Discovery of RMC-5552, a Selective Bi-Steric Inhibitor of mTORC1, for the Treatment of mTORC1-Activated Tumors

The bi-steric mTORC1-selective inhibitor RMC-5552 in tumors with activation of mTOR signaling: Preclinical activity in combination with RAS(ON) inhibitors in RAS-addicted tumors, and initial clinical findings from a single agent phase 1/1b study.

(2022) Howard A. Burris III et al.   JOURNAL OF CLINICAL ONCOLOGY

Sotorasib: First Approval

(2021) Hannah A. Blair   DRUGS

Selective inhibitors of mTORC1 activate 4EBP1 and suppress tumor growth

(2021) Bianca J. Lee et al.   Nature Chemical Biology

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

(2021) Bianca J. Lee et al.   Frontiers in Oncology

Research progress of mTOR inhibitors

(2020) Yifan Chen et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Derivation of Rapamycin: Adventures in Natural Product Chemistry

(2019) Sylvain Cottens et al.   CHIMIA

Molecular basis for class side effects associated with PI3K/AKT/mTOR pathway inhibitors

(2019) Ying Zhang et al.   Expert Opinion on Drug Metabolism & Toxicology

The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients

(2019) Jill Hallin et al.   Cancer Discovery

STK11/LKB1 Mutations and PD-1 Inhibitor Resistance in KRAS -Mutant Lung Adenocarcinoma

(2018) Ferdinandos Skoulidis et al.   Cancer Discovery

mTOR Cross-Talk in Cancer and Potential for Combination Therapy

(2018) Fabiana Conciatori et al.   Cancers

KRAS G12C NSCLC Models Are Sensitive to Direct Targeting of KRAS in Combination with PI3K Inhibition

(2018) Sandra Misale et al.   CLINICAL CANCER RESEARCH

Mechanisms of mTORC1 activation by RHEB and inhibition by PRAS40

(2017) Haijuan Yang et al.   NATURE

Overcoming mTOR resistance mutations with a new-generation mTOR inhibitor

(2016) Vanessa S. Rodrik-Outmezguine et al.   NATURE

Eukaryotic initiation factor 4E-binding protein 1 (4E-BP1): a master regulator of mRNA translation involved in tumorigenesis

(2016) J Musa et al.   ONCOGENE

mTOR kinase structure, mechanism and regulation

(2013) Haijuan Yang et al.   NATURE

Inhibition of PI3K/mTOR Leads to Adaptive Resistance in Matrix-Attached Cancer Cells

(2012) Taru Muranen et al.   CANCER CELL

Abstract B148: INK128 is a potent and selective TORC1/2 inhibitor with broad oral antitumor activity

(2012) K. Jessen et al.   MOLECULAR CANCER THERAPEUTICS

Reducing safety-related drug attrition: the use of in vitro pharmacological profiling

(2012) Joanne Bowes et al.   NATURE REVIEWS DRUG DISCOVERY

AKT Inhibition Relieves Feedback Suppression of Receptor Tyrosine Kinase Expression and Activity

(2011) Sarat Chandarlapaty et al.   CANCER CELL

PI3K inhibition results in enhanced HER signaling and acquired ERK dependency in HER2-overexpressing breast cancer

(2011) V Serra et al.   ONCOGENE

mTOR Kinase Inhibition Causes Feedback-Dependent Biphasic Regulation of AKT Signaling

(2011) V. S. Rodrik-Outmezguine et al.   Cancer Discovery

Rapamycin differentially inhibits S6Ks and 4E-BP1 to mediate cell-type-specific repression of mRNA translation

(2008) A. Y. Choo et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA