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Targeting epigenetic enzymes for autism treatment Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-07-20
Emerging preclinical autism research has shown the therapeutic promise of pharmacological inhibitors for epigenetic enzymes, such as histone deacetylases (HDAC), euchromatic histone methyltransferases (EHMT), and lysine-specific histone demethylase 1A (LSD1). These interventions restore gene expression, synaptic function, and behavioral performance in autism models, highlighting a new strategy for
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BTK inhibitors: past, present, and future Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-07-17
Bruton’s tyrosine kinase (BTK) inhibitors have revolutionized the treatment landscape for B cell lymphomas such as chronic lymphocytic leukemia (CLL). The first-in-class BTK inhibitor ibrutinib has recently been succeeded by covalent BTK inhibitors that are safer but still face challenges of resistance mutations. The noncovalent BTK inhibitor pirtobrutinib was recently approved for relapsed and refractory
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Magnesium for disease treatment and prevention: emerging mechanisms and opportunities Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-07-16
Magnesium (Mg2+) is a commonly used dietary supplement for the prevention and treatment of diseases. However, the efficacy and mechanisms of action of Mg2+ in most diseases have been controversial because of conflicting findings in earlier studies. Recent clinical and preclinical studies provide novel insights into the use of Mg2+ for the treatment and prevention of diseases affecting different organ
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Targeting TRPM channels for cerebral ischemia–reperfusion injury Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-07-16
Transient receptor potential melastatin (TRPM) channels have emerged as potential therapeutic targets for cerebral ischemia–reperfusion (I/R) injury. We highlight recent findings on the involvement of TRPM channels in oxidative stress, mitochondrial dysfunction, inflammation, and calcium overload. We also discuss the challenges and future directions in targeting TRPM channels for cerebral I/R injury
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Innovating cancer drug discovery with refined phenotypic screens Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-07-15
Before molecular pathways in cancer were known to a depth that could predict targets, drug development relied on phenotypic screening, where the effectiveness of candidate chemicals is judged from functional readouts without considering the mechanisms of action. The unraveling of tumor-specific pathways has brought targets for molecularly driven drug discovery, but precedents in the field have shown
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PANoptosis: a novel target for cardiovascular diseases Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-07-12 Qi Xiang, Zhen-Xi Geng, Xin Yi, Xiang Wei, Xue-Hai Zhu, Ding-Sheng Jiang
PANoptosis is a unique innate immune inflammatory lytic cell death pathway initiated by an innate immune sensor and driven by caspases and RIPKs. As a distinct pathway, the execution of PANoptosis cannot be hindered by targeting other cell death pathways, such as pyroptosis, apoptosis, or necroptosis. Instead, targeting key PANoptosome components can serve as a strategy to prevent this form of cell
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Subscription and Copyright Information Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-07-05
No Abstract
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GPCR-dependent and -independent arrestin signaling Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-06-20 Vsevolod V. Gurevich, Eugenia V. Gurevich
Biological activity of free arrestins is often overlooked. Based on available data, we compare arrestin-mediated signaling that requires and does not require binding to G-protein-coupled receptors (GPCRs). Receptor-bound arrestins activate ERK1/2, Src, and focal adhesion kinase (FAK). Yet, arrestin-3 regulation of Src family member Fgr does not appear to involve receptors. Free arrestin-3 facilitates
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Structures reveal how SGLT inhibitors work Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-06-18 Zejian Sun, Wenhao Cui, Lei Chen
Sodium glucose cotransporters (SGLTs) transport glucose against its concentration gradient by harnessing the electrochemical potential gradient of sodium ions. SGLT inhibitors are widely prescribed to treat diabetes and other conditions. Recent structural studies have uncovered how chemically diverse SGLT inhibitors bind and inhibit the transporter at the atomic level.
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Targeting GPX4 in ferroptosis and cancer: chemical strategies and challenges Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-06-11 Jiao Liu, Daolin Tang, Rui Kang
Selenoprotein glutathione peroxidase 4 (GPX4) serves as a crucial suppressor of oxidative stress-induced ferroptosis, making it an attractive target for disease therapy. Here, we discuss recent strategies and challenges associated with targeting GPX4 through covalent inhibitors, proteolysis targeting chimera (PROTAC) degraders, and cell-type-specific degraders in the context of cancer.
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A novel function of the M2 muscarinic receptor Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-06-08 Jürgen Wess, Liu Liu
The M2 muscarinic receptor (M2R) is a prototypic class A G protein-coupled receptor (GPCR). Interestingly, Fasciani et al. recently identified an internal translation start site within the M2 receptor mRNA, directing the expression of a C-terminal receptor fragment. Elevated during cellular stress, this polypeptide localizes to mitochondria where it inhibits oxidative phosphorylation.
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Multi-target drugs for Alzheimer's disease Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-06-09 Bengisu Turgutalp, Caghan Kizil
Alzheimer's disease (AD), a leading cause of dementia, increasingly challenges our healthcare systems and society. Traditional therapies aimed at single targets have fallen short owing to the complex, multifactorial nature of AD that necessitates simultaneous targeting of various disease mechanisms for clinical success. Therefore, targeting multiple pathologies at the same time could provide a synergistic
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Implications of innate immune sexual dimorphism for MASLD pathogenesis and treatment Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-06-08 Richell Booijink, Prakash Ramachandran, Ruchi Bansal
Growing evidence suggests that metabolic dysfunction-associated steatotic liver disease (MASLD) is significantly higher in men versus women. Increased prevalence is observed in postmenopausal women, suggesting that age and sex (hormones) influence MASLD development and progression. Molecular data further reveal that sex regulates the innate immune responses with an essential role in MASLD progression
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Targeting extranuclear histones to alleviate acute and chronic inflammation Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-06-08 Gerry A.F. Nicolaes, Oliver Soehnlein
Extracellular histones instigate an inflammatory triad – centered on cytotoxicity, immune cell stimulation, and coagulation – ultimately shaping the dynamics and outcome of various inflammatory pathologies. Given the virtual absence of beneficial functions of histones in the extracellular space, in recent years a number of interference strategies have emerged. In this review we summarize pathogenic
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Subscription and Copyright Information Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-06-06
No Abstract
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Artificial protein coronas: directing nanoparticles to targets Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-05-28 Giulio Caracciolo
The protein corona surrounding nanoparticles (NPs) offers exciting possibilities for targeted drug delivery. However, realizing this potential requires direct evidence of corona–receptor interactions in vivo; a challenge hampered by the limitations of in vitro settings. This opinion proposes that utilizing engineered protein coronas can address this challenge. Artificial coronas made of selected plasma
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Emerging paradigms and recent progress in targeting ErbB in cancers Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-05-25 Nicolas Stoup, Maxime Liberelle, Nicolas Lebègue, Isabelle Van Seuningen
The epidermal growth factor receptor (EGFR) family is a class of transmembrane proteins, highly regarded as anticancer targets due to their pivotal role in various malignancies. Standard cancer treatments targeting the ErbB receptors include tyrosine kinase inhibitors (TKIs) and monoclonal antibodies (mAbs). Despite their substantial survival benefits, the achievement of curative outcomes is hindered
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Anticancer drugs: How to select small molecule combinations? Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-05-22 Ruth Nussinov, Bengi Ruken Yavuz, Hyunbum Jang
Small molecules are at the forefront of anticancer therapies. Successive treatments with single molecules incur drug resistance, calling for combination. Here, we explore the tough choices oncologists face – not just which drugs to use but also the best treatment plans, based on factors such as target proteins, pathways, and gene expression. We consider the reality of cancer’s disruption of normal
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Defeating MYC with drug combinations or dual-targeting drugs Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-05-22 Philip E. Thompson, Jake Shortt
Members of the MYC family of proteins are a major target for cancer drug discovery, but the development of drugs that block MYC-driven cancers has not yet been successful. Approaches to achieve success may include the development of combination therapies or dual-acting drugs that target MYC at multiple nodes. Such treatments hold the possibility of additive or synergistic activity, potentially reducing
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TNIK’s emerging role in cancer, metabolism, and age-related diseases Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-05-21 Collin Y. Ewald, Fadi E. Pulous, Sarah Wing Yan Lok, Frank W. Pun, Alex Aliper, Feng Ren, Alex Zhavoronkov
Traf2- and Nck-interacting kinase (TNIK) has emerged as a key regulator of pathological metabolic signaling in several diseases and is a promising drug target. Originally studied for its role in cell migration and proliferation, TNIK possesses several newly identified functions that drive the pathogenesis of multiple diseases. Specifically, we evaluate TNIK’s newfound roles in cancer, metabolic disorders
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Tackling therapy resistance in cancer Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-05-21 Jerry C. Madukwe
No Abstract
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Parvalbumin interneuron cell-to-network plasticity: mechanisms and therapeutic avenues Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-05-18 Michael D. Hadler, Henrik Alle, Jörg R.P. Geiger
Alzheimer’s disease (AD) and schizophrenia (SCZ) represent two major neuropathological conditions with a high disease burden. Despite their distinct e…
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Emerging targets in lipid metabolism for cancer therapy Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-05-17 Alexander R. Terry, Nissim Hay
Cancer cells perturb lipid metabolic pathways for a variety of pro-tumorigenic functions, and deregulated cellular metabolism is a hallmark of cancer cells. Although alterations in lipid metabolism in cancer cells have been appreciated for over 20 years, there are no FDA-approved cancer treatments that target lipid-related pathways. Recent advances pertaining to cancer cell fatty acid synthesis (FAS)
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Directions to overcome therapy resistance in cancer Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-05-16 Ruth Nussinov, Thomas Weichhart, Zodwa Dlamini, Don L. Gibbons, Isabelle Van Seuningen, Jessica Konen, Huai-Qiang Ju
No Abstract
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Eflornithine for treatment of high-risk neuroblastoma Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-05-14 Jianxiong Jiang, Ying Yu
No Abstract
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Immune checkpoint blockade resistance in lung cancer: emerging mechanisms and therapeutic opportunities Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-05-13 Jessica M. Konen, Haoyi Wu, Don L. Gibbons
Immune checkpoint blockade (ICB) therapy works by inhibiting suppressive checkpoints that become upregulated after T cell activation, like PD-1/PD-L1 and CTLA-4. While the initial FDA approvals of ICB have revolutionized cancer therapies and fueled a burgeoning immuno-oncology field, more recent clinical development of new agents has been slow. Here, focusing on lung cancer, we review the latest research
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Enhancing oncogenic signaling to kill cancer cells Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-05-10 Maxim Noeparast, Oleg Timofeev, Martin Pichler
Cancer-targeted therapies that inhibit oncogenic signaling often lead to resistance and recurrence. In a recent study, propose activating oncogenic pathways and inducing replication stress, resulting in cell death and tumor-suppressive mechanisms in colorectal cancer (CRC). This approach could spark a new wave of target discovery, and drug development and repurposing against cancer.
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Peptide libraries: from epitope mapping to in-depth high-throughput analysis Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-05-08 Debora Iaculli, Steven Ballet
Peptide arrays are a valuable instrument in the characterization of protein–protein interactions (PPIs) and immunogenic regions. New methods were developed to exploit the high-throughput potential of peptide arrays to obtain more in-depth information, replacing traditional resource-intensive experiments. Here, we discuss the recent advances in peptide-array-based technologies and the remaining challenges
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Potential for targeting small heat shock protein modifications Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-05-03 Binyou Wang, Matthew R. Pratt
Small heat shock proteins (sHSPs) play key roles in cellular stress and several human diseases. The direct effects of some post-translational modifications (PTMs) on certain sHSPs have been characterized, raising the possibility that small molecules could be used to modulate these modifications and indirectly up- or downregulate sHSP activity.
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Subscription and Copyright Information Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-05-02
No Abstract
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Malolactone strikes: K-Ras-G12D's Achilles' heel Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-04-22 Christos Adamopoulos, Kostas A. Papavassiliou, Athanasios G. Papavassiliou
In a recent study in , exploiting strain release by malolactone-based electrophiles designed a first-in-class covalent inhibitor that targets the elusive aspartate of the Kirsten rat sarcoma viral oncogene homolog (K-Ras)-G12D variant, which is highly prevalent in pancreatic cancer. The compound drastically inhibited oncogenic signaling and tumor growth in preclinical K-Ras-G12D-mutant pancreatic cancer
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AML treatment: conventional chemotherapy and emerging novel agents Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-04-20 Mark Forsberg, Marina Konopleva
Acute myeloid leukemia (AML) is driven by complex mutations and cytogenetic abnormalities with profound tumoral heterogeneity, making it challenging to treat. Ten years ago, the 5-year survival rate of patients with AML was only 29% with conventional chemotherapy and stem cell transplantation. All attempts to improve conventional therapy over the previous 40 years had failed. Now, new genomic, immunological
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Heterobifunctional small molecules to modulate RNA function Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-04-18 Sandra Kovachka, Yuquan Tong, Jessica L. Childs-Disney, Matthew D. Disney
RNA has diverse cellular functionality, including regulating gene expression, protein translation, and cellular response to stimuli, due to its intricate structures. Over the past decade, small molecules have been discovered that target functional structures within cellular RNAs and modulate their function. Simple binding, however, is often insufficient, resulting in low or even no biological activity
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Electroceuticals: emerging applications beyond the nervous system and excitable tissues Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-04-18 Swarnalatha Balasubramanian, David A. Weston, Michael Levin, Devon Charles Cardoso Davidian
Electroceuticals have evolved beyond devices manipulating neuronal signaling for symptomatic treatment, becoming more precise and disease modulating and expanding beyond the nervous system. These advancements promise transformative applications in arthritis, cancer treatment, tissue regeneration, and more. Here, we discuss these recent advances and offer insights for future research.
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Direct in vivo CAR T cell engineering Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-04-12 Lauralie Short, Robert A. Holt, Pieter R. Cullis, Laura Evgin
T cells modified to express intelligently designed chimeric antigen receptors (CARs) are exceptionally powerful therapeutic agents for relapsed and refractory blood cancers and have the potential to revolutionize therapy for many other diseases. To circumvent the complexity and cost associated with broad-scale implementation of manufactured adoptive cell therapy products, alternative strategies to
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Frizzleds act as dynamic pharmacological entities Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-04-08 Gunnar Schulte, Magdalena M. Scharf, Julien Bous, Jan Hendrik Voss, Lukas Grätz, Pawel Kozielewicz
The Frizzled family of transmembrane receptors (FZD) belongs to the class F of G protein-coupled receptors (GPCRs). FZDs bind to and are activated by Wingless/Int1 (WNT) proteins. The WNT/FZD signaling system regulates crucial aspects of developmental biology and stem-cell regulation. Dysregulation of WNT/FZD communication can lead to developmental defects and diseases such as cancer and fibrosis.
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Targeting methionine metabolism in cancer: opportunities and challenges Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-04-05 Peng Bin, Chuanlong Wang, Hangchao Zhang, Yuqi Yan, Wenkai Ren
Reprogramming of methionine metabolism is a conserved hallmark of tumorigenesis. Recent studies have revealed mechanisms regulating methionine metabolism within the tumor microenvironment (TME) that drive both cancer development and antitumor immunity evasion. In this review article we summarize advancements in our understanding of tumor regulation of methionine metabolism and therapies in development
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Advisory Board and Contents Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-04-04
Abstract not available
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Subscription and Copyright Information Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-04-04
Abstract not available
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Genetically engineered loaded extracellular vesicles for drug delivery Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-03-19 Zuriñe Erana-Perez, Manoli Igartua, Edorta Santos-Vizcaino, Rosa Maria Hernandez
The use of extracellular vesicles (EVs) for drug delivery is being widely explored by scientists from several research fields. To fully exploit their therapeutic potential, multiple methods for loading EVs have been developed. Although exogenous methods have been extensively utilized, in recent years the endogenous method has gained significant attention. This approach, based on parental cell genetic
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Leveraging macrophage metabolism for anticancer therapy: opportunities and pitfalls Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-03-17 Piyal Saha, Paul Ettel, Thomas Weichhart
Tumor-associated macrophages (TAMs) constitute an important part of the tumor microenvironment (TME) that regulates tumor progression. Tumor-derived signals, hypoxia, and competition for nutrients influence TAMs to reprogram their cellular metabolism. This altered metabolic profile creates a symbiotic communication between tumor and other immune cells to support tumor growth. In addition, the metabolic
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Targeting Fks1 proteins for novel antifungal drug discovery Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-03-15 Vinit Kumar, Juan Huang, Yawen Dong, Ge-Fei Hao
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Hepatic mitochondrial reductive stress in the pathogenesis and treatment of steatotic liver disease Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-03-12 Mari J. Jokinen, Panu K. Luukkonen
Steatotic liver diseases (SLDs) affect one-third of the population, but the pathogenesis underlying these diseases is not well understood, limiting the available treatments. A common factor in SLDs is increased hepatic mitochondrial reductive stress, which occurs as a result of excessive lipid and alcohol metabolism. Recent research has also shown that genetic risk factors contribute to this stress
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Targeting mitochondrial dynamics and redox regulation in cardiovascular diseases Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-03-07 Mirza Ahmar Beg, Minqi Huang, Lance Vick, K.N. Shashanka Rao, Jue Zhang, Yiliang Chen
Accumulating evidence highlights the pivotal role of mitochondria in cardiovascular diseases (CVDs). Understanding the molecular mechanisms underlying mitochondrial dysfunction is crucial for developing targeted therapeutics. Recent years have seen substantial advancements in unraveling mitochondrial regulatory pathways in both normal and pathological states and the development of potent drugs. However
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Translational adaptation in breast cancer metastasis and emerging therapeutic opportunities Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-03-06 Siyu Chen, Albertas Navickas, Hani Goodarzi
Breast cancer’s tendency to metastasize poses a critical barrier to effective treatment, making it a leading cause of mortality among women worldwide. A growing body of evidence is showing that translational adaptation is emerging as a key mechanism enabling cancer cells to thrive in the dynamic tumor microenvironment (TME). Here, we systematically summarize how breast cancer cells utilize translational
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VMAT structures reveal exciting targets for drug development Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-02-29 Shimon Schuldiner, Lucy R. Forrest
Vesicular monoamine transporter (VMAT)-2 has a crucial role in the neurotransmission of biogenic amines. Recently, , , , and individually reported cryo-electron microscopy (EM) structures of human VMAT2, offering opportunities for developing improved therapeutics and deep insights into the functioning of this protein.
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Mitochondrial DNA competition: starving out the mutant genome Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-02-23 Antonella Spinazzola, Diego Perez-Rodriguez, Jan Ježek, Ian J. Holt
High levels of pathogenic mitochondrial DNA (mtDNA) variants lead to severe genetic diseases, and the accumulation of such mutants may also contribute to common disorders. Thus, selecting against these mutants is a major goal in mitochondrial medicine. Although mutant mtDNA can drift randomly, mounting evidence indicates that active forces play a role in the selection for and against mtDNA variants
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Histone lysine acetyltransferase inhibitors: an emerging class of drugs for cancer therapy Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-02-20 Jeffrey White, Frederick A. Derheimer, Kristen Jensen-Pergakes, Shawn O’Connell, Shikhar Sharma, Noah Spiegel, Thomas A. Paul
Lysine acetyltransferases (KATs) are a family of epigenetic enzymes involved in the regulation of gene expression; they represent a promising class of emerging drug targets. The frequent molecular dysregulation of these enzymes, as well as their mechanistic links to biological functions that are crucial to cancer, have led to exploration around the development of small-molecule inhibitors against KATs
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Recent advances in generative biology for biotherapeutic discovery Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-02-19 Marissa Mock, Christopher James Langmead, Peter Grandsard, Suzanne Edavettal, Alan Russell
Generative biology combines artificial intelligence (AI), advanced life sciences technologies, and automation to revolutionize the process of designing novel biomolecules with prescribed properties, giving drug discoverers the ability to escape the limitations of biology during the design of next-generation protein therapeutics. Significant hurdles remain, namely: (i) the inherently complex nature
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Alzheimer’s therapeutic development: shifting neurodegeneration to neuroregeneration Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-02-14 Miao-Kun Sun, Daniel L. Alkon
Alzheimer’s disease (AD), similar to AD-related dementias, is characterized by impaired/lost neuronal structures and functions due to a long progression of neurodegeneration. Derailed endogenous signal pathways and disease processes have critical roles in neurodegeneration and are pharmacological targets in inducing neuroregeneration. Pharmacologically switching/shifting the brain status from neurodegeneration
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Targeting chromosomal instability and aneuploidy in cancer Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-02-13 Sugandha Bhatia, Kum Kum Khanna, Pascal H.G. Duijf
Cancer development and therapy resistance are driven by chromosomal instability (CIN), which causes chromosome gains and losses (i.e., aneuploidy) and structural chromosomal alterations. Technical limitations and knowledge gaps have delayed therapeutic targeting of CIN and aneuploidy in cancers. However, our toolbox for creating and studying aneuploidy in cell models has greatly expanded recently.
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The role of NMR in advancing small molecule drug discovery Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-02-13 Leszek Poppe
Navigating the ever-evolving landscape of nuclear magnetic resonance (NMR) poses challenges for the industry. This work explores promising approaches that illuminate protein–ligand interactions in the context of structural dynamics, facilitating targeted drug discovery. I acknowledge existing limitations and highlight future opportunities, which may pave the way for broader NMR integration and faster
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Advances in inhibitor development targeting the PWWP domain Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-02-09 Yunyuan Huang, Yanxi Li, Jinrong Min
The PWWP domain binds to both histone and DNA of a nucleosome in a bivalent way. PWWP domain-containing proteins are involved in different biological processes, and their aberrant expression is implicated in various human diseases. Here, we discuss the recent developments and challenges in targeting the PWWP domain for therapeutic intervention.
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Advisory Board and Contents Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-02-01
Abstract not available
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Subscription and Copyright Information Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-02-01
Abstract not available
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Complex architecture of cardiac muscle thick filaments revealed Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-01-31 Pradeep K. Luther, Steve B. Marston
Muscle contraction is orchestrated by the well-understood thin filaments and the markedly complex thick filaments. Studies by . and , discussed here, have unravelled the structure of the mammalian heart thick filament in exquisite near-atomic detail and pave the way for understanding physiological modulation pathways and mutation-induced dysfunction and for designing potential drugs to modify defects
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The structure and function of olfactory receptors Trends Pharmacol. Sci. (IF 13.9) Pub Date : 2024-01-31 Chenyang Wu, Marc Xu, Junlin Dong, Wenqiang Cui, Shuguang Yuan
Olfactory receptors (ORs) form the most important chemosensory receptor family responsible for our sense of smell in the nasal olfactory epithelium. This receptor family belongs to the class A G protein-coupled receptors (GPCRs). Recent research has indicated that ORs are involved in many nonolfactory physiological processes in extranasal tissue, such as the brain, pancreas, and testes, and implies