Induced protein degradation: an emerging drug discovery paradigm

AC Lai, CM Crews - Nature reviews Drug discovery, 2017 - nature.com
Small-molecule drug discovery has traditionally focused on occupancy of a binding site that
directly affects protein function, and this approach typically precludes targeting proteins that …

The PROTAC technology in drug development

Y Zou, D Ma, Y Wang - Cell biochemistry and function, 2019 - Wiley Online Library
Currently, a new technology termed PROTAC, proteolysis targeting chimera, has been
developed for inducing the protein degradation by a targeting molecule. This technology …

Rational approaches, design strategies, structure activity relationship and mechanistic insights for anticancer hybrids

K Nepali, S Sharma, M Sharma, PMS Bedi… - European journal of …, 2014 - Elsevier
A Hybrid drug which comprises the incorporation of two drug pharmacophores in one single
molecule are basically designed to interact with multiple targets or to amplify its effect …

Allylic C–H amination cross-coupling furnishes tertiary amines by electrophilic metal catalysis

SZ Ali, BG Budaitis, DFA Fontaine, AL Pace, JA Garwin… - Science, 2022 - science.org
Intermolecular cross-coupling of terminal olefins with secondary amines to form complex
tertiary amines—a common motif in pharmaceuticals—remains a major challenge in …

Chemical genetic control of protein levels: selective in vivo targeted degradation

JS Schneekloth Jr, FN Fonseca… - Journal of the …, 2004 - ACS Publications
Genetic loss of function analysis is a powerful method for the study of protein function.
However, some cell biological questions are difficult to address using traditional genetic …

[图书][B] Anticancer agents from natural products

GM Cragg, DGI Kingston, DJ Newman - 2005 - taylorfrancis.com
Plants, marine organisms, and microorganisms have evolved complex chemical defense
and signaling systems that are designed to protect them from predators and provide other …

Advances in receptor‐mediated, tumor‐targeted drug delivery

DE Large, JR Soucy, J Hebert… - Advanced …, 2019 - Wiley Online Library
Receptor‐mediated drug delivery presents an opportunity to enhance therapeutic efficiency
by accumulating drug within the tissue of interest and reducing undesired, off‐target effects …

Natural product hybrids as new leads for drug discovery

LF Tietze, HP Bell… - Angewandte Chemie …, 2003 - Wiley Online Library
Natural products play an important role in the development of drugs, especially for the
treatment of infections and cancer, as well as immunosuppressive compounds. However …

Estrogen signaling: An emanating therapeutic target for breast cancer treatment

T Saha, S Makar, R Swetha, G Gutti… - European journal of …, 2019 - Elsevier
Breast cancer, a most common malignancy in women, was known to be associated with
steroid hormone estrogen. The discovery of estrogen receptor (ER) gave us not only a …

Heat shock proteins in the regulation of apoptosis: new strategies in tumor therapy: a comprehensive review

AS Sreedhar, P Csermely - Pharmacology & therapeutics, 2004 - Elsevier
Heat shock proteins (Hsp) form the most ancient defense system in all living organisms on
earth. These proteins act as molecular chaperones by helping in the refolding of misfolded …