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Targeting intrinsically disordered proteins in rational drug discovery

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Morgan A. Gingerich, Xueying Liu, Biaoxin Chai, Gemma L. Pearson, Michael P. Vincent, Tracy Stromer, Jie Zhu, Vaibhav Sidarala, Aaron Renberg, Debashish Sahu, Daniel J. Klionsky, Santiago Schnell & Scott A. Soleimanpour. (2023) An intrinsically disordered protein region encoded by the human disease gene CLEC16A regulates mitophagy. Autophagy 19:2, pages 525-543.
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Bi Zhao & Lukasz Kurgan. (2021) Surveying over 100 predictors of intrinsic disorder in proteins. Expert Review of Proteomics 18:12, pages 1019-1029.
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Deepak Kumar, Murali Aarthy, Prateek Kumar, Sanjeev Kumar Singh, Vladimir N. Uversky & Rajanish Giri. (2020) Targeting the NTPase site of Zika virus NS3 helicase for inhibitor discovery. Journal of Biomolecular Structure and Dynamics 38:16, pages 4827-4837.
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Marianne D. Sadar. (2020) Discovery of drugs that directly target the intrinsically disordered region of the androgen receptor. Expert Opinion on Drug Discovery 15:5, pages 551-560.
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Charles Oo & Suraj S. Kalbag. (2016) Leveraging the attributes of biologics and small molecules, and releasing the bottlenecks: a new wave of revolution in drug development. Expert Review of Clinical Pharmacology 9:6, pages 747-749.
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Articles from other publishers (58)

Shijie Xu & Akira Onoda. (2023) Accurate and Fast Prediction of Intrinsically Disordered Protein by Multiple Protein Language Models and Ensemble Learning. Journal of Chemical Information and Modeling.
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Mak Djulbegovic, David J. Taylor Gonzalez, Michael Antonietti, Vladimir N. Uversky, Carol L. Shields & Carol L. Karp. (2023) Intrinsic disorder may drive the interaction of PROS1 and MERTK in uveal melanoma. International Journal of Biological Macromolecules 250, pages 126027.
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Giovanna Viola, Fulvio Floriani, Carlo Giorgio Barracchia, Francesca Munari, Mariapina D'Onofrio & Michael Assfalg. (2023) Ultrasmall Gold Nanoparticles as Clients of Biomolecular Condensates. Chemistry – A European Journal 29:46.
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Sushmita Basu, Jörg Gsponer & Lukasz Kurgan. (2023) DEPICTER2: a comprehensive webserver for intrinsic disorder and disorder function prediction. Nucleic Acids Research 51:W1, pages W141-W147.
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Ki-Young Lee & Bong-Jin Lee. (2023) Dynamics-Based Regulatory Switches of Type II Antitoxins: Insights into New Antimicrobial Discovery. Antibiotics 12:4, pages 637.
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Shuqi Luo, Samuel Wohl, Wenwei Zheng & Sichun Yang. (2023) Biophysical and Integrative Characterization of Protein Intrinsic Disorder as a Prime Target for Drug Discovery. Biomolecules 13:3, pages 530.
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Bingqing Han, Chongjiao Ren, Wenda Wang, Jiashan Li & Xinqi Gong. (2023) Computational Prediction of Protein Intrinsically Disordered Region Related Interactions and Functions. Genes 14:2, pages 432.
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Mak B. Djulbegovic, David J. Taylor, Vladimir N. Uversky, Anat Galor, Carol L. Shields & Carol L. Karp. (2022) Intrinsic Disorder in BAP1 and Its Association with Uveal Melanoma. Genes 13:10, pages 1703.
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Arpita Das, Kuldeep Giri, Rama N. Behera, Sudipa Maity & Kiran Ambatipudi. (2022) BoMiProt 2.0: An update of the bovine milk protein database. Journal of Proteomics 267, pages 104696.
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Lukasz Kurgan. (2022) Resources for computational prediction of intrinsic disorder in proteins. Methods 204, pages 132-141.
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Carlo Giorgio Barracchia, Francesca Parolini, Angela Volpe, Daniele Gori, Francesca Munari, Stefano Capaldi, Mariapina D’Onofrio & Michael Assfalg. (2022) Camouflaged Fluorescent Silica Nanoparticles Target Aggregates and Condensates of the Amyloidogenic Protein Tau. Bioconjugate Chemistry 33:7, pages 1261-1268.
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Gregory-Neal W. Gomes, Ashley Namini & Claudiu C. Gradinaru. (2022) Integrative Conformational Ensembles of Sic1 Using Different Initial Pools and Optimization Methods. Frontiers in Molecular Biosciences 9.
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Haixiang Pei, Weikai Guo, Yangrui Peng, Hai Xiong & Yihua Chen. (2022) Targeting key proteins involved in transcriptional regulation for cancer therapy: Current strategies and future prospective. Medicinal Research Reviews 42:4, pages 1607-1660.
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Orkid Coskuner-Weber, Ozan Mirzanli & Vladimir N. Uversky. (2022) Intrinsically disordered proteins and proteins with intrinsically disordered regions in neurodegenerative diseases. Biophysical Reviews 14:3, pages 679-707.
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Chandra Has, P. Sivadas & Sovan Lal Das. (2022) Insights into Membrane Curvature Sensing and Membrane Remodeling by Intrinsically Disordered Proteins and Protein Regions. The Journal of Membrane Biology 255:2-3, pages 237-259.
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Sophia D. Staerz, Corey L. Jones & Jetze J. Tepe. (2022) Design, Synthesis, and Biological Evaluation of Potent 20S Proteasome Activators for the Potential Treatment of α-Synucleinopathies. Journal of Medicinal Chemistry 65:9, pages 6631-6642.
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Bruno Rizzuti. (2022) Molecular simulations of proteins: From simplified physical interactions to complex biological phenomena. Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics 1870:3, pages 140757.
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Guillermo Iruela, Alejandro Fernández, Amin Sagar, Francisco Javier Carvajal, Pau Bernadó & Miquel Pons. (2022) A FRET-Based Biosensor for the Src N-Terminal Regulatory Element. Biosensors 12:2, pages 96.
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Fanni Sebák, Péter Ecsédi, Wolfgang Bermel, Burkhard Luy, László Nyitray & Andrea Bodor. (2021) Selective 1 H α NMR Methods Reveal Functionally Relevant Proline cis/trans Isomers in Intrinsically Disordered Proteins: Characterization of Minor Forms, Effects of Phosphorylation, and Occurrence in Proteome . Angewandte Chemie International Edition 61:1.
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Fanni Sebák, Péter Ecsédi, Wolfgang Bermel, Burkhard Luy, László Nyitray & Andrea Bodor. (2021) Selective 1 H α NMR Methods Reveal Functionally Relevant Proline cis/trans Isomers in Intrinsically Disordered Proteins: Characterization of Minor Forms, Effects of Phosphorylation, and Occurrence in Proteome . Angewandte Chemie 134:1.
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Konda Mani Saravanan, Muthu Kannan, Prabhakar Meera, Nagaraj Bharathkumar & Thirunavukarasou Anand. (2022) E3 ligases: a potential multi-drug target for different types of cancers and neurological disorders. Future Medicinal Chemistry 14:3, pages 187-201.
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Bi Zhao & Lukasz Kurgan. (2022) Deep learning in prediction of intrinsic disorder in proteins. Computational and Structural Biotechnology Journal 20, pages 1286-1294.
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Alan Kadek, Kristina Lorenzen & Charlotte Uetrecht. (2021) In a flash of light: X-ray free electron lasers meet native mass spectrometry. Drug Discovery Today: Technologies 39, pages 89-99.
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Gang Hu, Akila Katuwawala, Kui Wang, Zhonghua Wu, Sina Ghadermarzi, Jianzhao Gao & Lukasz Kurgan. (2021) flDPnn: Accurate intrinsic disorder prediction with putative propensities of disorder functions. Nature Communications 12:1.
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Leonardo G. Dettori, Diego Torrejon, Arijita Chakraborty, Arijit Dutta, Mohamed Mohamed, Csaba Papp, Vladimir A. Kuznetsov, Patrick Sung, Wenyi Feng & Alaji Bah. (2021) A Tale of Loops and Tails: The Role of Intrinsically Disordered Protein Regions in R-Loop Recognition and Phase Separation. Frontiers in Molecular Biosciences 8.
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Mueed Ur Rahman, Ashfaq Ur Rehman, Taaha Arshad & Hai-Feng Chen. (2021) Disaggregation mechanism of prion amyloid for tweezer inhibitor. International Journal of Biological Macromolecules 176, pages 510-519.
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Ilinka Clerc, Amin Sagar, Alessandro Barducci, Nathalie Sibille, Pau Bernadó & Juan Cortés. (2021) The diversity of molecular interactions involving intrinsically disordered proteins: A molecular modeling perspective. Computational and Structural Biotechnology Journal 19, pages 3817-3828.
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Grzegorz M. Popowicz. 2021. Encyclopedia of Molecular Pharmacology. Encyclopedia of Molecular Pharmacology 1169 1179 .
Richard John Wheeler. (2020) Therapeutics—how to treat phase separation-associated diseases. Emerging Topics in Life Sciences 4:3, pages 331-342.
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Akila Katuwawala, Christopher J Oldfield & Lukasz Kurgan. (2020) Accuracy of protein-level disorder predictions. Briefings in Bioinformatics 21:5, pages 1509-1522.
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Jianlin Chen, Xiaorong Liu & Jianhan Chen. (2020) Targeting Intrinsically Disordered Proteins through Dynamic Interactions. Biomolecules 10:5, pages 743.
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Anchala Kumari, Pallavi Somvanshi & Abhinav Grover. (2020) Ameliorating amyloid aggregation through osmolytes as a probable therapeutic molecule against Alzheimer's disease and type 2 diabetes. RSC Advances 10:21, pages 12166-12182.
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Joseph Carmicheal, Pranita Atri, Sunandini Sharma, Sushil Kumar, Ramakanth Chirravuri Venkata, Prakash Kulkarni, Ravi Salgia, Dario Ghersi, Sukhwinder Kaur & Surinder K. Batra. (2020) Presence and structure‐activity relationship of intrinsically disordered regions across mucins. The FASEB Journal 34:2, pages 1939-1957.
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Vladimir N. Uversky. 2020. Structural Biology in Drug Discovery. Structural Biology in Drug Discovery 587 612 .
Kyle M. Alpha, Weiyi Xu & Christopher E. Turner. 2020. Actin Cytoskeleton in Cancer Progression and Metastasis - Part A. Actin Cytoskeleton in Cancer Progression and Metastasis - Part A 1 52 .
Grzegorz M. Popowicz. 2020. Encyclopedia of Molecular Pharmacology. Encyclopedia of Molecular Pharmacology 1 10 .
Sina Ghadermarzi, Xingyi Li, Min Li & Lukasz Kurgan. (2019) Sequence-Derived Markers of Drug Targets and Potentially Druggable Human Proteins. Frontiers in Genetics 10.
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Constantinos G. Neochoritis, Jack Atmaj, Aleksandra Twarda-Clapa, Ewa Surmiak, Lukasz Skalniak, Lisa-Maria Köhler, Damian Muszak, Katarzyna Kurpiewska, Justyna Kalinowska-Tłuścik, Barbara Beck, Tad A. Holak & Alexander Dömling. (2019) Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction. European Journal of Medicinal Chemistry 182, pages 111588.
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Tapojyoti Das & David Eliezer. (2019) Membrane interactions of intrinsically disordered proteins: The example of alpha-synuclein. Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics 1867:10, pages 879-889.
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Gregg Siegal & Philipp Selenko. (2019) Cells, drugs and NMR. Journal of Magnetic Resonance 306, pages 202-212.
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Marco Schiavina, Maria Grazia Murrali, Letizia Pontoriero, Valerio Sainati, Rainer Kümmerle, Wolfgang Bermel, Roberta Pierattelli & Isabella C. Felli. (2019) Taking Simultaneous Snapshots of Intrinsically Disordered Proteins in Action. Biophysical Journal 117:1, pages 46-55.
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Judit Oláh & Judit Ovádi. (2019) Pharmacological targeting of α‐synuclein and TPPP /p25 in Parkinson's disease: challenges and opportunities in a Nutshell . FEBS Letters 593:13, pages 1641-1653.
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Hye Min Lee, Soon Bin Kwon, Ahyun Son, Doo Hyun Kim, Kyun-Hwan Kim, Jonghyo Lim, Young-Guen Kwon, Jin Sun Kang, Byung Kyu Lee, Young Ho Byun & Baik L. Seong. (2019) Stabilization of Intrinsically Disordered DKK2 Protein by Fusion to RNA-Binding Domain. International Journal of Molecular Sciences 20:11, pages 2847.
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Anne Martinelli, Fernanda Lopes, Elisa John, Célia Carlini & Rodrigo Ligabue-Braun. (2019) Modulation of Disordered Proteins with a Focus on Neurodegenerative Diseases and Other Pathologies. International Journal of Molecular Sciences 20:6, pages 1322.
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Hao Ruan, Qi Sun, Weilin Zhang, Ying Liu & Luhua Lai. (2019) Targeting intrinsically disordered proteins at the edge of chaos. Drug Discovery Today 24:1, pages 217-227.
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Gustavo Fuertes, Laura Nevola & Santiago Esteban-Martín. 2019. Intrinsically Disordered Proteins. Intrinsically Disordered Proteins 275 327 .
Lavinia Carabet, Paul Rennie & Artem Cherkasov. (2018) Therapeutic Inhibition of Myc in Cancer. Structural Bases and Computer-Aided Drug Discovery Approaches. International Journal of Molecular Sciences 20:1, pages 120.
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David W. Baggett & Abhinav Nath. (2018) The Rational Discovery of a Tau Aggregation Inhibitor. Biochemistry 57:42, pages 6099-6107.
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Tracy L. Nero, Michael W. Parker & Craig J. Morton. (2018) Protein structure and computational drug discovery. Biochemical Society Transactions 46:5, pages 1367-1379.
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Yansong Miao, Teepiyanut Tipakornsaowapak, Liangzhen Zheng, Yuguang Mu & Eric Lewellyn. (2018) Phospho‐regulation of intrinsically disordered proteins for actin assembly and endocytosis. The FEBS Journal 285:15, pages 2762-2784.
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Murali Aarthy, Deepak Kumar, Rajanish Giri & Sanjeev Kumar Singh. (2018) E7 oncoprotein of human papillomavirus: Structural dynamics and inhibitor screening study. Gene 658, pages 159-177.
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Maria Grazia Murrali, Marco Schiavina, Valerio Sainati, Wolfgang Bermel, Roberta Pierattelli & Isabella C. Felli. (2018) 13C APSY-NMR for sequential assignment of intrinsically disordered proteins. Journal of Biomolecular NMR 70:3, pages 167-175.
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Farid Rahimi. (2018) Aptamers Selected for Recognizing Amyloid β-Protein—A Case for Cautious Optimism. International Journal of Molecular Sciences 19:3, pages 668.
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Toshihiko Sugiki, Kyoko Furuita, Toshimichi Fujiwara & Chojiro Kojima. (2018) Current NMR Techniques for Structure-Based Drug Discovery. Molecules 23:1, pages 148.
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Hao-Bo Guo, Yue Ma, Gerald A. Tuskan, Xiaohan Yang & Hong Guo. (2018) Classification of Complete Proteomes of Different Organisms and Protein Sets Based on Their Protein Distributions in Terms of Some Key Attributes of Proteins. International Journal of Genomics 2018, pages 1-12.
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Sławomir Wójcik, Melissa Birol, Elizabeth Rhoades, Andrew D. Miranker & Zachary A. Levine. 2018. Intrinsically Disordered Proteins. Intrinsically Disordered Proteins 703 734 .
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Rajanish Giri, Deepak Kumar, Nitin Sharma & Vladimir N. Uversky. (2016) Intrinsically Disordered Side of the Zika Virus Proteome. Frontiers in Cellular and Infection Microbiology 6.
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