How many kinases are druggable? A review of our current understanding
Biochem J. 2023 Aug 30;480(16):1331-1363. doi: 10.1042/BCJ20220217.ABSTRACTThere are over 500 human kinases ranging from very well-studied to almost completely ignored. Kinases are tractable and implicated in many diseases, making them ideal targets for medicinal chemistry campaigns, but is it possible to discover a drug for each individual kinase? For every human kinase, we gathered data on their citation count, availability of chemical probes, approved and investigational drugs, PDB structures, and biochemical and cellular assays. Analysis of these factors highlights which kinase groups have a wealth of information avail...
Source: The Biochemical Journal - August 29, 2023 Category: Biochemistry Authors: Brian Anderson Peter Rosston Han Wee Ong Mohammad Anwar Hossain Zachary W Davis-Gilbert David H Drewry Source Type: research
How many kinases are druggable? A review of our current understanding
Biochem J. 2023 Aug 30;480(16):1331-1363. doi: 10.1042/BCJ20220217.ABSTRACTThere are over 500 human kinases ranging from very well-studied to almost completely ignored. Kinases are tractable and implicated in many diseases, making them ideal targets for medicinal chemistry campaigns, but is it possible to discover a drug for each individual kinase? For every human kinase, we gathered data on their citation count, availability of chemical probes, approved and investigational drugs, PDB structures, and biochemical and cellular assays. Analysis of these factors highlights which kinase groups have a wealth of information avail...
Source: The Biochemical Journal - August 29, 2023 Category: Biochemistry Authors: Brian Anderson Peter Rosston Han Wee Ong Mohammad Anwar Hossain Zachary W Davis-Gilbert David H Drewry Source Type: research
How many kinases are druggable? A review of our current understanding
Biochem J. 2023 Aug 30;480(16):1331-1363. doi: 10.1042/BCJ20220217.ABSTRACTThere are over 500 human kinases ranging from very well-studied to almost completely ignored. Kinases are tractable and implicated in many diseases, making them ideal targets for medicinal chemistry campaigns, but is it possible to discover a drug for each individual kinase? For every human kinase, we gathered data on their citation count, availability of chemical probes, approved and investigational drugs, PDB structures, and biochemical and cellular assays. Analysis of these factors highlights which kinase groups have a wealth of information avail...
Source: The Biochemical Journal - August 29, 2023 Category: Biochemistry Authors: Brian Anderson Peter Rosston Han Wee Ong Mohammad Anwar Hossain Zachary W Davis-Gilbert David H Drewry Source Type: research
How many kinases are druggable? A review of our current understanding
Biochem J. 2023 Aug 30;480(16):1331-1363. doi: 10.1042/BCJ20220217.ABSTRACTThere are over 500 human kinases ranging from very well-studied to almost completely ignored. Kinases are tractable and implicated in many diseases, making them ideal targets for medicinal chemistry campaigns, but is it possible to discover a drug for each individual kinase? For every human kinase, we gathered data on their citation count, availability of chemical probes, approved and investigational drugs, PDB structures, and biochemical and cellular assays. Analysis of these factors highlights which kinase groups have a wealth of information avail...
Source: The Biochemical Journal - August 29, 2023 Category: Biochemistry Authors: Brian Anderson Peter Rosston Han Wee Ong Mohammad Anwar Hossain Zachary W Davis-Gilbert David H Drewry Source Type: research
How many kinases are druggable? A review of our current understanding
Biochem J. 2023 Aug 30;480(16):1331-1363. doi: 10.1042/BCJ20220217.ABSTRACTThere are over 500 human kinases ranging from very well-studied to almost completely ignored. Kinases are tractable and implicated in many diseases, making them ideal targets for medicinal chemistry campaigns, but is it possible to discover a drug for each individual kinase? For every human kinase, we gathered data on their citation count, availability of chemical probes, approved and investigational drugs, PDB structures, and biochemical and cellular assays. Analysis of these factors highlights which kinase groups have a wealth of information avail...
Source: The Biochemical Journal - August 29, 2023 Category: Biochemistry Authors: Brian Anderson Peter Rosston Han Wee Ong Mohammad Anwar Hossain Zachary W Davis-Gilbert David H Drewry Source Type: research
How many kinases are druggable? A review of our current understanding
Biochem J. 2023 Aug 30;480(16):1331-1363. doi: 10.1042/BCJ20220217.ABSTRACTThere are over 500 human kinases ranging from very well-studied to almost completely ignored. Kinases are tractable and implicated in many diseases, making them ideal targets for medicinal chemistry campaigns, but is it possible to discover a drug for each individual kinase? For every human kinase, we gathered data on their citation count, availability of chemical probes, approved and investigational drugs, PDB structures, and biochemical and cellular assays. Analysis of these factors highlights which kinase groups have a wealth of information avail...
Source: The Biochemical Journal - August 29, 2023 Category: Biochemistry Authors: Brian Anderson Peter Rosston Han Wee Ong Mohammad Anwar Hossain Zachary W Davis-Gilbert David H Drewry Source Type: research
How many kinases are druggable? A review of our current understanding
Biochem J. 2023 Aug 30;480(16):1331-1363. doi: 10.1042/BCJ20220217.ABSTRACTThere are over 500 human kinases ranging from very well-studied to almost completely ignored. Kinases are tractable and implicated in many diseases, making them ideal targets for medicinal chemistry campaigns, but is it possible to discover a drug for each individual kinase? For every human kinase, we gathered data on their citation count, availability of chemical probes, approved and investigational drugs, PDB structures, and biochemical and cellular assays. Analysis of these factors highlights which kinase groups have a wealth of information avail...
Source: The Biochemical Journal - August 29, 2023 Category: Biochemistry Authors: Brian Anderson Peter Rosston Han Wee Ong Mohammad Anwar Hossain Zachary W Davis-Gilbert David H Drewry Source Type: research
Cancer-associated somatic mutations in human phosphofructokinase-1 reveal a critical electrostatic interaction for allosteric regulation of enzyme activity
Biochem J. 2023 Aug 25:BCJ20230207. doi: 10.1042/BCJ20230207. Online ahead of print.ABSTRACTMetabolic reprogramming, including increased glucose uptake and lactic acid excretion, is a hallmark of cancer. The glycolytic "gatekeeper" enzyme phosphofructokinase-1 (PFK1), which catalyzes the step committing glucose to breakdown, is dysregulated in cancers. While altered PFK1 activity and expression in tumors have been demonstrated, little is known about the effects of cancer-associated somatic mutations. Somatic mutations in PFK1 inform our understanding of allosteric regulation by identifying key amino acid residues involved ...
Source: The Biochemical Journal - August 25, 2023 Category: Biochemistry Authors: Maria A Voronkova Heather L Hansen Madison P Cooper Jacob Miller Narayanasami Sukumar Werner J Geldenhuys Aaron Robart Bradley Webb Source Type: research
Seasonal cold induces divergent structural/biochemical adaptations in different skeletal muscles of Columba livia: Evidence for nonshivering thermogenesis in adult birds
Biochem J. 2023 Aug 25:BCJ20230245. doi: 10.1042/BCJ20230245. Online ahead of print.ABSTRACTBirds are endothermic homeotherms even though they lack the well-studied heat producing brown adipose tissue (BAT), found in several clades of eutherian mammals. Earlier studies in ducklings have demonstrated that skeletal muscle is the primary organ of nonshivering thermogenesis (NST) plausibly via futile calcium (Ca2+)-handling through ryanodine receptor (RyR) and sarco-endoplasmic reticulum Ca2+-ATPase (SERCA). However, recruitment of futile Ca2+-cycling in adult avian skeletal muscle has not been documented. Studies in mammals s...
Source: The Biochemical Journal - August 25, 2023 Category: Biochemistry Authors: Punyadhara Pani Gourabamani Swalsingh Sunil Pani Unmod Senapati Bijayashree Sahu Benudhara Pati Subhasmita Rout Naresh C Bal Source Type: research
The impact of climate change on maize chemical defenses
Biochem J. 2023 Aug 30;480(16):1285-1298. doi: 10.1042/BCJ20220444.ABSTRACTClimate change is increasingly affecting agriculture, both at the levels of crops themselves, and by altering the distribution and damage caused by insect or microbial pests. As global food security depends on the reliable production of major crops such as maize (Zea mays), it is vital that appropriate steps are taken to mitigate these negative impacts. To do this a clear understanding of what the impacts are and how they occur is needed. This review focuses on the impact of climate change on the production and effectiveness of maize chemical defens...
Source: The Biochemical Journal - August 25, 2023 Category: Biochemistry Authors: Jessica P Yactayo-Chang Anna K Block Source Type: research
Cancer-associated somatic mutations in human phosphofructokinase-1 reveal a critical electrostatic interaction for allosteric regulation of enzyme activity
Biochem J. 2023 Aug 25:BCJ20230207. doi: 10.1042/BCJ20230207. Online ahead of print.ABSTRACTMetabolic reprogramming, including increased glucose uptake and lactic acid excretion, is a hallmark of cancer. The glycolytic "gatekeeper" enzyme phosphofructokinase-1 (PFK1), which catalyzes the step committing glucose to breakdown, is dysregulated in cancers. While altered PFK1 activity and expression in tumors have been demonstrated, little is known about the effects of cancer-associated somatic mutations. Somatic mutations in PFK1 inform our understanding of allosteric regulation by identifying key amino acid residues involved ...
Source: The Biochemical Journal - August 25, 2023 Category: Biochemistry Authors: Maria A Voronkova Heather L Hansen Madison P Cooper Jacob Miller Narayanasami Sukumar Werner J Geldenhuys Aaron Robart Bradley Webb Source Type: research
Seasonal cold induces divergent structural/biochemical adaptations in different skeletal muscles of Columba livia: Evidence for nonshivering thermogenesis in adult birds
Biochem J. 2023 Aug 25:BCJ20230245. doi: 10.1042/BCJ20230245. Online ahead of print.ABSTRACTBirds are endothermic homeotherms even though they lack the well-studied heat producing brown adipose tissue (BAT), found in several clades of eutherian mammals. Earlier studies in ducklings have demonstrated that skeletal muscle is the primary organ of nonshivering thermogenesis (NST) plausibly via futile calcium (Ca2+)-handling through ryanodine receptor (RyR) and sarco-endoplasmic reticulum Ca2+-ATPase (SERCA). However, recruitment of futile Ca2+-cycling in adult avian skeletal muscle has not been documented. Studies in mammals s...
Source: The Biochemical Journal - August 25, 2023 Category: Biochemistry Authors: Punyadhara Pani Gourabamani Swalsingh Sunil Pani Unmod Senapati Bijayashree Sahu Benudhara Pati Subhasmita Rout Naresh C Bal Source Type: research
The impact of climate change on maize chemical defenses
Biochem J. 2023 Aug 30;480(16):1285-1298. doi: 10.1042/BCJ20220444.ABSTRACTClimate change is increasingly affecting agriculture, both at the levels of crops themselves, and by altering the distribution and damage caused by insect or microbial pests. As global food security depends on the reliable production of major crops such as maize (Zea mays), it is vital that appropriate steps are taken to mitigate these negative impacts. To do this a clear understanding of what the impacts are and how they occur is needed. This review focuses on the impact of climate change on the production and effectiveness of maize chemical defens...
Source: The Biochemical Journal - August 25, 2023 Category: Biochemistry Authors: Jessica P Yactayo-Chang Anna K Block Source Type: research
Cancer-associated somatic mutations in human phosphofructokinase-1 reveal a critical electrostatic interaction for allosteric regulation of enzyme activity
Biochem J. 2023 Aug 25:BCJ20230207. doi: 10.1042/BCJ20230207. Online ahead of print.ABSTRACTMetabolic reprogramming, including increased glucose uptake and lactic acid excretion, is a hallmark of cancer. The glycolytic "gatekeeper" enzyme phosphofructokinase-1 (PFK1), which catalyzes the step committing glucose to breakdown, is dysregulated in cancers. While altered PFK1 activity and expression in tumors have been demonstrated, little is known about the effects of cancer-associated somatic mutations. Somatic mutations in PFK1 inform our understanding of allosteric regulation by identifying key amino acid residues involved ...
Source: The Biochemical Journal - August 25, 2023 Category: Biochemistry Authors: Maria A Voronkova Heather L Hansen Madison P Cooper Jacob Miller Narayanasami Sukumar Werner J Geldenhuys Aaron Robart Bradley Webb Source Type: research
Seasonal cold induces divergent structural/biochemical adaptations in different skeletal muscles of Columba livia: Evidence for nonshivering thermogenesis in adult birds
Biochem J. 2023 Aug 25:BCJ20230245. doi: 10.1042/BCJ20230245. Online ahead of print.ABSTRACTBirds are endothermic homeotherms even though they lack the well-studied heat producing brown adipose tissue (BAT), found in several clades of eutherian mammals. Earlier studies in ducklings have demonstrated that skeletal muscle is the primary organ of nonshivering thermogenesis (NST) plausibly via futile calcium (Ca2+)-handling through ryanodine receptor (RyR) and sarco-endoplasmic reticulum Ca2+-ATPase (SERCA). However, recruitment of futile Ca2+-cycling in adult avian skeletal muscle has not been documented. Studies in mammals s...
Source: The Biochemical Journal - August 25, 2023 Category: Biochemistry Authors: Punyadhara Pani Gourabamani Swalsingh Sunil Pani Unmod Senapati Bijayashree Sahu Benudhara Pati Subhasmita Rout Naresh C Bal Source Type: research
