PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

M He, C Cao, Z Ni, Y Liu, P Song, S Hao, Y He… - … and Targeted Therapy, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …

Achieving clinical success with BET inhibitors as anti-cancer agents

T Shorstova, WD Foulkes, M Witcher - British journal of cancer, 2021 - nature.com
The transcriptional upregulation of oncogenes is a driving force behind the progression of
many tumours. However, until a decade ago, the concept of 'switching off'these oncogenic …

Mammalian SWI/SNF chromatin remodeling complexes: emerging mechanisms and therapeutic strategies

RC Centore, GJ Sandoval, LMM Soares, C Kadoch… - Trends in Genetics, 2020 - cell.com
Small molecule-based targeting of chromatin regulatory factors has emerged as a promising
therapeutic strategy in recent years. The development and ongoing clinical evaluation of …

MYC: a multipurpose oncogene with prognostic and therapeutic implications in blood malignancies

SE Ahmadi, S Rahimi, B Zarandi, R Chegeni… - Journal of hematology & …, 2021 - Springer
MYC oncogene is a transcription factor with a wide array of functions affecting cellular
activities such as cell cycle, apoptosis, DNA damage response, and hematopoiesis. Due to …

BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design

W Farnaby, M Koegl, MJ Roy, C Whitworth… - Nature chemical …, 2019 - nature.com
Targeting subunits of BAF/PBAF chromatin remodeling complexes has been proposed as an
approach to exploit cancer vulnerabilities. Here, we develop proteolysis targeting chimera …

Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation

O Gilan, I Rioja, K Knezevic, MJ Bell, MM Yeung… - Science, 2020 - science.org
The two tandem bromodomains of the BET (bromodomain and extraterminal domain)
proteins enable chromatin binding to facilitate transcription. Drugs that inhibit both …

[HTML][HTML] Transcriptional addiction in cancer

JE Bradner, D Hnisz, RA Young - Cell, 2017 - cell.com
Cancer arises from genetic alterations that invariably lead to dysregulated transcriptional
programs. These dysregulated programs can cause cancer cells to become highly …

MYC, metabolism, and cancer

ZE Stine, ZE Walton, BJ Altman, AL Hsieh, CV Dang - Cancer discovery, 2015 - AACR
The MYC oncogene encodes a transcription factor, MYC, whose broad effects make its
precise oncogenic role enigmatically elusive. The evidence to date suggests that MYC …

Genomic spectra of biliary tract cancer

H Nakamura, Y Arai, Y Totoki, T Shirota, A Elzawahry… - Nature …, 2015 - nature.com
The incidence of biliary tract cancer (BTC), including intrahepatic (ICC) and extrahepatic
(ECC) cholangiocarcinoma and gallbladder cancer, has increased globally; however, no …

Systematic mapping of functional enhancer–promoter connections with CRISPR interference

CP Fulco, M Munschauer, R Anyoha, G Munson… - Science, 2016 - science.org
Gene expression in mammals is regulated by noncoding elements that can affect physiology
and disease, yet the functions and target genes of most noncoding elements remain …