Discovery of potent Mcl-1/Bcl-xL dual inhibitors by using a hybridization strategy based on structural analysis of target proteins Y Tanaka, K Aikawa, G Nishida, M Homma, S Sogabe, S Igaki, Y Hayano, ... Journal of medicinal chemistry 56 (23), 9635-9645, 2013 | 130 | 2013 |
K-Ras (G12D)-selective inhibitory peptides generated by random peptide T7 phage display technology K Sakamoto, Y Kamada, T Sameshima, M Yaguchi, A Niida, S Sasaki, ... Biochemical and biophysical research communications 484 (3), 605-611, 2017 | 123 | 2017 |
Derivatization of inhibitor of apoptosis protein (IAP) ligands yields improved inducers of estrogen receptor α degradation N Ohoka, Y Morita, K Nagai, K Shimokawa, O Ujikawa, I Fujimori, M Ito, ... Journal of Biological Chemistry 293 (18), 6776-6790, 2018 | 115 | 2018 |
Development of protein degradation inducers of oncogenic BCR‐ABL protein by conjugation of ABL kinase inhibitors and IAP ligands N Shibata, N Miyamoto, K Nagai, K Shimokawa, T Sameshima, N Ohoka, ... Cancer science 108 (8), 1657-1666, 2017 | 113 | 2017 |
Targeting the allosteric site of oncoprotein BCR-ABL as an alternative strategy for effective target protein degradation K Shimokawa, N Shibata, T Sameshima, N Miyamoto, O Ujikawa, H Nara, ... ACS medicinal chemistry letters 8 (10), 1042-1047, 2017 | 99 | 2017 |
Crystal structure of a human K-Ras G12D mutant in complex with GDP and the cyclic inhibitory peptide KRpep-2d S Sogabe, Y Kamada, M Miwa, A Niida, T Sameshima, M Kamaura, ... ACS medicinal chemistry letters 8 (7), 732-736, 2017 | 83 | 2017 |
Football-and Bullet-shaped GroEL-GroES Complexes Coexist during the Reaction Cycle*♦ T Sameshima, T Ueno, R Iizuka, N Ishii, N Terada, K Okabe, T Funatsu Journal of Biological Chemistry 283 (35), 23765-23773, 2008 | 58 | 2008 |
Pharmacological difference between degrader and inhibitor against oncogenic BCR-ABL kinase N Shibata, K Shimokawa, K Nagai, N Ohoka, T Hattori, N Miyamoto, ... Scientific reports 8 (1), 13549, 2018 | 57 | 2018 |
Rapid Determination of the Specificity Constant of Irreversible Inhibitors (kinact/KI) by Means of an Endpoint Competition Assay I Miyahisa, T Sameshima, MS Hixon Angewandte Chemie 127 (47), 14305-14308, 2015 | 56 | 2015 |
Denatured proteins facilitate the formation of the football-shaped GroEL–(GroES)2 complex T Sameshima, R Iizuka, T Ueno, T Funatsu Biochemical Journal 427 (2), 247-254, 2010 | 55 | 2010 |
Investigation of the structural requirements of K-Ras (G12D) selective inhibitory peptide KRpep-2d using alanine scans and cysteine bridging A Niida, S Sasaki, K Yonemori, T Sameshima, M Yaguchi, T Asami, ... Bioorganic & medicinal chemistry letters 27 (12), 2757-2761, 2017 | 52 | 2017 |
Single-molecule study on the decay process of the football-shaped GroEL-GroES complex using zero-mode waveguides T Sameshima, R Iizuka, T Ueno, J Wada, M Aoki, N Shimamoto, ... Journal of Biological Chemistry 285 (30), 23159-23164, 2010 | 52 | 2010 |
Discovery of 3-Benzyl-1-(trans-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-arylurea Derivatives as Novel and Selective Cyclin-Dependent Kinase 12 (CDK12 … M Ito, T Tanaka, A Toita, N Uchiyama, H Kokubo, N Morishita, MG Klein, ... Journal of medicinal chemistry 61 (17), 7710-7728, 2018 | 49 | 2018 |
Different degradation mechanisms of inhibitor of apoptosis proteins (IAPs) by the specific and nongenetic IAP-dependent protein eraser (SNIPER) N Ohoka, O Ujikawa, K Shimokawa, T Sameshima, N Shibata, T Hattori, ... Chemical and Pharmaceutical Bulletin 67 (3), 203-209, 2019 | 46 | 2019 |
Identification of novel, potent, and orally available GCN2 inhibitors with type I half binding mode J Fujimoto, O Kurasawa, T Takagi, X Liu, H Banno, T Kojima, Y Asano, ... ACS Medicinal Chemistry Letters 10 (10), 1498-1503, 2019 | 40 | 2019 |
Discovery of an irreversible and cell-active BCL6 inhibitor selectively targeting Cys53 located at the protein–protein interaction interface T Sameshima, T Yamamoto, O Sano, S Sogabe, S Igaki, K Sakamoto, ... Biochemistry 57 (8), 1369-1379, 2018 | 27 | 2018 |
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application Y Hirozane, M Toyofuku, T Yogo, Y Tanaka, T Sameshima, I Miyahisa, ... Bioorganic & medicinal chemistry letters 29 (21), 126641, 2019 | 17 | 2019 |
Small-scale panel comprising diverse gene family targets to evaluate compound promiscuity T Sameshima, T Yukawa, Y Hirozane, M Yoshikawa, T Katoh, H Hara, ... Chemical Research in Toxicology 33 (1), 154-161, 2019 | 13 | 2019 |
High-throughput quantitative intrinsic thiol reactivity evaluation using a fluorescence-based competitive endpoint assay T Sameshima, I Miyahisa, S Yamasaki, M Gotou, T Kobayashi, ... SLAS DISCOVERY: Advancing Life Sciences R&D 22 (9), 1168-1174, 2017 | 13 | 2017 |
Rapid multi-reagents exchange TIRFM microfluidic system for single biomolecular imaging T Arakawa, T Sameshima, Y Sato, T Ueno, Y Shirasaki, T Funatsu, S Shoji Sensors and Actuators B: Chemical 128 (1), 218-225, 2007 | 8 | 2007 |