Richard Alan Engh

Professor, Biomolekylær og strukturkjemi, Norstruct Institutt for kjemi

77644073

richard.engh@uit.no

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Tromsø

FPARK G 222 (Klikk for større kartbeskrivelse)

Enzym-ligand vekselvirkninger

Drug design

Cheminformatics

Vitenskapelige artikler og bokkapitler
Andre

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.

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.

Thakkar, Balmukund; Engh, Richard Alan. Comparative conformational analyses and molecular dynamics studies of glycylglycine methyl ester and glycylglycine N -methylamide. (Fulltekst: http://pubs.rsc.org/en/content/articlelanding/2018/ra/c7ra13712e RSC Advances 2018; Volum 8 (8). ISSN 2046-2069.s 4445 - 4453.s doi: 10.1039/c7ra13712e.

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; Svendsen, John Sigurd Mjøen; Engh, Richard Alan. Density Functional Studies on Secondary Amides: Role of Steric Factors in Cis/Trans Isomerization. (https://www.mdpi.com/1420-3049/23/10/2455/s1) (Fulltekst: https://www.mdpi.com/1420-3049/23/10/2455/htm (Sammendrag: https://www.mdpi.com/1420-3049/23/10/2455) Molecules 2018; Volum 23. ISSN 1420-3049.s doi: 10.3390/molecules23102455.

Thakkar, Balmukund; Albrigtsen, Marte; Svendsen, John Sigurd Mjøen; Andersen, Jeanette hammer; Engh, Richard Alan. Biofocussed chemoprospecting: An efficient approach for drug discovery. (Fulltekst: http://onlinelibrary.wiley.com/doi/10.1111/cbdd.12934/full (Sammendrag: http://onlinelibrary.wiley.com/wol1/doi/10.1111/cbdd.12934/abstract) Chemical Biology and Drug Design (CB&DD) 2017; Volum 90 (1). ISSN 1747-0277.s 128 - 140.s doi: 10.1111/cbdd.12934.

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.

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.

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: http://pubs.acs.org/doi/10.1021/acs.jpca.7b05584 Journal of Physical Chemistry A 2017; Volum 121 (36). ISSN 1089-5639.s 6830 - 6837.s doi: 10.1021/acs.jpca.7b05584.

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.

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; 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.

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.

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.

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: https://www.sciencedirect.com/science/article/pii/S1570963915001442 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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

Engh, Richard Alan. Diversity of target profiles for ABL kinase inhibitors. Symposium on "Current challenges and future strategies in haematology" 2019-04-04 - 2019-04-04 2019.

Engh, Richard Alan. Protein structures "in crystallo" and "in vivo: do they match? Are they useful?. 3rd MCBiology Symposium "The Secret Life of the Cell" 2018-11-22 - 2018-11-22 2018.

Engh, Richard Alan. Prospects for linking TKI protein kinase inhibition profiles to CML modelling parameters. 19th Annual John Goldman Conference on Chronic Myeloid Leukemia: Biology and Therapy 2017-10-12 - 2017-10-15 2017.

Engh, Richard Alan. Unpredictable protein kinase flexibility: curse or blessing for inhibitor discovery?. 2nd Annual MC-Biology Symposium 2016-11-17 - 2016-11-17 2016.

Thakkar, Balmukund; Gani, Osman; Engh, Richard Alan. Practical Applications of Informatics Tools to Identify Drug Targets for Novel Compounds from Bio- and Chemoprospecting. 52nd NBS contact meeting 2016-01-21 - 2016-01-24 2016.

Alam, Kazi Asraful; Rothweiler, Ulli; Engh, Richard Alan. Static and dynamic interactions between the glycine-rich loop of protein kinases and ATP site inhibitors. Norwegian Biochemical Society contact meeting 2016-01-21 - 2016-01-24 2016.

Boomgaren, Marc; Gani, Osman; Engh, Richard Alan; Hansen, Jørn H. Bioactive Heterocycle Libraries for Anticancer Drug Discovery - Development of Covalent Binding TK Inhibitors. Organikerdagarna 2016-06-14 - 2016-06-17 2016.

Thakkar, Balmukund; Engh, Richard Alan. PKA to Rho Kinase (ROCK): Assessing Structural Similarity via Surrogates. BioStruct Open Day 2015-03-20 - 2015-03-20 2015.

Alam, Kazi Asraful; Engh, Richard Alan. Selectivity Determinants of Aurora Kinases. Annual BioStruct Conference 2015 2015-08-27 - 2015-08-30 2015. 2015-08-27 - 2015-08-30 2015.

Alam, Kazi Asraful; Engh, Richard Alan. The Glycine Rich Loop As Selectivity Determinant For Protein Kinase Inhibitors. Annual BioStruct Conference 2015-08-27 - 2015-08-30 2015.

Boomgaren, Marc; Gani, Osman A.B.S.M.; Engh, Richard Alan; Hansen, Jørn H. Bioactive Heterocycle Libraries for Anticancer Drug Discovery. BioStruct/Molecular and Clinical Cancer Research School Open Day 2015-03-20 - 2015.

Thakkar, Balmukund; Hansen, Jørn H; Engh, Richard Alan. Design and Synthesis of Tartaric Acid Bisamides: Focus on Kinase Inhibition. BioStruct 4th Annual Conference 2013-08-29 - 2013-09-01 2013.

Thakkar, Balmukund; Svendsen, John Sigurd Mjøen; Engh, Richard Alan. Design and Synthesis of diverse Piperazine-2,5-diones and their uncyclized analogues as potential kinase inhibitors. BioStruct open day seminar 2013-05-08 - 2013-05-08 2013.

Åberg, espen; Seternes, Ole Morten; Engh, Richard Alan; Gruber, Franz. Fra Mutasjon til Medisin. Forskningsdagene i Tromsø 2013 - Kreftforeningens Stand 2013-09-20 - 2013-09-21 2013.

Gruber, Franz; Ernst, Thomas; Porkka, Kimmo; Engh, Richard Alan; Mikkola, ingvild; Maier, Jacqueline; Lange, Thoralf; Hochhaus, Andreas. Dynamics of the emergence of dasatinib and nilotinib resistance in imatinib-resistant CML patients. Leukemia 2012; Volum 26 (1). ISSN 0887-6924.s 172 - 177.s doi: 10.1038/leu.2011.187.

Kancha, RK; von Bubnoff, N.; Bartosch, N; Peschel, C.; Engh, Richard Alan; Duyster, J.. Irreversible inhibitors overcome lapatinib resistance due to ERBB2 kinase domain mutations. Onkologie (Basel) 2011; Volum 34. ISSN 0378-584X.s 118 - 118.

von Bubnoff, N; Gorantla, SP; Engh, Richard Alan; de Oliveira, Taianá Maia; Thoene, S; Åberg, espen; Peschel, C; Duyster, J. Sorafenib and Nilotinib Are Candidates to Overcome Imatinib Resistance in Myeloproliferation with FIP1L1-PDGFRA. Blood 2009; Volum 114 (22). ISSN 0006-4971.s 1138 - 1138.