Richard Alan Engh
Professor, Biomolekylær og strukturkjemi, Norstruct
Stillingsbeskrivelse
Professor, Biomolekylær og strukturkjemi, Norstruct
- Lorenz, Robin; Wu, Jian; Herberg, Friedrich W.; Taylor, Susan; Engh, Richard Alan. Drugging the Undruggable: How Isoquinolines and PKA Initiated the Era of Designed Protein Kinase Inhibitor Therapeutics. Biochemistry 2021; Volum 60 (46). ISSN 0006-2960.s 3470 - 3484.s doi: 10.1021/acs.biochem.1c00359.
- Stensen, Wenche; Rothweiler, Ulli; Engh, Richard Alan; Stasko, Melissa R.; Bederman, Ilya; Costa, Alberto C. S.; Fugelli, Anders; Svendsen, John Sigurd Mjøen. Novel DYRK1A Inhibitor Rescues Learning and Memory Deficits in a Mouse Model of Down Syndrome. (fulltekst) Pharmaceuticals 2021; Volum 14. ISSN 1424-8247.s doi: 10.3390/ph14111170.
- Alam, Kazi Asraful; Gani, Osman; Engh, Richard Alan. Inhibitor binding of mutants of protein kinase A with GGGXXG and GXGXXA glycine-rich loop motifs. Journal of Molecular Recognition 2020; Volum 2020. ISSN 0952-3499.s doi: 10.1002/jmr.2882.
- Tarnowski, Krzysztof; Klimecka, Maria; Ciesielski, Arkadiusz; Goch, Grazyna; Kulik, Anna; Fedak, Halina; Poznanski, Jaroslaw; Lichocka, Malgorzata; Pierechod, Marcin Miroslaw; Engh, Richard Alan; Dadlez, Michal; Dobrowolska, Grazyna; Bucholc, Maria. Two SnRK2-Interacting Calcium Sensor Isoforms Negatively Regulate SnRK2 Activity by Different Mechanisms. Plant Physiology 2020; Volum 182 (2). ISSN 0032-0889.s 1142 - 1160.s doi: 10.1104/pp.19.00900.
- Thakkar, Balmukund; Engh, Richard Alan. Comparative conformational analyses and molecular dynamics studies of glycylglycine methyl ester and glycylglycine N -methylamide. (fulltekst) RSC Advances 2018; Volum 8 (8). ISSN 2046-2069.s 4445 - 4453.s doi: 10.1039/c7ra13712e.
- Thakkar, Balmukund; Svendsen, John Sigurd Mjøen; Engh, Richard Alan. Density Functional Studies on Secondary Amides: Role of Steric Factors in Cis/Trans Isomerization. (data) (fulltekst) (sammendrag) Molecules 2018; Volum 23. ISSN 1420-3049.s doi: 10.3390/molecules23102455.
- Czarna, Anna Lucja; Jinhua, Wang; Zelencova, Diana; Liu, Yao; Deng, Xianming; Choi, Hwan Geun; Zhang, Tinghu; Zhou, Wenjun; Chang, Jae Won; Kildalsen, Hanne; Seternes, Ole Morten; Gray, Nathanael S.; Engh, Richard Alan; Rothweiler, Ulli. Novel Scaffolds for Dual Specificity Tyrosine-Phosphorylation-Regulated Kinase (DYRK1A) Inhibitors. Journal of Medicinal Chemistry 2018; Volum 61 (17). ISSN 0022-2623.s 7560 - 7572.s doi: 10.1021/acs.jmedchem.7b01847.
- Thakkar, Balmukund; Albrigtsen, Marte; Svendsen, John Sigurd Mjøen; Andersen, Jeanette hammer; Engh, Richard Alan. Biofocussed chemoprospecting: An efficient approach for drug discovery. (fulltekst) (sammendrag) Chemical Biology and Drug Design (CB&DD) 2017; Volum 90 (1). ISSN 1747-0277.s 128 - 140.s doi: 10.1111/cbdd.12934.
- Thakkar, Balmukund; Svendsen, John Sigurd Mjøen; Engh, Richard Alan. Cis/Trans Isomerization in Secondary Amides: Reaction Paths, Nitrogen Inversion and Relevance to Peptidic Systems. (fulltekst) Journal of Physical Chemistry A 2017; Volum 121 (36). ISSN 1089-5639.s 6830 - 6837.s doi: 10.1021/acs.jpca.7b05584.
- Narayanan, Dilip; Gani, Osman; Gruber, Franz; Engh, Richard Alan. Data driven polypharmacological drug design for lung cancer: Analyses for targeting ALK, MET, and EGFR. Journal of Cheminformatics 2017; Volum 9 (43). ISSN 1758-2946.s 1 - 19.s doi: 10.1186/s13321-017-0229-8.
- Woywod, Clemens Joachim; Gruber, Franz; Engh, Richard Alan; Flå, Tor. Dynamical models of mutated chronic myelogenous leukemia cells for a postimatinib treatment scenario: Response to dasatinib or nilotinib therapy. PLOS ONE 2017; Volum 12 (7). ISSN 1932-6203.s doi: 10.1371/journal.pone.0179700.
- Ivan, Taavi; Enkvist, Erki; Viira, Birgit; Manoharan, Ganesh babu; Raidaru, Gerda; Pflug, Alexander; Alam, Kazi Asraful; Zaccolo, Manuela; Engh, Richard Alan; Uri, Asko. Bifunctional ligands for inhibition of tight-binding protein-protein interactions. Bioconjugate chemistry 2016; Volum 27 (8). ISSN 1043-1802.s 1900 - 1910.s doi: 10.1021/acs.bioconjchem.6b00293.
- Rothweiler, Ulli; Stensen, Wenche; Brandsdal, Bjørn Olav; Isaksson, Johan; Leeson, Frederick Alan; Engh, Richard Alan; Svendsen, John Sigurd Mjøen. Probing the ATP-Binding Pocket of Protein Kinase DYRK1A with Benzothiazole Fragment Molecules. Journal of Medicinal Chemistry 2016; Volum 59 (21). ISSN 0022-2623.s 9814 - 9824.s doi: 10.1021/acs.jmedchem.6b01086.
- Rothweiler, Ulli; Eriksson, Jonas; Stensen, Wenche; Leeson, Frederick Alan; Engh, Richard Alan; Svendsen, John Sigurd. Luciferin and derivatives as a DYRK selective scaffold for the design of protein kinase inhibitors. European Journal of Medicinal Chemistry 2015; Volum 94. ISSN 0223-5234.s 140 - 148.s doi: 10.1016/j.ejmech.2015.02.035.
- Alexeeva, Marina; Åberg, espen; Engh, Richard Alan; Rothweiler, Ulli. The structure of a dual-specificity tyrosine phosphorylation-regulated kinase 1A-PKC412 complex reveals disulfide-bridge formation with the anomalous catalytic loop HRD(HCD) cysteine.. Acta Crystallographica Section D: Biological Crystallography 2015; Volum 71. ISSN 0907-4449.s 1207 - 1215.s doi: 10.1107/S1399004715005106.
- Gani, Osman A.B.S.M.; Thakkar, Balmukund; Narayanan, Dilip; Alam, Kazi Asraful; Kyomuhendo, Peter; Rothweiler, Ulli; Tello-Franco, Veronica; Engh, Richard Alan. Assessing protein kinase target similarity: Comparing sequence, structure, and cheminformatics approaches. (fulltekst) Biochimica et Biophysica Acta - Proteins and Proteomics 2015; Volum 1854 (10). ISSN 1570-9639.s 1605 - 1616.s doi: 10.1016/j.bbapap.2015.05.004.
- Martin, Eric; Knapp, Stefan; Engh, Richard Alan; Moebitz, Henrik; Varin, Thibault; Roux, Benoit; Meiler, Jens; Berdini, Valerio; Baumann, Alexander; Vieth, Michal. Perspective on computational and structural aspects of kinase discovery from IPK2014. Biochimica et Biophysica Acta - Proteins and Proteomics 2015; Volum 1854 (10). ISSN 1570-9639.s 1595 - 1604.s doi: 10.1016/j.bbapap.2015.03.014.
- Lauber, Birgit S.; Hardegger, Leo A.; Alam, Kazi Asraful; Lund, Bjarte Aarmo; Dumele, Oliver; Harder, Michael; Kuhn, Bernd; Engh, Richard Alan; Diederich, François. Addressing the Glycine-Rich Loop of Protein Kinases by a Multi-Facetted Interaction Network: Inhibition of PKA and a PKB Mimic. Chemistry - A European Journal 2015; Volum 22 (1). ISSN 0947-6539.s 211 - 221.s doi: 10.1002/chem.201503552.
- Illert, Anna L; Seitz, Anna K.; Rummelt, Christoph; Kreutmair, Stefanie; Engh, Richard Alan; Goodstal, Samantha; Peschel, Christian; Duyster, Justus; von Bubnoff, Nikolas. Inhibition of aurora kinase B is important for biologic activity of the dual inhibitors of BCR-ABL and aurora kinases R763/ AS703569 and PHA-739358 in BCR-ABL transformed cells. PLOS ONE 2014; Volum 9 (11). ISSN 1932-6203.s doi: 10.1371/journal.pone.0112318.
- Gani, Osman A.B.S.M.; Narayanan, Dilip; Engh, Richard Alan. Evaluating the Predictivity of Virtual Screening for Abl Kinase Inhibitors to Hinder Drug Resistance. Chemical Biology and Drug Design (CB&DD) 2013; Volum 82 (5). ISSN 1747-0277.s 506 - 519.s doi: 10.1111/cbdd.12170.
- Åberg, espen; Lund, Bjarte Aarmo; Pflug, Alexander; Gani, Osman A.B.S.M.; Rothweiler, Ulli; Oliveira, Taiana Maia De; Engh, Richard Alan. Structural origins of AGC protein kinase inhibitor selectivities: PKA as a drug discovery tool. Biological chemistry 2012; Volum 393 (10). ISSN 1431-6730.s 1121 - 1129.s doi: 10.1515/hsz-2012-0248.
- Pflug, Alexander; Johnson, Kenneth; Engh, Richard Alan. Anomalous dispersion analysis of inhibitor flexibility: a case study of the kinase inhibitor H-89. Acta Crystallographica. Section F : Structural Biology and Crystallization Communications 2012; Volum 68. ISSN 1744-3091.s 873 - 877.s doi: 10.1107/S1744309112028655.
- Østnes Hanssen, Kine; Andersen, Jeanette hammer; Stiberg, Trine; Engh, Richard Alan; Svenson, Johan; Genevière, Anne-Marie; Hansen, Espen. Antitumoral and Mechanistic Studies of Ianthelline Isolated from the Arctic Sponge Stryphnus fortis. Anticancer Research 2012; Volum 32 (10). ISSN 0250-7005.s 4287 - 4297.
- von Bubnoff, N.; Gorantla, S.P.; Engh, Richard Alan; Oliveira, Taiana Maia De; Thöne, S.; Åberg, espen; Peschel, C.; Duyster, J.. The low frequency of clinical resistance to PDGFR inhibitors in myeloid neoplasms with abnormalities of PDGFRA might be related to the limited repertoire of possible PDGFRA kinase domain mutations in vitro. Oncogene 2011; Volum 30 (8). ISSN 0950-9232.s 933 - 943.s doi: 10.1038/onc.2010.476.
- Oliveira, Taiana Maia De; Ahmad, Rafi; Engh, Richard Alan. VX680 Binding in Aurora A: pi-pi Interactions Involving the Conserved Aromatic Amino Acid of the Flexible Glycine-Rich Loop. Journal of Physical Chemistry A 2011; Volum 115 (16). ISSN 1089-5639.s 3895 - 3904.s doi: 10.1021/jp108286r.
- Rothweiler, Ulli; Åberg, espen; Johnson, Kenneth; Hansen, Tom Egil; Jørgensen, Jorunn B; Engh, Richard Alan. p38 alpha MAP Kinase Dimers with Swapped Activation Segments and a Novel Catalytic Loop Conformation. Journal of Molecular Biology (JMB) 2011; Volum 411 (2). ISSN 0022-2836.s 474 - 485.s doi: 10.1016/j.jmb.2011.06.013.
- Pflug, Alexander; Oliveira, Taiana Maia De; Bossemeyer, Dirk; Engh, Richard Alan. Mutants of protein kinase A that mimic the ATP-binding site of Aurora kinase. Biochemical Journal 2011; Volum 440. ISSN 0264-6021.s 85 - 93.s doi: 10.1042/BJ20110592.
- Kancha, Rama Krishna; von Bubnoff, Nikolas; Bartosch, Natalie; Peschel, Christian; Engh, Richard Alan; Duyster, Justus. Differential sensitivity of ERBB2 kinase domain mutations towards lapatinib. PLOS ONE 2011; Volum 6(10):e26760. ISSN 1932-6203.s doi: 10.1371/journal.pone.0026760.
- Prime, ME; Courtney, SM; Brookfield, FA; Marston, RW; Walker, V; Warne, J; Boyd, AE; Kairies, NA; Von der Saal, W; Limberg, A; Georges, G; Engh, Richard Alan; Goller, B; Rueger, P; Rueth, M. Phthalazinone pyrazoles as potent, selective, and orally bioavailable inhibitors of Aurora-A kinase. Journal of Medicinal Chemistry 2011; Volum 54 (1). ISSN 0022-2623.s 312 - 319.s doi: 10.1021/jm101346r.
- Gani, Osman A.B.S.M.; Engh, Richard Alan. Protein kinase inhibition of clinically important staurosporine analogues. Natural product reports (Print) 2010; Volum 27 (4). ISSN 0265-0568.s 489 - 498.s doi: 10.1039/b923848b.
- Pflug, Alexander; Rogozina, Jevgenia; Lavogina, Darja; Enkvist, Erki; Uri, Asko; Engh, Richard Alan; Bossemeyer, Dirk. Diversity of Bisubstrate Binding Modes of Adenosine Analogue-Oligoarginine Conjugates in Protein Kinase A and Implications for Protein Substrate Interactions. Journal of Molecular Biology (JMB) 2010; Volum 403 (1). ISSN 0022-2836.s 66 - 77.s doi: 10.1016/j.jmb.2010.08.028.
- Pflug, Alexander; de Oliveira, Taianá Maia; Bossemeyer, Dirk; Engh, Richard Alan. Mutants of protein kinase A with Aurora kinase inhibitor specificity. Acta Biochimica Polonica 2009. ISSN 0001-527X.s 66 - 67.
- von Bubnoff, N; Engh, Richard Alan; Åberg, espen; Sanger, J; Peschel, C; Duyster, J. FMS-Like Tyrosine Kinase 3-Internal Tandem Duplication Tyrosine Kinase Inhibitors Display a Nonoverlapping Profile of Resistance Mutations In vitro. Cancer Research 2009; Volum 69 (7). ISSN 0008-5472.s 3032 - 3041.s doi: 10.1158/0008-5472.CAN-08-2923.
- Engh, Richard Alan. Protein kinase inhibitors highlight the complexities of drug-target non-covalent interactions. Biotechnology & Biotechnological Equipment (Sofia) 2008; Volum 22. ISSN 1310-2818.s 772 - 777.
Forskningsinteresser
Enzym-ligand vekselvirkninger
Drug design
Cheminformatics