Results 181 to 190 of about 5,785,146 (400)

Technological Discontinuities and the Comparative Strategic Value of New Capabilites: Evidence from the Comparison of Small- and Large-Molecule Targeted Anti-Cancer Drug Discovery [PDF]

Traditional creative destruction theories distinguish disruptions as competence-destroying or competence-enhancing to incumbents’ capabilities, with the former case resulting in incumbents’ loss of competitive advantage in in-house R&D performance (even ...
M. Lourdes Sosa
core  

Crystal structures of DCAF1-PROTAC-WDR5 ternary complexes provide insight into DCAF1 substrate specificity

Nature Communications
Proteolysis-targeting chimeras (PROTACs) have been explored for the degradation of drug targets for more than two decades. However, only a handful of E3 ligase substrate receptors have been efficiently used. Downregulation and mutation of these receptors
Mark F. Mabanglo, Brian Wilson, Mahmoud Noureldin, Serah W. Kimani, Ahmed Mamai, Chiara Krausser, Héctor González-Álvarez, Smriti Srivastava, Mohammed Mohammed, Laurent Hoffer, Manuel Chan, Jamie Avrumutsoae, Alice Shi Ming Li, Taraneh Hajian, Sarah Tucker, Stuart Green, Magdalena Szewczyk, Dalia Barsyte-Lovejoy, Vijayaratnam Santhakumar, Suzanne Ackloo, Peter Loppnau, Yanjun Li, Almagul Seitova, Taira Kiyota, Jue George Wang, Gilbert G. Privé, Douglas A. Kuntz, Bhashant Patel, Vaibhavi Rathod, Anand Vala, Bhimsen Rout, Ahmed Aman, Gennady Poda, David Uehling, Jailall Ramnauth, Levon Halabelian, Richard Marcellus, Rima Al-awar, Masoud Vedadi   +38 more
doaj   +1 more source

Landscape of BRAF transcript variants in human cancer

Molecular Oncology, EarlyView.
We investigate the annotation of BRAF variants, focusing on protein‐coding BRAF‐220 (formerly BRAF‐reference) and BRAF‐204 (BRAF‐X1). The IsoWorm pipeline allows us to quantify these variants in human cancer, starting from RNA‐sequencing data. BRAF‐204 is more abundant than BRAF‐220 and impacts patient survival.
Maurizio S. Podda, Danilo Tatoni, Gianluca Mattei, Alberto Magi, Romina D'Aurizio, Laura Poliseno   +5 more
wiley   +1 more source

Identification of a phenyl ester covalent inhibitor of caseinolytic protease and analysis of the ClpP1P2 inhibition in mycobacteria

mLife
The caseinolytic protease complex ClpP1P2 is crucial for protein homeostasis in mycobacteria and stress response and virulence of the pathogens. Its role as a potential drug target for combating tuberculosis (TB) has just begun to be substantiated in ...
Genhui Xiao, Yumeng Cui, Liangliang Zhou, Chuya Niu, Bing Wang, Jinglan Wang, Shaoyang Zhou, Miaomiao Pan, Chi Kin Chan, Yan Xia, Lan Xu, Yu Lu, Shawn Chen   +12 more
doaj   +1 more source

Clue to the discovery of novel psychotropic drugs based on the control of excessive neuronal function activating by intracellular Ca2+ modulation.

, 1994
Yasuo Watanabe, Takeshi Shibuya
openalex   +1 more source

Impact of genomics on drug discovery and clinical medicine [PDF]

, 2000
Gérard Emilien, Michel Ponchon, Carlos Caldas, Ole Isacson, J.M. Maloteaux   +4 more
openalex   +1 more source

TRPM8 levels determine tumor vulnerability to channel agonists

Molecular Oncology, EarlyView.
TRPM8 is a Ca2+ permissive channel. Regardless of the amount of its transcript, high levels of TRPM8 protein mark different tumors, including prostate, breast, colorectal, and lung carcinomas. Targeting TRPM8 with channel agonists stimulates inward calcium currents followed by emptying of cytosolic Ca2+ stores in cancer cells.
Alessandro Alaimo, Francesco Giuseppe Carbone, Kristi Buzo, Nicole Annesi, Sacha Genovesi, Annalisa Lorenzato, Karen Widmann, Michela Libergoli, Elisa Marmocchi, Giovanni Bertalot, Alberto Brolese, Mauro Giulio Papotti, Luca Molinaro, Orazio Caffo, Mattia Barbareschi, Alberto Bardelli, Alessandro Romanel, Sabrina Arena, Andrea Lunardi   +18 more
wiley   +1 more source

Inverse agonism at G protein‐coupled receptors: (patho)physiological relevance and implications for drug discovery [PDF]

, 2000
Rianne A.F. de Ligt, Angeliki P. Kourounakis, Adriaan P. IJzerman   +2 more
openalex   +1 more source

The anticancer effect of the HDAC inhibitor belinostat is enhanced by inhibitors of Bcl‐xL or Mcl‐1 in ovarian cancer

Molecular Oncology, EarlyView.
The pan‐HDAC inhibitor belinostat increases the expression of the pro‐apoptotic proteins Bim, Puma, and Noxa and induces apoptosis in ovarian cancer cell lines and patient‐derived tumor organoids when used at high concentrations. Moreover, inhibiting the anti‐apoptotic proteins Bcl‐xL or Mcl‐1 sensitizes these preclinical models to the cytotoxic effect
Cécilia Thomine, Sterenn Guillemot, Louis‐Bastien Weiswald, Romane Florent, Edwige Abeilard, Florence Giffard, Emilie Brotin, Mélanie Briand, Enora Dolivet, Laurent Poulain, Marie Villedieu   +10 more
wiley   +1 more source

Correction to: Pharmacological inhibition of nSMase2 reduces brain exosome release and α-synuclein pathology in a Parkinson’s disease model

Molecular Brain, 2021
Chunni Zhu, Tina Bilousova, Samantha Focht, Michael Jun, Chris Jean Elias, Mikhail Melnik, Sujyoti Chandra, Jesus Campagna, Whitaker Cohn, Asa Hatami, Patricia Spilman, Karen Hoppens Gylys, Varghese John   +12 more
doaj   +1 more source