mayer, Moriz, Gmaschitz, Gerhard, Phan, Jason, Little, Andrew, Abbott, Jason R., Sun, Qi, Gmachl, Michael, Rudolph, Dorothea, Arnhof, Heribert, Rumpel, Klaus, Savarese, Fabio, Gerstberger, Thomas, Mischerikow, Nikolai, Treu, Matthias, Herdeis, Lorenz, Wunberg, Tobias, Gollner, Andreas, Weinstabl, Harald, Mantoulidis, Andreas, Krämer, Oliver, McConnell, Darryl B., W. Fesik, Stephen
Published in Journal of medicinal chemistry (10.11.2022)

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Journal Article

Oligonucleotide Analogues with Integrated Bases and Backbone Part 30 Synthesis and Association of a Self-Complementary Thiomethylene-Linked Octanucleoside

Oligonucleotide Analogues with Integrated Bases and Backbone Part 30 Synthesis and Association of a Self-Complementary Thiomethylene-Linked Octanucleoside

by Herdeis, Lorenz, Thomas, Siji, Bernet, Bruno, Vasella, Andrea
Published in Helvetica chimica acta (01.07.2013)

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Journal Article

Abstract B103: Development and characterisation of KRASmulti inhibitors for the treatment of KRAS mutant pancreatic ductal adenocarcinoma

Abstract B103: Development and characterisation of KRASmulti inhibitors for the treatment of KRAS mutant pancreatic ductal adenocarcinoma

by Tedeschi, Antonio, Schaaf, Otmar, Gmachl, Michael, Herdeis, Lorenz, Rocchetti, Francesca, Popow, Johannes, Schischlik, Fiorella, Gerlach, Daniel, Lipp, Jesse, Bröker, Joachim, Mantoulidis, Andreas, Smethurst, Chris, Kessler, Dirk, Boettcher, Jark, Wunberg, Tobias, Santoro, Valeria, Waterson, Alex, Phan, Jason, Little, Andrew, Abbott, Jason, Sun, Qi, Fesik, Stephen, Mcconnell, Darryl, Pearson, Mark A., Kraut, Norbert, Rudolph, Dorothea
Published in Cancer research (Chicago, Ill.) (16.01.2024)

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Journal Article

Abstract A087: BI KRASmulti, a first-in-class, orally bioavailable and direct inhibitor of diverse oncogenic KRAS variants drives tumor regression in KRAS G12V-driven preclinical models

Abstract A087: BI KRASmulti, a first-in-class, orally bioavailable and direct inhibitor of diverse oncogenic KRAS variants drives tumor regression in KRAS G12V-driven preclinical models

by Peng, David H, Tedeschi, Antonio, Herdeis, Lorenz, Savarese, Fabio, Rocchetti, Francesca, Johannes, Popow, Huber, Heinrich J, Melillo, Nicola, Dickinson, Jake, Mistry, Hitesh B, Wilding, Birgit, Treu, Matthias, Fuchs, Julian, Broker, Joachim, Wunberg, Tobias, Schischlik, Fiorella, Lipp, Jesse, Ramamoorthy, Vandhana, Daniele, Joseph R, Kopetz, Scott, Kim, Michael, Gibbons, Don L, Vellano, Christopher P, Marszalek, Joseph R, Heffernan, Timothy P, McConnell, Darryl, Pearson, Mark, Kraut, Norbert, Rudolph, Dorothea
Published in Molecular cancer therapeutics (01.12.2023)

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Journal Article

Abstract A085: BI KRASmulti, a first-in-class, orally bioavailable and direct inhibitor of diverse oncogenic KRAS variants drives tumor regression in preclinical models and validates wild-type amplified KRAS as a therapeutic target

Abstract A085: BI KRASmulti, a first-in-class, orally bioavailable and direct inhibitor of diverse oncogenic KRAS variants drives tumor regression in preclinical models and validates wild-type amplified KRAS as a therapeutic target

by Tedeschi, Antonio, Herdeis, Lorenz, Santoro, Valeria, Savarese, Fabio, Wilding, Birgit, Treu, Matthias, Fuchs, Julian, Bröker, Joachim, Wunberg, Tobias, Gmachl, Michael, Klaus, Rumpel, Schischlik, Fiorella, Lipp, Jesse, Peng, David H., Williams, Mariah, Deckard, Charles, Ramamoorthy, Vandhana, Daniele, Joseph R., Ajani, Jaffer A., Meric-Bernstam, Funda, Vellano, Christopher P., Marszalek, Joseph R., Heffernan, Timothy P., McConnell, Darryl, Pearson, Mark, Kraut, Norbert, Rudolph, Dorothea
Published in Molecular cancer therapeutics (01.12.2023)

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Journal Article

Abstract A092: Determinants of sensitivity to BI KRASmulti inhibitor using high-throughput in-vitro drug screens

Abstract A092: Determinants of sensitivity to BI KRASmulti inhibitor using high-throughput in-vitro drug screens

by Schischlik, Fiorella, Tedeschi, Antonio, Rudolph, Dorothea, Gerlach, Daniel, Wilding, Birgit, Treu, Matthias, Fuchs, Julian, Herdeis, Lorenz, Broeker, Joachim, Wunberg, Tobias, Boghossian, Andrew S., Rees, Matthew G., Ronan, Melissa M., Roth, Jennifer A., McConnell, Darryl, Pearson, Mark, Kraut, Norbert, Haslinger, Christian, Lipp, Jesse
Published in Molecular cancer therapeutics (01.12.2023)

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Journal Article

암 치료를 위한 고리형 2-아미노-3-시아노 티오펜 및 유도체

암 치료를 위한 고리형 2-아미노-3-시아노 티오펜 및 유도체

by GOLLNER ANDREAS, STADTMUELLER HEINZ, TREU MATTHIAS, LITTLE ANDREW, MANTOULIDIS ANDREAS, CUI JIANWEN, HODGES TIM, PHAN JASON, HERDEIS LORENZ, SMETHURST CHRISTIAN ALAN PAUL, WUNBERG TOBIAS, SARKAR DHRUBA, SOKOL KEVIN, WILDING BIRGIT, FUCHS JULIAN, WATERSON ALEX, FESIK STEPHEN W, BROEKER JOACHIM, RAMHARTER JUERGEN, ABBOTT JASON, SUN QI
Year of Publication 27.08.2024

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Patent

Oligonucleotide Analogues with Integrated Bases and Backbone. Part 30

Oligonucleotide Analogues with Integrated Bases and Backbone. Part 30

by Herdeis, Lorenz, Thomas, Siji, Bernet, Bruno, Vasella, Andrea
Published in Helvetica chimica acta (01.07.2013)

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Journal Article

Abstract 3321: KRASmulti inhibitor BI 3706674, an orally bioavailable, direct inhibitor of diverse oncogenic KRAS variants drives tumor regression in KRASG12V-driven preclinical models

Abstract 3321: KRASmulti inhibitor BI 3706674, an orally bioavailable, direct inhibitor of diverse oncogenic KRAS variants drives tumor regression in KRASG12V-driven preclinical models

by Peng, David Hwa, Tedeschi, Antonio, Herdeis, Lorenz, Schaaf, Otmar, Savarese, Fabio, Rocchetti, Francesca, Popow, Johannes, Huber, Heinrich J., Wilding, Birgit, Treu, Matthias, Fuchs, Julian, Bröeker, Joachim, Wunberg, Tobias, Schischlik, Firoella, Lipp, Jesse, Williams, Mariah, Chandler, Vaness, Deckard, Charles E., Ramamoorthy, Vandhana, Daniele, Joseph R., Kopetz, Scott, Kim, Michael, Gibbons, Don L., Vellano, Christopher P., Marszalek, Joseph R., Heffernan, TImothy P., McConnell, Darryl, Pearson, Mark, Kraut, Norbert, Rudolph, Dorothea
Published in Cancer research (Chicago, Ill.) (22.03.2024)

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Journal Article

Oligonucleotide Analogues with Integrated Bases and Backbone Part 32 Thiomethylene- and Aminomethylene-Linked GG Dinucleosides of the ONIB Type: Formation of Quadruplexes

Oligonucleotide Analogues with Integrated Bases and Backbone Part 32 Thiomethylene- and Aminomethylene-Linked GG Dinucleosides of the ONIB Type: Formation of Quadruplexes

by Schulze-Adams, Martina, Bernet, Bruno, Touboul, David, Egli, Daniel, Herdeis, Lorenz, Vasella, Andrea
Published in Helvetica chimica acta (01.09.2014)

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Journal Article

Oligonucleotide Analogues with Integrated Bases and Backbone. Part 32

Oligonucleotide Analogues with Integrated Bases and Backbone. Part 32

by Schulze-Adams, Martina, Bernet, Bruno, Touboul, David, Egli, Daniel, Herdeis, Lorenz, Vasella, Andrea
Published in Helvetica chimica acta (01.09.2014)

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Journal Article

Abstract 3317: KRASmulti inhibitor BI 3706674 shows efficacy in KRAS-driven preclinical models of cancer that supports clinical testing in patients with tumors harbouring KRASG12V mutations and KRAS wild-type amplifications

Abstract 3317: KRASmulti inhibitor BI 3706674 shows efficacy in KRAS-driven preclinical models of cancer that supports clinical testing in patients with tumors harbouring KRASG12V mutations and KRAS wild-type amplifications

by Tedeschi, Antonio, Peng, David H., Schischlik, Fiorella, Herdeis, Lorenz, Schaaf, Otmar, Santoro, Valeria, Gerlach, Daniel, Savarese, Fabio, Lipp, Jesse, Haslinger, Christian, Rocchetti, Francesca, Popow, Johannes, Huber, Heinrich J., Wilding, Birgit, Treu, Matthias, Fuchs, Julian, Broeker, Joachim, Wunber, Tobias, Gmachl, Michael, Rumpel, Klaus, Rees, Matthew, Ron, Melissa, Roth, Jennifer, Williams, Mariah, Deckard, Charles, Ramamoorthy, Vandhana, Daniele, Joseph R., Ajani, Jaffer A., Meric-Bernstam, Funda, Kopetz, Scott, Kim, Michael, Gibbons, Don L., Vellano, Christopher P., Marszalek, Joseph R., Heffernan, Timothy P., McConnell, Darryl, Pearson, Mark, Kraut, Norbert, Rudolph, Dorothea
Published in Cancer research (Chicago, Ill.) (22.03.2024)

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Journal Article

Oligonucleotide Analogues with Integrated Bases and Backbone. Part 27

Oligonucleotide Analogues with Integrated Bases and Backbone. Part 27

by Herdeis, Lorenz, Bernet, Bruno, Augustine, Anu, Kälin, Roland E., Brändli, André W., Vasella, Andrea
Published in Helvetica chimica acta (01.04.2011)

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Journal Article

Diastereoselective Formation of Metallamacrocyclic (Arene)RuII and CpRhIII Complexes

Diastereoselective Formation of Metallamacrocyclic (Arene)RuII and CpRhIII Complexes

by Lehaire, Marie-Line, Scopelliti, Rosario, Herdeis, Lorenz, Polborn, Kurt, Mayer, Peter, Severin, Kay
Published in Inorganic chemistry (08.03.2004)

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Journal Article

Oligonucleotide Analogues with Integrated Bases and Backbone Part 27 Synthesis and Association of Thiomethylene-Linked Cytidine-Derived Dinucleosides and Tetranucleosides

Oligonucleotide Analogues with Integrated Bases and Backbone Part 27 Synthesis and Association of Thiomethylene-Linked Cytidine-Derived Dinucleosides and Tetranucleosides

by Herdeis, Lorenz, Bernet, Bruno, Augustine, Anu, Kaelin, Roland E., Braendli, Andre W., Vasella, Andrea
Published in Helvetica chimica acta (01.04.2011)

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Journal Article

Diastereoselective formation of metallamacrocyclic (arene)Ru(II) and CpRh(III) complexes

Diastereoselective formation of metallamacrocyclic (arene)Ru(II) and CpRh(III) complexes

by Lehaire, Marie-Line, Scopelliti, Rosario, Herdeis, Lorenz, Polborn, Kurt, Mayer, Peter, Severin, Kay
Published in Inorganic chemistry (08.03.2004)

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Journal Article

Diastereoselective Formation of Metallamacrocyclic (Arene)Ru II and CpRh III Complexes

Diastereoselective Formation of Metallamacrocyclic (Arene)Ru II and CpRh III Complexes

by Lehaire, Marie-Line, Scopelliti, Rosario, Herdeis, Lorenz, Polborn, Kurt, Mayer, Peter, Severin, Kay
Published in Inorganic chemistry (01.03.2004)

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Journal Article