RapaLink-1

rapamycin and an mTOR kinase inhibitor are covalently linked

Also Known As:

40-O-(2-((1-(32-(4-amino-3-(2-aminobenzo(d)oxazol-5-yl)-1H-pyrazolo(3,4-d)pyrimidin-1-yl)-27-oxo-3,6,9,12,15,18,21,24-octaoxa-28-azadotriacontyl)-1H-1,2,3-triazol-4-yl)methoxy)ethyl)-rapamycin

Networked: 12 relevant articles (3 outcomes, 2 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Organic Chemicals: 133
- Lactones: 1549
  - Macrolides: 4391
    - Sirolimus: 9779
      - RapaLink-1: 12

Experts

1.	Jacinto, Estela: 3 articles (01/2021 - 01/2020)
2.	Patel, Nikhil: 3 articles (01/2021 - 01/2020)
3.	Beimers, Lijkele: 2 articles (01/2021 - 01/2020)
4.	De Filippo, Maria Rosaria: 2 articles (01/2021 - 01/2020)
5.	De Menna, Marta: 2 articles (01/2021 - 01/2020)
6.	Karkampouna, Sofia: 2 articles (01/2021 - 01/2020)
7.	Klima, Irena: 2 articles (01/2021 - 01/2020)
8.	Kloen, Peter: 2 articles (01/2021 - 01/2020)
9.	Kruithof-de Julio, Marianna: 2 articles (01/2021 - 01/2020)
10.	La Manna, Federico: 2 articles (01/2021 - 01/2020)

Related Diseases

1.	Renal Cell Carcinoma (Grawitz Tumor) 05/01/2020 - "The aim of the present study was to evaluate the in vitro and in vivo therapeutic efficacy of Rapalink-1 against renal cell carcinoma (RCC) compared to temsirolimus, which is commonly used as a small molecule inhibitor of mTOR and is a derivative of rapamycin. " 05/01/2020 - "Potential new therapy of Rapalink-1, a new generation mammalian target of rapamycin inhibitor, against sunitinib-resistant renal cell carcinoma."
2.	Neoplasms (Cancer) 01/01/2020 - "Mice treated with Rapalink-1 showed a significantly delayed tumor growth compared to control and cells recovered from the tumors of treated animals showed a marked decrease of CD44 expression. " 01/01/2021 - "Corrigendum: Dual-mTOR Inhibitor Rapalink-1 Reduces Prostate Cancer Patient-Derived Xenograft Growth and Alters Tumor Heterogeneity." 01/01/2020 - "Dual-mTOR Inhibitor Rapalink-1 Reduces Prostate Cancer Patient-Derived Xenograft Growth and Alters Tumor Heterogeneity." 01/01/2017 - "RapaLink-1 showed better efficacy than rapamycin or TORKi, potently blocking cancer-derived, activating mutants of mTOR. " 12/21/2020 - "Rapalink-1 Targets Glioblastoma Stem Cells and Acts Synergistically with Tumor Treating Fields to Reduce Resistance against Temozolomide."
3.	Glioblastoma (Glioblastoma Multiforme) 01/01/2018 - "We also review mechanistic data by which RapaLink-1 blocks p-4EBP1 and discuss future clinical strategies for 4EBP1 inhibition in glioblastoma. " 12/21/2020 - "Rapalink-1 Targets Glioblastoma Stem Cells and Acts Synergistically with Tumor Treating Fields to Reduce Resistance against Temozolomide." 01/01/2022 - "We show that this drug combination mitigates the systemic effects of mTOR inhibitors but retains the efficacy of RapaLink-1 in glioblastoma xenografts. "
4.	Brain Ischemia (Cerebral Ischemia) 01/01/2021 - "In this study, we investigated how Rapalink-1, a third-generation mTOR inhibitor, would affect neuronal survival and BBB disruption in the very early stage of cerebral ischemia-reperfusion that is within the time window of thrombolysis therapy. " 01/01/2021 - "Commentary: Rapalink-1 Increased Infarct Size in Early Cerebral Ischemia-Reperfusion With Increased Blood-Brain Barrier Disruption." 01/01/2021 - "Rapalink-1 Increased Infarct Size in Early Cerebral Ischemia-Reperfusion With Increased Blood-Brain Barrier Disruption." 01/01/2021 - "Taken together, our data suggest that inhibiting both mTORC1 and mTORC2 by Rapalink-1 could worsen the neuronal damage in the early stage of cerebral ischemia-reperfusion and that the aggravation of BBB disruption could be one of the contributing factors."
5.	Prostatic Neoplasms (Prostate Cancer) 01/01/2021 - "Corrigendum: Dual-mTOR Inhibitor Rapalink-1 Reduces Prostate Cancer Patient-Derived Xenograft Growth and Alters Tumor Heterogeneity." 01/01/2020 - "Dual-mTOR Inhibitor Rapalink-1 Reduces Prostate Cancer Patient-Derived Xenograft Growth and Alters Tumor Heterogeneity."

Related Drugs and Biologics

1.	Sirolimus (Rapamycin)
2.	temsirolimus
3.	Drug Combinations
4.	MTOR Inhibitors
5.	TOR Serine-Threonine Kinases
6.	Therapeutic Uses
7.	Phosphotransferases (Kinase)
8.	Hydroxychloroquine (Plaquenil)
9.	Antibodies
10.	Sunitinib (Sutent)

Related Therapies and Procedures

1.	Therapeutics