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An ATP-competitive Mammalian Target of Rapamycin Inhibitor Reveals Rapamycin-resistant Functions of mTORC1

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The translational landscape of mTOR signalling steers cancer initiation and metastasis

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Active-Site Inhibitors of mTOR Target Rapamycin-Resistant Outputs of mTORC1 and mTORC2

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mTORC1-Mediated Cell Proliferation, But Not Cell Growth, Controlled by the 4E-BPs

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Genome Sequencing Identifies a Basis for Everolimus Sensitivity

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RAPIDASH: Tag-free enrichment of ribosome-associated proteins reveals composition dynamics in embryonic tissue, cancer cells, and macrophages

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A Bifunctional MAPK/PI3K Antagonist for Inhibition of Tumor Growth and Metastasis

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The Molecular and Clinical Landscape of Pancreatic Neuroendocrine Tumors

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Non-Thermal Plasma Induces Antileukemic Effect Through mTOR Ubiquitination

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The prospect of substrate-based kinase inhibitors to improve target selectivity and overcome drug resistance

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Disentangling the signaling pathways of mTOR complexes, mTORC1 and mTORC2, as a therapeutic target in glioblastoma

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MNK, mTOR or eIF4E-selecting the best anti-tumor target for blocking translation initiation

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Simultaneous targeting of AMPK and mTOR is a novel therapeutic strategy against prostate cancer

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mTOR Inhibition via Displacement of Phosphatidic Acid Induces Enhanced Cytotoxicity Specifically in Cancer Cells

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Rapamycin and trametinib: a rational combination for treatment of NSCLC

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Mapping of mTOR drug targets: Featured platforms for anti-cancer drug discovery

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Unveiling the Role of Mechanistic Target of Rapamycin Kinase (MTOR) Signaling in Cancer Progression and the Emergence of MTOR Inhibitors as Therapeutic Strategies

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G0S2 represses PI3K/mTOR signaling and increases sensitivity to PI3K/mTOR pathway inhibitors in breast cancer

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Genetic pathogenesis of the epileptogenic lesions in Tuberous Sclerosis Complex: Therapeutic targeting of the mTOR pathway

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Brain-specific inhibition of mTORC1 eliminates side effects resulting from mTORC1 blockade in the periphery and reduces alcohol intake in mice

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A bi-steric mTORC1-selective inhibitor overcomes drug resistance in breast cancer

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Pharmacophore-guided fragment-based design of novel mammalian target of rapamycin inhibitors: extra precision docking, fingerprint-based 2D and atom-based 3D-QSAR modelling

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Inhibition of mTOR Pathway by Rapamycin Decreases P-glycoprotein Expression and Spontaneous Seizures in Pharmacoresistant Epilepsy

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Tackling endocrine resistance in ER-positive HER2-negative advanced breast cancer: A tale of imprecision medicine

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Targeting mTOR in the Context of Diet and Whole-body Metabolism

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Defining the role of mTOR pathway in the regulation of stem cells of glioblastoma

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A new generation of mTORC1 inhibitor attenuates alcohol intake and reward in mice

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Molecular Interplay between Dormant Bone Marrow-Resident Cells (BMRCs) and CTCs in Breast Cancer

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Dodging the bullet: therapeutic resistance mechanisms in pediatric cancers

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RPTOR blockade suppresses brain metastases of NSCLC by interfering the ceramide metabolism via hijacking YY1 binding

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Orthosteric and Allosteric Dual Targeting of the Nuclear Receptor RORγt with a Bitopic Ligand

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Combining Oncolytic Viruses and Small Molecule Therapeutics: Mutual Benefits

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Rapalink-1 Increased Infarct Size in Early Cerebral Ischemia–Reperfusion With Increased Blood–Brain Barrier Disruption

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Efficacy of a Novel Bi-Steric mTORC1 Inhibitor in Models of B-Cell Acute Lymphoblastic Leukemia

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mTOR‐dependent immunometabolism as Achilles' heel of anticancer therapy

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Mechanisms of acquired resistance to rapalogs in metastatic renal cell carcinoma

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Ribosome Biogenesis and Function in Cancer: From Mechanisms to Therapy

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mTOR as an eligible molecular target for possible pharmacological treatment of nonalcoholic steatohepatitis

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Challenges and Emerging Opportunities for Targeting mTOR in Cancer

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Bivalent mTOR inhibitors — the next generation

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Exploring Molecular Descriptors and Fingerprints to Predict mTOR Kinase Inhibitors using Machine Learning Techniques

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Targeting mTOR Kinase for Cancer Treatment: A Comprehensive Review With Clinical Insights

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Rheb1-Independent Activation of mTORC1 in Mammary Tumors Occurs through Activating Mutations in mTOR

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A cell-based chemical-genetic screen for amino acid stress response inhibitors reveals torins reverse stress kinase GCN2 signaling

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eIF4A1 enhances LARP1-mediated translational repression during mTORC1 inhibition

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Strategies to Overcome Resistance Mutations of Bruton's Tyrosine Kinase Inhibitor Ibrutinib

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Rapalog resistance is associated with mesenchymal-type changes in Tsc2-null cells

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Anti‑proliferative effect of cardamonin on mTOR inhibitor‑resistant cancer cells

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Targeted therapy for mTORC1-driven tumours through HDAC inhibition by exploiting innate vulnerability of mTORC1 hyper-activation

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A renaissance in targeting the PI3K/AKT/mTOR pathway

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Translatome analysis of tuberous sclerosis complex 1 patient-derived neural progenitor cells reveals rapamycin-dependent and independent alterations

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Bi-steric mTORC1 inhibitors induce apoptotic cell death in tumor models with hyperactivated mTORC1

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RapaLink-1 plays an antithrombotic role in antiphospholipid syndrome by improving autophagy both in vivo and vitro

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A patent review of mTOR inhibitors for cancer therapy (2011–2020)

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Advances in autophagy as a target in the treatment of tumours

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Macrophages play a role in inflammatory transformation of colorectal cancer

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Oncogenic kinases and perturbations in protein synthesis machinery and energetics in neoplasia

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CNS Anticancer Drug Discovery and Development: 2016 conference insights

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eIF4F-mediated dysregulation of mRNA translation in cancer

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PTEN loss confers sensitivity to rapalogs in clear cell renal cell carcinoma

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Designing drugs and chemical probes with the dualsteric approach

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Unconventional mechanism of action and resistance to rapalogs in renal cancer

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Structure‐Guided Drug Design Targeting Abl Kinase: How Structure and Regulation Can Assist in Designing New Drugs

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mTOR Signaling: Roles in Hepatitis B Virus Infection and Hepatocellular Carcinoma

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eIF4A controls translation of estrogen receptor alpha and is a therapeutic target in advanced breast cancer

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Autophagy as a pharmacological target in hematopoiesis and hematological disorders

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Leveraging conformational ensembles in allosteric drug discovery

Nussinov, R., Regev, C., & Jang, H. (2026) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2026.01.006 · Cited by 14

mTOR hypoactivity leads to trophectoderm cell failure by enhancing lysosomal activation and disrupting the cytoskeleton in preimplantation embryo

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Negative regulation of amino acid signaling by MAPK-regulated 4F2hc/Girdin complex

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Gemcitabine and Selected mTOR Inhibitors in Uterine Sarcomas and Carcinosarcoma Cells- an Isobolographic Analysis

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The Bumpy Road towards mTOR Inhibition in Glioblastoma: Quo Vadis?

Papavassiliou, K. A., & Papavassiliou, A. G. (2021) · Biomedicines · doi:10.3390/biomedicines9121809 · Cited by 13

Targeting autophagy drug discovery: Targets, indications and development trends

Jiang, M., Wu, W., Xiong, Z., Ye, Z., Ye, Z., & Wu, Z. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.116117 · Cited by 13

Rational design of multi-targeting ruthenium- and platinum-based anticancer complexes

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Structure-Guided Design and Initial Studies of a Bifunctional MEK/PI3K Inhibitor (ST-168)

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mTOR Kinase Inhibition Effectively Decreases Progression of a Subset of Neuroendocrine Tumors that Progress on Rapalog Therapy and Delays Cardiac Impairment

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Mechanistic target of rapamycin (MTOR) protein expression in the tumor and its microenvironment correlates with more aggressive pathology at cystectomy

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Emerging Therapies for Breast CancerPreprint

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The Precision-Guided Use of PI3K Pathway Inhibitors for the Treatment of Solid Malignancies

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Playing the Devil’s Advocate: Should We Give a Second Chance to mTOR Inhibition in Renal Clear Cell Carcinoma? – ie Strategies to Revert Resistance to mTOR Inhibitors

Pezzicoli, G., Filoni, E., Gernone, A., Cosmai, L., Rizzo, M., & Porta, C. (2021) · Cancer Management and Research · doi:10.2147/cmar.s267220 · Cited by 12

DNA-modularized construction of bivalent ligands precisely regulates receptor binding and activation

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eIF4A1 Is a Prognostic Marker and Actionable Target in Human Hepatocellular Carcinoma

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Anticancer Hybrids

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Resistance is futile with fourth-generation EGFR inhibitors

Marasco, M., & Misale, S. (2022) · Nature Cancer · doi:10.1038/s43018-022-00365-2 · Cited by 12

Delay of human early development via in vitro diapausePreprint

Iyer, D. P., van der Weijden, V. A., Khoei, H. H., McCarthy, A., Rayón, T., Simon, C. S., Dunkel, I., Wamaitha, S. E., Elder, K. T., Snell, P., et al. (2023) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2023.05.29.541316 · Cited by 14

The Bi-steric, mTORC1-Selective Inhibitor, RMC-5552, in Advanced Solid Tumors: A Phase 1 Trial

Schram, A. M., Naqash, A. R., Haura, E. B., Riess, J. W., Ulahannan, S. V., Ou, S. I., Münster, P. N., Cheng, M. L., Gustafson, W. C., Bitman, B., et al. (2025) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-25-2112 · Cited by 11

mTOR pathway diseases: challenges and opportunities from bench to bedside and the mTOR node

Ritter, L. M., Annear, N. M. P., Baple, E. L., Ben-Chaabane, L. Y., Bódi, I., Brosson, L., Cadwgan, J., Coslett, B., Crosby, A. H., Davies, D. M., et al. (2025) · Orphanet Journal of Rare Diseases · doi:10.1186/s13023-025-03740-1 · Cited by 12

Deficiency in the Treatment Description of mTOR Inhibitor Resistance in Medulloblastoma, a Systematic Review

Alammar, H., Nassani, R., Alshehri, M. M., Aljohani, A. A., & Alrfaei, B. M. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms23010464 · Cited by 11

Node-based differential network analysis in genomics

Zhang, X.-F., Ou-Yang, L., & Yan, H. (2017) · Computational Biology and Chemistry · doi:10.1016/j.compbiolchem.2017.03.010 · Cited by 11

Novel therapeutic approaches in GEP-NETs based on genetic and epigenetic alterations

Pozas, J., Alonso‐Gordoa, T., Román, M. S., Santoni, M., Thirlwell, C., Grande, E., & Molina‐Cerrillo, J. (2022) · Biochimica et Biophysica Acta (BBA) - Reviews on Cancer · doi:10.1016/j.bbcan.2022.188804 · Cited by 12

In vitro delivery of mTOR inhibitors by kidney-targeted micelles for autosomal dominant polycystic kidney disease

Cox, A., Tung, M., Li, H., Hallows, K. R., & Chung, E. J. (2023) · SLAS TECHNOLOGY · doi:10.1016/j.slast.2023.02.001 · Cited by 12

Mitochondrial metabolic rewiring sensitizes mTORC1 inhibitor persister cells to cuproptosis

Du, H., Liu, H.-J., Łośko, M., Yang, Y. C., Yuan, M., Henske, E. P., Asara, J. M., Singh, M., & Kwiatkowski, D. J. (2025) · JCI Insight · doi:10.1172/jci.insight.187448 · Cited by 10

Discovery of novel hybrids of mTOR inhibitor and NO donor as potential anti-tumor therapeutics

Gao, X., Zhao, F., Wang, Y., Ma, X., Chai, H., Han, J., & Fang, F. (2023) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2023.117402 · Cited by 10

Lost in translation: a neglected mTOR target for lymphangioleiomyomatosis

Evans, J. F., McCormack, F. X., Sonenberg, N., & Krymskaya, V. P. (2023) · European Respiratory Review · doi:10.1183/16000617.0100-2023 · Cited by 10

The Bi-steric Inhibitor RMC-5552 Reduces mTORC1 Signaling and Growth in Lymphangioleiomyomatosis

Evans, J. F., Ledwell, O. A., Tang, Y., Rue, R. W., Mukhitov, A. R., Diesler, R., Lin, S. M., Vanka, K. S., Basil, M. C., Cantu, E., et al. (2024) · American Journal of Respiratory Cell and Molecular Biology · doi:10.1165/rcmb.2024-0242oc · Cited by 10

mTORC1 Selective Nano‐Inhibitor by Disrupting the Lysosomal Arginine‐SLC38A9‐ mTORC1‐CDKs Axis for Precision Bladder Cancer Therapy

Kong, L., Xu, K., Bao, X., Ye, K., Fan, D., Wang, N., Deng, Y., Wang, W., Wei, S., & Zhou, L. (2025) · Advanced Materials · doi:10.1002/adma.202504798 · Cited by 11

High-depth sequencing of paired primary and metastatic tumours: Implications for personalised medicine

Grellety, T., Lucchesi, C., Hostein, I., Auzanneau, C., Khalifa, E., Soubeyran, I., & Italiano, A. (2017) · European Journal of Cancer · doi:10.1016/j.ejca.2017.07.019 · Cited by 10

HybridMolDB: A Manually Curated Database Dedicated to Hybrid Molecules for Chemical Biology and Drug Discovery

Li, Y., Zhao, C., Zhang, J., Zhai, S., Wei, B., & Wang, L. (2019) · Journal of Chemical Information and Modeling · doi:10.1021/acs.jcim.9b00314 · Cited by 10

dbMCS: A Database for Exploring the Mutation Markers of Anti-Cancer Drug Sensitivity

Shen, Y., Zhang, Y., Xue, W., & Yue, Z. (2021) · IEEE Journal of Biomedical and Health Informatics · doi:10.1109/jbhi.2021.3100424 · Cited by 10

In Silico Discovery of a Small Molecule Suppressing Lung Carcinoma A549 Cells Proliferation and Inducing Autophagy via mTOR Pathway Inhibition

Liu, J., Liu, L., Tian, Z., Li, Y., Shi, C., Shi, J., Wei, S., Zhao, Y., Zhang, W., Bai, B., et al. (2018) · Molecular Pharmaceutics · doi:10.1021/acs.molpharmaceut.8b00996 · Cited by 9

Targeting the PI3K/AKT/mTOR Signaling Pathway in Primary Central Nervous System Lymphoma: Current Status and Future Prospects

Zhang, X., & Liu, Y. (2020) · CNS & Neurological Disorders - Drug Targets · doi:10.2174/1871527319666200517112252 · Cited by 10

mTOR activation induces endolysosomal remodeling and nonclassical secretion of IL-32 via exosomes in inflammatory reactive astrocytesPreprint

Leng, K., Rooney, B., McCarthy, F., Xia, W., Rose, I. V. L., Bax, S., Chin, M. Y., Fathi, S., Herrington, K. A., Leonetti, M. D., et al. (2021) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2021.09.11.459904 · Cited by 10

MAPK and mTORC1 signaling converge to drive cyclin D1 protein production to enable cell cycle reentry in melanoma persister cells

Nangia, V., Ashraf, H. M., Marikar, N. C., Passanisi, V. J., Christopher, R., & Spencer, S. L. (2025) · Science Signaling · doi:10.1126/scisignal.adw3231 · Cited by 11

TOR Inhibitors Synergistically Suppress the Growth and Development of Phytophthora infestans, a Highly Destructive Pathogenic Oomycete

Zhang, S., Khalid, A. R., Guo, D., Zhang, J., Xiong, F., & Ren, M. (2021) · Frontiers in Microbiology · doi:10.3389/fmicb.2021.596874 · Cited by 9

Genomic and Transcriptome Analysis to Identify the Role of the mTOR Pathway in Kidney Renal Clear Cell Carcinoma and Its Potential Therapeutic Significance

Che, X., Qi, X., Xu, Y., Wang, Q., & Wu, G. (2021) · Oxidative Medicine and Cellular Longevity · doi:10.1155/2021/6613151 · Cited by 9

Design, Synthesis, and Biological Evaluation of mTOR-Targeting PROTACs Based on MLN0128 and Pomalidomide

Zhang, Q., Yan, P., Zhao, P., Zhao, D., Cao, H., Lü, J., & Mao, B. (2022) · Chemical and Pharmaceutical Bulletin · doi:10.1248/cpb.c22-00576 · Cited by 9

Abstract IA25: Third-generation inhibitors of mTOR

Shokat, K. M. (2017) · Cancer Research · doi:10.1158/1538-7445.transcontrol16-ia25

Abstract 2147: Overcoming mTOR resistance mutations with a new generation mTOR inhibitor

Rodrik-Outmezguine, V. S., Okaniwa, M., Yao, Z., Novotny, C. J., McWhirter, C. L., Banaji, A., Won, H. H., Wong, W. P. E., Berger, M., de Stanchina, E., et al. (2016) · Cancer Research · doi:10.1158/1538-7445.am2016-2147 · Cited by 1

Abstract 1726: Acquired resistance to rapamycin and mTOR kinase inhibitors is mediated by non-overlapping mutations in distinct sites in the mTOR protein

Rodrik-Outmezguine, V. S., Yao, Z., Mukherjee, R., Cai, L., Barratt, D. G., Ward, R., Klinowska, T. C. M., de Stanchina, E., Berger, M., Baselga, J. M., et al. (2014) · Cancer Research · doi:10.1158/1538-7445.am2014-1726 · Cited by 1

Abstract PR04: mTOR mutations in cancer

Grabiner, B. C., Wagle, N., Allen, E. M. V., Garraway, L. A., Lorch, J. H., & Sabatini, D. M. (2015) · Molecular Cancer Therapeutics · doi:10.1158/1538-8514.pi3k14-pr04

Abstract PD1-8: Acquired resistance to rapamycin and mTOR kinase inhibitors is mediated by non-overlapping mutations in distinct sites in the mTOR protein

Rodrik-Outmezguine, V., Yao, Z., Berger, M., de Stanchina, E., Klinowska, T. C. M., Barratt, D., Baselga, J. M., & Rosen, N. (2013) · Cancer Research · doi:10.1158/0008-5472.sabcs13-pd1-8